Search Result
Results for "
Rats
" in MedChemExpress (MCE) Product Catalog:
8
Biochemical Assay Reagents
19
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-131929
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NO Synthase
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Inflammation/Immunology
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AE-ITU dihydrobromide is the dihydrobromide form of AE-ITU. AE-ITU dihydrobromide is a selective inhibitor for inducible NO synthase (iNOS), and attenuates the liver dysfunction caused by endotoxaemia in rats .
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- HY-162345
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Others
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Cardiovascular Disease
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CK-963 is an activator for cardiac troponin (cTnC) with Ki of 11.5 μM. CK-963 exhibits activity in enhancing cardiac contractility in Sprague-Dawley rats .
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- HY-116239
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- HY-126021
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Cholinesterase (ChE)
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Neurological Disease
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Mobam is a insecticide against Anoplura Pediculidae. Mobam inhibits cholinesterase (ChE) levels in rats plasma, erythrocytes, and brain, suppresses the avoidance behavior in rats .
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- HY-161942
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PCSK9
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Metabolic Disease
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PCSK9-IN-31 (Compound WX002) is an orally active PCSK9 inhibitor. PCSK9-IN-31 can lower low-density lipoprotein cholesterol (LDL-C) and total cholesterol (TC) in high cholesterol fed model rats .
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- HY-105128
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WIN 32729
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Others
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Endocrinology
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Epostane (WIN 32729) is an orally active inhibitor for 3β-hydroxysteroid dehydrogenase, with IC50 of 1.45 nM. Epostane blocks ovulation and pregnancy in rats .
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- HY-N4209
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Others
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Cardiovascular Disease
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3α-Dihydrocadambine is a natural product isolated from the heartwoods of Anthocephalus cadamba.3α-Dihydrocadambine exhibits dose-dependent hypotensive and anti-hypertensive effects in anesthetized normotensive rats and in conscious spontaneously hypertensive rats .
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- HY-131528
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CAS 997
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Others
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Neurological Disease
Metabolic Disease
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Tenilsetam (CAS 997) is an antidementia compound. Tenilsetam is an advanced glycation end product (AGE) inhibitor. Tenilsetam inhibits early retinopathy in experimental diabetes rats .
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- HY-114690
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BVT.3531
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Potassium Channel
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Neurological Disease
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PNU-140975 (BVT.3531) is a novel and potent bioactive compound. PNU-140975 can reduce body weight and activates KATP channel in isolated arcuate neurons in rats .
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- HY-15402
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BMS 207940
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Endothelin Receptor
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Cardiovascular Disease
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Edonentan (BMS 207940) is an antagonist for endothelin receptor (ETA receptor), with a Ki of 10 pM. Edonentan is metabolic stable, exhibits good pharmakokinetic characters in rats. Edonentan regulates the endothelin system, blocks the big Endothelin-induced pressor response in rats model .
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- HY-W116576
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Others
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Cancer
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3-Methoxycatechol is intermediate for the antivascular agents combretastatin A-1 (HY-121993) and combretastatin B-1. 3-Methoxycatechol promotes esophageal carcinogenesis in rats models .
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- HY-D1005A6
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PEG-PPG-PEG, 2200 (Averag)
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Biochemical Assay Reagents
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Others
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Poloxamer 124 L44 is block polymer of polyoxyethylene and polyoxypropylene with average molecular mass of 2200. Poloxamer 124 L44 reveals toxicity with an oral LD50 of 5 g/kg in albino rats. Poloxamer 124 L44 causes ocular irritation. Poloxamer 124 L44 forms thermoreversible hydrogel, that is utilized in food additives, drug delivery carriers in cosmetics, pharmaceutical ingredients and tissue engineering .
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- HY-105090
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5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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Lerisetron is a potent 5-HT3 antagonists and possess high-affinity binding for the 5-HT3 receptors with pKi value of 9.2. Lerisetron has a potent ability to inhibit the 5-HT-evoked reflex bradycardia in urethane-anesthetized rats .
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- HY-120276
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GR3027
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GABA Receptor
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Neurological Disease
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Golexanolone is a GABAA receptor modulating steroid antagonist. Golexanolone reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in hyperammonemic rats .
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- HY-116183
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HCV
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Infection
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ITX 4520 is an orally active and potent hepatitis C virus entry inhibitor exhibiting an excellent PK profile in both rats and dogs .
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- HY-129706
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Others
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Cardiovascular Disease
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LY127210 (free base) is a potent vasodilator with antihypertensive effects that reduces pressure in chloralose-anesthetized spontaneously hypertensive rats primarily by direct arteriolar dilation and to a lesser extent by decreasing cardiac output. LY127210 (free base) reduces blood pressure, heart rate and left ventricular end-diastolic pressure in hypertensive rats by reducing vascular resistance .
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- HY-113555
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- HY-122063
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NO Synthase
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Inflammation/Immunology
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FR260330 is a selective, orally active inhibitor for inducible nitric oxide synthase (iNOS) through suppression of iNOS dimerization. FR260330 inhibits the NO accumulation in rat splenocytes and human DLD-110 cells, with IC50 of 27 and 10 nM. FR260330 ameliorates the Lipopolysaccharides (HY-D1056)-induced inflammatory diseases in rats model .
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- HY-115597
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Calcium Channel
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Neurological Disease
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BTT-266 is an antagonist forcalcium channel, through suppression of the CaVα1-AID-CaVβ3 interaction, with a Ki of 1.4 μM. BTT-266 modulates the activation of voltage-dependent CaV2.2. BTT-266 exhibits analgesic efficacy against neuropathic pain in rats model .
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- HY-125047
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UK 3557
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Monoamine Oxidase
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Neurological Disease
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Daledalin tosylate (UK 3557) has mono-amine oxidase inhibitory activity in vitro, probably by acting as a substrate. Daledalin tosylate also has antidepressant effects. Daledalin tosylate potentiates amphetamine-induced excitation in rats, antagonises Reserpine (HY-N0480)-hypothermia in mice, tetrabenazine-sedation in rats and Reserpine (HY-N0480)- and Tetrabenazine (HY-B0590)-induced ptosis in mice with . Daledalin tosylate is proming for rasearch of depressive illness .
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- HY-106909A
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KAE-393
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5-HT Receptor
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Cardiovascular Disease
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YM114 is a highly potent and selective (5-HT)3-receptor antagonist that does not affect Veratridine (HY-N6691)- or electrical stimulation-induced bradycardia in anesthetized rats. YM114 inhibits 2-methyl-5-HT (HY-19358)-induced Bezold-Jarisch reflex, which originates from (5-HT)3-receptor located on the endings of vagal afferent nerves in the heart .
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- HY-161609
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Myosin
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Cardiovascular Disease
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Myosin modulator 2 (Compound B172) is a modulator for myosin, that inhibits ATPase in rabbits psoas, porcine atria and in porcine ventricle, with IC25s of 2.013, 2.94 and 20.93 μM, respectively. Myosin modulator 2 regulates systolic cardiac performance in Sprague Dawley rats .
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- HY-161608
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Myosin
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Cardiovascular Disease
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Myosin modulator 1 (Compound B141) is a modulator for myosin, that inhibits ATPase in rabbits psoas, porcine atria and in porcine ventricle, with IC25s of 0.42, 0.13 and 3.09 μM, respectively. Myosin modulator 1 regulates systolic cardiac performance in Sprague Dawley rats .
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- HY-11098
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R170591
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RSV
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Infection
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JNJ 2408068 is a potent RSV (respiratory syncytial virus) inhibitor. JNJ 2408068 significantly inhibits replication of RSV A and B subtypes in the lungs of cotton rats without any evidence of toxicity. The minimum protective dose of JNJ 2408068 appears to be approximately 0.39 mg/kg .
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- HY-144801A
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Potassium Channel
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Cardiovascular Disease
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DDO-02005 is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine .
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- HY-15018A
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Oxytocin Receptor
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Endocrinology
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SSR126768A free base is an orally active antagonist for oxytocin receptor, with Ki of 0.44 nM. SSR126768A free base is a tocolytic agent, that antagonizes the Oxytocin (HY-17571)-induced intracellular Ca 2+ increase and prostaglandin release in human uterine smooth muscle cells, inhibits thus the Oxytocin (HY-17571)-induced uterine contraction and delays parturition in pregnant rats in labor .
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- HY-160921
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SL65.0155 free base
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5-HT Receptor
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Neurological Disease
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Capeserod (SL65.0155 free base) is an agonist for serotonin receptor (5-HT receptor), with a Ki of 0.6 nM for 5-HT4 receptor. Capeserod enhances expression of phopshorilated cAMP-response element binding protein (p-CREB), vascular endothelium growth factor (VEGF), brain-derived neurotrophic factor (BDNF) and B cell lymphoma-2 (Bcl-2) proteins in hippocampus, and exhibits antidepressant-like efficacy in Wistar rats models .
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- HY-144801
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Potassium Channel
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Cardiovascular Disease
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DDO-02005 (free base) is a potent Kv1.5 potassium channel inhibitor with an IC50 value of 0.72 μM. DDO-02005 (free base) has good anti-atrial fibrillation (AF) effect in CaCl2-ACh AF rats model and effective anti-arrhythmic activity caused by aconitine .
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- HY-154795
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Caspase
NOD-like Receptor (NLR)
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Inflammation/Immunology
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Magnesium isoglycyrrhizinate hydrate is the active component found in licorice plant (Glycyrrhiza glabra). Magnesium isoglycyrrhizinate hydrate exhibits anti-inflammatory activity through NLRP3 inflammasome pathway, and attenuates the chronic obstructive pulmonary disease in rats .
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- HY-163455
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HCN Channel
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Neurological Disease
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pan-HCN-IN-1 (Compound J&J12e) is an inhibitor for hyperpolarization-activated and cyclic-nucleotide-gated 1 (HCN1) ion channel, with IC50 of 58 nM. pan-HCN-IN-1 reduces the voltage sag response and enhances EPSP summation in ex vivo rats brain slices .
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- HY-159624
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GABA Receptor
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Neurological Disease
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KK-92A, a blood-brain barrier penetrated GABAB positive allosteric modulator (PAM), suppresses alcohol self-administration and cue-induced reinstatement of alcohol seeking in rats .
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- HY-P3662
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Tyrosinase
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Cancer
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Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2 is a melanotropin, a melanocyte-stimulating hormone. Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2 stimulates tyrosinase and exhibits thermoregulatory effect in rats model .
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![Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2](//file.medchemexpress.eu/product_pic/hy-p3662.gif)
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- HY-W013989
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Epoxide Hydrolase
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Cardiovascular Disease
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1,3-Dicyclohexylurea (DCU) is an orally active and potent sEH (soluble epoxide hydrolase) inhibitor. Oral Delivery of 1,3-Dicyclohexylurea nanosuspension enhances exposure and lowers blood pressure in hypertensive Rats .
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- HY-126758
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Apoptosis
Glutathione Peroxidase
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Inflammation/Immunology
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Ludartin a sesquiterpene lactone, which can be isolated from the plant Artemisia carruthii Wood. Ludartin reduces the expression of myeloperoxidase and malondialdehyde, enhances the expression of glutathione and superoxide dismutase in spinal cord tissue. Ludartin inhibits neuronal apoptosis. Ludartin inhibits the upregulation of tumor necrosis factor-α, interleukin-1β, and interleukin-6. Ludartin improves the motor function of rats with spinal cord injury .
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- HY-158090
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Others
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Cancer
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Triptolide palmitate is the derivative of Triptolide (HY-32735). Triptolide palmitate exhibits cytotoxicity against cancer cell MCF-7 and A549, with IC50 of 7.5 and 6.4 μM. Triptolide palmitate exhibits a half-time T1/2 of 50.4 min in Sprague Dawley rats. Triptolide palmitate can be utilizd as drug carrier .
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- HY-116680
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5-HT Receptor
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Cardiovascular Disease
Neurological Disease
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LY53857 is a potent antagonist of vasoconstriction and serotonin-mediated 5-HT2 receptors. LY53857 did not reduce mean arterial blood pressure in spontaneously hypertensive rats (SHR) at doses that blocked the depressor response to serotonin and blocked central serotonin receptors. In addition, LY53857 was able to enhance neurotransmitter release in rat vas deferens and guinea pig ileal nerves .
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- HY-129639
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DL-204-IT
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Others
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Others
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L11204 (DL-204-IT) is a potent inhibitor of prostaglandin metabolism. L11204 inhibits PMS-induced superovulation and reduced the number of recoverable ova in the oviducts of hamsters. L11204 also inhibits chorionic gonadotrophin-induced ovarian hypertrophy and steroidogenesi in rats. L11204 is promising for research of reproductive system disorders .
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- HY-114527
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Apoptosis
Stearoyl-CoA Desaturase (SCD)
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Cancer
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TPMP-I-2 is an anticancer agent that induces cancer cell lines Apoptosis and decreases protein levels of stearoyl-CoA desaturase. TPMP-I-2 prolongs the survival time of nude rats in a simulated micrometastatic cervical cancer model and reduces tumor growth in a breast cancer model in nude mice combined with immunotoxins .
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- HY-151138
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Glucosidase
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Metabolic Disease
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α-Glucosidase-IN-16 is a potent and orally active α-glucosidase inhibitor with an IC50 value of 3.28 μM. α-Glucosidase-IN-16 can reduce the level of blood glucose in Streptozotocin-induced diabetic rats. Antidiabetic activity .
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- HY-123298
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Src
Akt
Apoptosis
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Cancer
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Chrysotoxine is a dual inhibitor of Src/Akt. Chrysotoxine suppresses cancer stem cells (CSCs) phenotypes by down-regulating Src/Akt signaling. Chrysotoxine reduces cell viability and increases apoptosis level in H460 and H23 cells instead of non-tumor cell lines. Chrysotoxine shows rapid excretion and low bioavailability in rats. Chrysotoxine is used in cancer research .
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- HY-B0747
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EPA ethyl ester; Ethyl eicosapentaenoate; AMR101
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Endogenous Metabolite
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Metabolic Disease
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Eicosapentaenoic acid ethyl ester (EPA ethyl ester) is an orally active ω-3 fatty acid agent. Eicosapentaenoic acid ethyl ester could improve the activity of liver β-oxidase in vitro, reduce the level of liver total triglyceride, increase the content of liver triglyceride and phospholipid ω-3 fatty acid, and increase the total ω-3 fatty acid level in rats .
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- HY-113695
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Angiotensin-converting Enzyme (ACE)
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Others
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BW A575C is a dual inhibitor against angiotensin converting enzyme (ACE) and β-adrenoceptor. BW A575C produces a competitive blockade of Isoprenaline (HY-108353)-induced tachycardia in a guinea-pig right atrial. BW A575C also inhibits Angiotensin I (HY-P1032)-induced pressor responses in rats. BW A575C is promising for research of hypertensive diseases .
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- HY-116262
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Phosphodiesterase (PDE)
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Cardiovascular Disease
Inflammation/Immunology
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SCH 51866 is a potent, selective and orally active inhibitor of PDE1 (IC50=70 nM) and PDE5 (IC50=60 nM). SCH 51866 inhibits collagen-induced aggregation of human washed platelets (IC50=10 μM), prevents neointimal formation in balloon catheter-injured carotid arteries of spontaneously hypertensive rats (SHR), and reduces blood pressure in SHR. SCH 51866 can be used in the study of hypertension .
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- HY-160602
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Free Fatty Acid Receptor
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Metabolic Disease
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CPL207280 is an orally active GPR40/FFA1 agonist with an antidiabetic effect. CPL207280 can effectively enhance glucose-stimulated insulin secretion and improve glucose tolerance in MIN6 pancreatic β-cells as well as in healthy Wistar Han rats and diabetic rat models. CPL207280 can be used for the research of type 2 diabetes .
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- HY-150700
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ERK
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Metabolic Disease
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RLX-33 is a potent, selective and blood-brain barrier (BBB) penetrant relaxin family peptide 3 (RXFP3) antagonist, also blocks relaxin-3-induced ERK1/2 phosphorylation, with IC50 values of 2.36 μM for RXFP3, 7.82 and 13.86 μM for ERK1 and ERK2 phosphorylation, respectively. RLX-33 can block the stimulation of food intake induced by the RXFP3-selective agonist R3/I5 in rats. RLX-33 can be used for the research of metabolic syndrome .
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- HY-16219
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Gd-EOB-DTPA disodium; ZK 139834
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Biochemical Assay Reagents
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Cancer
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Gadoxetate (Gd-EOB-DTPA) Disodium is a contrast agent in magnetic resonance imaging (MRI) of the hepatobiliary system, which accumulates in normal, functioning hepatocytes. Gadoxetate Disodium aggravates liver fibrosis (LF) induced gadolinium deposition in the liver and deep cerebellar nuclei (DCN) of rats without significant acute histological alterations. Gadoxetate Disodium is used to evaluate focal liver lesions, such as hepatocellular carcinoma or dysplastic nodules .
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- HY-14939A
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Histamine Receptor
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Inflammation/Immunology
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Vapitadine hydrochloride (Compound 3a) is a selective, orally active and nonsedating antihistamine agent, which exhibits a good binding affinity with human cloned histamine H1 receptor with a Ki of 19 nM. Vapitadine hydrochloride decreases the histamine-induced lethality (ED50 is 0.056-1.2 mg/kg), antagonizes the cutaneous reactions to histamine (ED50 is 0.51-1.4 mg/kg) in rats .
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- HY-105294
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Dopamine Receptor
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Others
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FR 64822 is a dopamine D2 receptor agonist that can induce antinociceptive activity in rats and mice by indirectly stimulating dopamine D2 receptors. FR 64822 can promote penile erection in juvenile rats and improve amnesia in rats induced by scopolamine during passive avoidance tasks .
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- HY-B1331
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Cyromazin; CGA-72662
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Endogenous Metabolite
Parasite
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Neurological Disease
Metabolic Disease
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Cyromazine (CGA-72662) is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects. Cyromazine reduced the number of germ cells by interfering with the Ecdysone (HY-N0179) signaling pathway. Cyromazine induces renal toxicity attenuated and restored by green tea extract in rats .
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- HY-W250580
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Biochemical Assay Reagents
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Others
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Dimethicone is an orally active biochemical assay reagents consisting of a fully methylated linear siloxane polymer whose ends are blocked by trimethylsiloxane units. Dimethicone can lubricate hair and physically block the respiratory system of lice to remove lice. Dimethicone has potential applications in cosmetics and daily cleaning products .
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- HY-B1331R
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Endogenous Metabolite
Parasite
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Neurological Disease
Metabolic Disease
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Cyromazine (Standard) is the analytical standard of Cyromazine. This product is intended for research and analytical applications. Cyromazine (CGA-72662) is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects. Cyromazine reduced the number of germ cells by interfering with the Ecdysone (HY-N0179) signaling pathway. Cyromazine induces renal toxicity attenuated and restored by green tea extract in rats .
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- HY-B1984
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4,4'-DDD; p,p'-Dichlorodiphenyl dichloroethane
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Drug Metabolite
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Others
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p,p'-DDD is a major metabolite of p,p'-DDT. p,p'-DDD occurs in the feces and livers of rats, that are given p,p'-DDT by stomach tube, but not of rats injected intraperitoneally with p,p'-DDT .
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- HY-120481
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FAAH
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Neurological Disease
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JNJ-40413269 is an inhibitor for FAAH, that inhibits human FAAH and rats FAAH with IC50 of 28 nM and 270 nM. JNJ-40413269 exhibits analgesic efficacy in rat spinal nerve ligation model and exhibits good pharmacokinetic characteristics in rats .
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- HY-B0962
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mAChR
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Neurological Disease
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Piperidolate hydrochloride is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs).
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- HY-B0962A
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mAChR
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Neurological Disease
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Piperidolate is an antimuscarinic, inhibits intestinal cramp induced by acetylcholine (rats and dogs).
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- HY-W096159
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Endogenous Metabolite
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Metabolic Disease
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D-Biotinol is the nutrition of Lactobacillus arabinosus, L. casei, or Saccharomyces cerevisiae. D-Biotinol replaces the D-biotin (HY-B0511) in saving egg white induced biotin deficiency in rats. D-Biotinol is orally active and displays to be converted to biotin by rats .
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- HY-N1115
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(+)-Tubotaiwine; NSC 306222; Tubotaiwin
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Others
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Cardiovascular Disease
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Tubotaiwine ((+)-Tubotaiwine), an alkaloid, has beneficial effect on cadmium (Cd) induced hypertension in rats. Tubotaiwine regulates systolic, diastolic and mean arterial blood pressure of the Cd exposed rats. Tubotaiwine reduces arterial stiffness, inhibits of oxidative stress and increases vascular remodeling .
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- HY-B1978
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Fungal
Reactive Oxygen Species
Androgen Receptor
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Infection
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Iprodione is an orally active diformimide fungicide. Iprodione can specifically cause oxidative damage by producing free radicals (ROS). Iprodione is also an antiandrogen agent that delays adolescent development in rats and reduces sexual behavior and reproductive ability in rats .
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- HY-107482
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Nicotinoyl-GABA; Nicotinoyl-γ-aminobutyric acid
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GABA Receptor
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Neurological Disease
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Picamilon is an orally active derivative of γ-aminobutyric acid that has nootropic effect. Picamilon improves the epilepsy model in rats and promotes correction of functional disorders of the pancreas during Alloxan (HY-W017227)-induced diabetes mellitus in rats .
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- HY-P4296
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Amino Acid Derivatives
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Others
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H-Gly-Sar-Sar-OH is an orally active tripeptide. H-Gly-Sar-Sar-OH is transported through PepT1 within Caco-2 cells. H-Gly Sar Sar OH has potential applications in material transportation .
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- HY-161505
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Transthyretin (TTR)
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Others
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Transthyretin-IN-3 (compound 6) is a designed benzofuran analogue. Transthyretin-IN-3 selectively binds to plasma transthyretin (TTR) to inhibit Amyloid aggregation (IC50=5.0±0.2 μM). Transthyretin-IN-3 can bind to TTR's thyroxine binding site specifically by carrying chlorine substituents at specific locations in its structure. This binding can prevent TTR tetramers from dissociating into unstable monomers .
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- HY-W011873A
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C16:1(9Z); C16:1 n-7; (9Z)-Hexadecenoic acid
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Endogenous Metabolite
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Neurological Disease
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Palmitoleic acid sodium, a composition of fatty acid, is implicated in the prevention of death from cerebrovascular disorders in SHRSP rats.
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- HY-W011873
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- HY-121528
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- HY-109519
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Others
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Others
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Simethicone is an orally active defoamer. Simethicone reduces the surface tension of air bubbles in the gastrointestinal tract, causing them to be expelled by vomiting, exhalation or absorption into the bloodstream. Simethicone has potential applications in flatulence and colic .
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- HY-114761
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Prostaglandin Receptor
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Cardiovascular Disease
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Prostaglandin F2α dimethyl amine is a Prostaglandin F2α (HY-12956) derivative. Prostaglandin F2α dimethyl amine is an antagonist for Prostaglandin F receptor (FP) . Prostaglandin F2α dimethyl amine blocks the cardiovascular responses induced by orexin and Arachidonic acid (HY-109590) .
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- HY-113329
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Taurocyamine
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Endogenous Metabolite
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Metabolic Disease
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Guanidinoethyl sulfonate (Taurocyamine), a transport antagonist of taurine, induces much urinary taurine excretion with a resulting decrease in the tissue taurine content and readily produces taurine-deficient fetal rats in pregnant rats . Guanidinoethyl sulfonate, a structural analogue of taurine, acts as a competitive inhibitor of taurine transport .
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- HY-135761S
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Fungal
Cholinesterase (ChE)
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Infection
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Penconazole-d7 is the deuterium labeled Penconazole[1]. Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats[2][3].
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- HY-111081C
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Sigma Receptor
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Neurological Disease
|
|
(±)-PPCC oxalate is a sigma-1 agonist that mainly interacts with sigma-1 receptors with Ki of 1.5 nM. (±)-PPCC oxalate has effective anti-amnesia effects in rats with mild or severe cognitive impairment, and can improve the cognitive abilities of rats .
|
-
- HY-12586
-
|
|
Others
|
Others
|
|
AZD6564 is an orally active inhibitor for fibrinolysis through disruption of plasma kinase-fibrin interaction. AZD6564 dissolves human plasma clot with an IC50 of 0.44 μM. AZD6564 ameliorates hemorrhage in rats with EC50 of 1.62 μM, and exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-P0037
-
|
Org 30850ANT
|
Others
GnRH Receptor
|
Endocrinology
|
|
Org-30850 is a potent LHRH antagonist designed for treating hormone-dependent disorders. In animal studies, a single subcutaneous dose effectively inhibited ovulation in rats and significantly reduced testosterone levels in male rats for up to 48 hours post-administration. Daily doses of Org-30850 in female rats suppressed estrous cycles, decreased uterine and ovarian weights, and lowered estradiol and FSH serum levels. In male rats, prolonged treatment resulted in reversible reductions in gonadal function and testosterone levels, with almost complete recovery observed after cessation of treatment. Unlike comparable LHRH antagonists, Org-30850 exhibited minimal injection site irritation and no edematous reactions, suggesting a more favorable therapeutic profile .
|
-
- HY-100189
-
|
|
Others
|
Metabolic Disease
|
|
LS2265 is a taurine derivative of fenofibrate and can induce proliferation of peroxisomes in liver cells of rats.
|
-
- HY-119602
-
|
CI-911
|
Others
|
Neurological Disease
|
|
Rolziracetam is a nootropic agent of the racetam family and improves short-term memory in rats and monkeys .
|
-
- HY-N11503
-
|
|
Others
|
Inflammation/Immunology
|
|
Disialyllacto-N-tetraose is a human milk oligosaccharide that prevents necrotising enterocolitis in neonatal rats .
|
-
- HY-19005
-
-
- HY-B0476S
-
|
Acetophenetidin-d5
|
COX
|
Inflammation/Immunology
|
|
Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
|
-
- HY-107652
-
|
|
mAChR
|
Neurological Disease
|
|
AF-DX 384 is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
|
-
- HY-121550
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
ME3221 is an angiotensin AT1 receptor antagonist that effectively antagonizes the pressor response to angiotensin II in rats and marmosets without affecting the hypotensive response to bradykinin. It demonstrates potent antihypertensive effects in renal hypertensive rats and spontaneously hypertensive rats (SHR), with efficacy comparable to or better than losartan in vivo. ME3221's repeated administration in SHR results in sustained and stable hypotensive effects without affecting heart rate, indicating its potential for treating both renal and essential hypertension similarly to losartan .
|
-
- HY-145713
-
|
HBV-IN-19
|
HBV
|
Infection
|
|
GS-8873 is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 causes neurofunctional deficits in rats and cynomolgus monkeys .
|
-
- HY-117038
-
|
|
Others
|
Endocrinology
|
|
Anordiol is an antiestrogenic compound with weak estrogenic activity. It can reduce the parameters of uterine growth (including uterine wet weight, soluble protein content, and DNA content) induced by estradiol in rats and can also regulate the estrous cycle in rats. Anordiol holds potential application value in the research of antiestrogen-related diseases .
|
-
- HY-105495
-
-
- HY-129208
-
|
|
Antibiotic
Fungal
|
Infection
|
|
Viridicatumtoxin is a new mycotoxin extracted from Penicillium viridicatum with a LD50 of 122.4 mg/kg in rats.
|
-
- HY-106300
-
-
- HY-135222
-
|
5-Methoxy-6-methyl-2-aminoindan hydrochloride
|
5-HT Receptor
|
Neurological Disease
|
|
MMAI (5-Methoxy-6-methyl-2-aminoindan) hydrochloride is a selective serotonin releaser that does not produce psychoactive or hallucinogenic effects in the context of drug discrimination in rats. MMAI hydrochloride induces a behavioral syndrome in rats, including hypokinesia with freezing, spinning, Straub tail, flat posture, and reduced sleep time .
|
-
- HY-B0476S1
-
|
|
COX
|
Inflammation/Immunology
|
|
Phenacetin- 13C is the 13C labeled Phenacetin[1]. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[2][3][4].
|
-
- HY-118821
-
|
|
CRFR
|
Metabolic Disease
|
|
JTC-017, a specific corticotropin-releasing hormone receptor 1 antagonist, attenuates hippocampal noradrenaline release, visceral perception, adrenocorticotropic hormone release, and anxiety after acute colorectal distention in rats. JTC-017 blocks stress-induced changes in colonic motility after chronic colorectal distention in rats .
|
-
- HY-124223
-
|
|
mAChR
|
Neurological Disease
|
|
AF-DX 384 (methanesulfonate) is a selective antagonist of M2 and M4 muscarinic acetylcholine receptors (Kis=6.03 and 10 nM, respectively) . AF-DX 384 (methanesulfonate) reverses deficits in novel object recognition and passive avoidance in aged rats, as well as in young rats with impairments induced by scopolamine .
|
-
- HY-116927
-
-
- HY-144289
-
|
|
Glucokinase
|
Metabolic Disease
|
|
BMS-820132 is an orally active and partial glucokinase (GK) activator with a AC50 of 29 nM. BMS-820132 decreases the glucose levels in glucose tolerance test (OGTT) model in normal rats, but not Zucker diabetic fatty (ZDF) rats. BMS-820132 exhibits pharmacological toxicity secondary to strong GK activation .
|
-
- HY-B1984S
-
|
4,4'-DDD-d8; p,p'-Dichlorodiphenyl dichloroethane-d8
|
Drug Metabolite
|
Others
|
|
p,p'-DDD-d8 is the deuterium labeled p,p'-DDD[1]. p,p'-DDD is a major metabolite of p,p'-DDT. p,p'-DDD occurs in the feces and livers of rats, that are given p,p'-DDT by stomach tube, but not of rats injected intraperitoneally with p,p'-DDT[2][3].
|
-
- HY-B1984R
-
|
|
Drug Metabolite
|
Others
|
|
p,p'-DDD (Standard) is the analytical standard of p,p'-DDD. This product is intended for research and analytical applications. p,p'-DDD is a major metabolite of p,p'-DDT. p,p'-DDD occurs in the feces and livers of rats, that are given p,p'-DDT by stomach tube, but not of rats injected intraperitoneally with p,p'-DDT .
|
-
- HY-D1782
-
-
- HY-N9226
-
|
|
Others
|
Metabolic Disease
|
|
Glucocheirolin, a natural compound that can be isolated from Erysimum corinthium Boiss, possesses antinutritional and toxic effects in rats .
|
-
- HY-123440
-
-
- HY-B1978R
-
|
|
Fungal
Reactive Oxygen Species
Androgen Receptor
|
Infection
|
|
Iprodione (Standard) is the analytical standard of Iprodione. This product is intended for research and analytical applications. Iprodione is an orally active diformimide fungicide. Iprodione can specifically cause oxidative damage by producing free radicals (ROS). Iprodione is also an antiandrogen agent that delays adolescent development in rats and reduces sexual behavior and reproductive ability in rats .
|
-
- HY-164034
-
|
|
nAChR
|
Endocrinology
|
|
Ganglefene is a blocker for n-choline receptor, which leads to the sexual dysfunction in the offspring in adulthood, when administrated to pregnant rats .
|
-
- HY-117926
-
|
|
RAR/RXR
|
Cancer
|
|
AGN 191701 is a selective retinoic acid X receptor (RXR) agonist that causes liver enlargement in rats without hepatocellular necrosis .
|
-
- HY-N0300
-
|
DL-Tetrahydropalmatine
|
Dopamine Receptor
Apoptosis
|
Neurological Disease
|
|
Tetrahydropalmatine possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats .
|
-
- HY-119320
-
|
Aethimidinum
|
Others
|
Cancer
|
|
Ethimidine (Aethimidinum) can reduce the blood serum free SH (sulfhydryl) in in rats previously transplanted with sarcoma or carcinoma cells .
|
-
- HY-B1247
-
|
|
Endogenous Metabolite
|
Others
|
|
Protoporphyrin IX is a final intermediate in the heme biosynthetic pathway, which acts as a radiation sensitizer enhancing ROS generation even in a hypoxic state and inducing DNA damage. Protoporphyrin IX also acts as a photo sensitizer undergoing photobleaching that occurs through direct degradation by light irradiation. Protoporphyrin IX is formed and accumulated following 5-aminolevulinic acid (5-ALA) (HY-W000450) administration in the tumor cells of rats. Protoporphyrin IX causes selective improvement of basal cell carcinoma when activated red fluorescence of a peak wavelength at 405 nm. Protoporphyrin IX is promising for research of sonodynamic and photodynamic agents for a wide range of cancers, such as bladder cancer and nodular basal cell carcinoma .
|
-
- HY-B1448AS
-
|
|
Apoptosis
Calcium Channel
|
Cardiovascular Disease
|
|
(Rac)-Benidipine-d7 is the deuterium labeled Benidipine[1]. Benidipine is a potent and orally active calcium channel antagonist[2]. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells[3]. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats[4].
|
-
- HY-W012946S
-
|
|
Acyltransferase
ATP Citrate Lyase
Endogenous Metabolite
|
Metabolic Disease
|
|
2-Furoic acid-d3 is the deuterium labeled 2-Furoic acid[1]. 2-Furoic acid (Furan-2-carboxylic acid) is an organic compound produced through furfural oxidation[2]. 2-Furoic acid exhibits hypolipidemic effet, lowers both serum cholesterol and serum triglyceride levels in rats[3].
|
-
- HY-108667
-
|
|
P2X Receptor
|
Others
|
|
TNP-ATP triethylammonium is a selective P2X receptor antagonist. TNP-ATP triethylammonium shows antinociceptive effects in rats .
|
-
- HY-118370
-
-
- HY-114614
-
|
|
Parasite
|
Infection
|
|
Clenpirin is a insecticide against cattle ticks Boophilus microplus. Clenpirin exhibits slightly toxicity to rats with LD50 of 3050 mg/kg .
|
-
- HY-106043
-
|
Wy 40972
|
GnRH Receptor
|
Endocrinology
|
|
Lutrelin (Wy 40972) is a luteinizing hormone releasing hormone (LHRH) agonist. Lutrelin inhibits the growth of the endometrial expiant in rats .
|
-
- HY-14562
-
|
|
mAChR
|
Neurological Disease
|
|
TBPB is an allosteric M1 mAChR agonist(EC50=289 nM) that regulates amyloid processing and produces antipsychotic-like activity in rats.
|
-
- HY-W687496
-
|
Vitamin A acid methyl ester
|
Others
|
Others
|
|
Methyl retinoate (Vitamin A acid methyl ester) is a derivative of vitamin A. Methyl retinoate causes degenerative changes in the seminiferous tubules in Sprague Dawley rats .
|
-
- HY-A0117
-
|
Temocapril diacid; Temocaprilate; RS 5139
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Temocaprilat (Temocapril diacid) is an inhibitor of angiotensin-converting enzyme (ACE). Temocaprilat alleviates the inhibitory effect of high glucose on the proliferation of aortic endothelial cells. Temocaprilat has potential applications in hypertension and vascular inflammation .
|
-
- HY-106447
-
|
|
Others
|
Metabolic Disease
|
|
Losulazine is an antihypertensive agent acting by a sympatholytic mechanism. Losulazine's hypotensive activity depends on the presence of an intact, functional sympathetic nervous system .
|
-
- HY-116309
-
-
- HY-105583
-
|
|
Others
|
Others
|
|
Cloforex (Frenapyl) is an orally effective amphetamine-type anorexic and a precursor to Clophentermine. Cloforex can be used to induce foam cell accumulation in rats .
|
-
- HY-101749
-
-
- HY-U00013
-
|
HCT 1206; NO-flurbiprofen; Nitroxybutyl flurbiprofen
|
COX
|
Cardiovascular Disease
|
|
Nitroflurbiprofen is a cyclooxygenase (COX) inhibitor with nitric oxide (NO)-donating properties, modulates the increased intrahepatic vascular tone in portal hypertensive cirrhotic rats.
|
-
- HY-111634
-
|
|
Constitutive Androstane Receptor
|
Cancer
|
|
Epsilon-momfluorothrin is a type I synthetic pyrethroid insecticide, activates constitutive androstane receptor (CAR), and induces hepatocellular tumors in rats .
|
-
- HY-N0300A
-
|
DL-Tetrahydropalmatine hydrochloride
|
Dopamine Receptor
|
Neurological Disease
|
|
Tetrahydropalmatine (DL-Tetrahydropalmatine) hydrochloride possesses analgesic effects. Tetrahydropalmatine hydrochloride acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats .
|
-
- HY-137204
-
|
|
GABA Receptor
|
Neurological Disease
|
|
COR659 is a potent and effective GABAB positive allosteric modulator (PAM). COR659 suppresses alcohol and chocolate self-administration in rats .
|
-
- HY-W092533
-
|
|
Tryptophan Hydroxylase
|
Neurological Disease
|
|
6-Fluorotryptophan, a competitive inhibitor of tryptophan hydroxylase, produced a transient disruption of sleep in rats chronically implanted with EEG recording electrodes .
|
-
- HY-N11449
-
|
|
Others
|
Others
|
|
Nardoaristolone B, a non-sesquiterpene compound isolated from the root of Nardostachys jatamansi, has protective effects on cardiomyocyte injury in neonatal rats .
|
-
- HY-111327
-
|
|
Glucosidase
|
Metabolic Disease
|
|
Valibose is analpha-glucosidaseinhibitor, and ameliorates the metabolic disorder of glucose and lipids and the nephropathy in Streptozotocin (HY-13753)-induced diabetic rats .
|
-
- HY-75680
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
FaX-IN-1 (compound 11A) is an intermediate in the preparation of FaX inhibitors and was used to study the inhibitory activity against venous thrombosis in rats .
|
-
- HY-N2026S1
-
|
Propyl parahydroxybenzoate-d4; Propyl 4-hydroxybenzoate-d4
|
Apoptosis
Bacterial
Endogenous Metabolite
|
Infection
|
|
Propylparaben-d4 is the deuterium labeled Propylparaben[1]. Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats[2][3][4].
|
-
- HY-121598
-
|
SC-36602
|
Apoptosis
|
Cardiovascular Disease
|
|
Actisomide (SC-36602) is an antiarrhythmic agent. Absorption of actisomide in rats and its in vitro uptake in CaCo-2 cells are pH-dependent .
|
-
- HY-13056
-
|
|
Drug Metabolite
|
Neurological Disease
|
|
SMND-309 is a metabolite of salvianolic acid B, and exhibits neuroprotective effects in cultured neurons and in permanent middle cerebral artery occlusion rats .
|
-
- HY-B0099
-
|
MCI-186
|
MMP
Apoptosis
|
Neurological Disease
|
|
Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
|
-
- HY-W011873S
-
-
- HY-N7981
-
|
|
NF-κB
|
Neurological Disease
|
|
Pratensein, a flavonoid, ameliorates β-amyloid-induced cognitive impairment in rats via reducing oxidative damage and restoring synapse and BDNF levels .
|
-
- HY-W011873S1
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Palmitoleic acid-d13 is the deuterium labeled Palmitoleic acid. Palmitoleic acid, a composition of fatty acid, is implicated in the prevention of death from cerebrovascular disorders in SHRSP rats.
|
-
- HY-W011873S2
-
|
|
Endogenous Metabolite
|
Neurological Disease
|
|
Palmitoleic acid- 13C16 is the 13C labeled Palmitoleic acid. Palmitoleic acid, a composition of fatty acid, is implicated in the prevention of death from cerebrovascular disorders in SHRSP rats.
|
-
- HY-148158
-
-
- HY-103500
-
-
- HY-126848
-
-
- HY-W047156
-
|
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
Allantoxanamide is a uricase inhibitor. Allantoxanamide-induced rats serve as animal models for studying purine biosynthesis, drug-induced hyperuricemia and hyperuricosuria, and related nephropathy .
|
-
- HY-15402D
-
|
BMS 207940 hydrate
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Edonentan (BMS 207940) hydrate is a potent and selective antagonist of the endothelin A (ETA) receptor, with a Ki of 10 pM. In rats, Edonentan has superior (100%) oral bioavailbility .
|
-
- HY-145454A
-
|
(-)-3-PPP
|
Dopamine Receptor
|
Neurological Disease
|
|
Preclamol is a dopamine (DA) agonist with autoreceptor as well as postsynaptic receptor stimulatory properties. Preclamol inhibits the locomotor activity of mice and rats in low doses .
|
-
- HY-124399
-
|
|
Endogenous Metabolite
PPAR
|
Metabolic Disease
|
|
Peroxisome proliferator-activated receptors (PPARs) play an important role in regulating lipid and glucose metabolism, and oleoylethanolamide (OEA) is a natural ligand for PPARα. N-Octadecyl-N'-propyl-sulfamide is an analog of OEA and a potent activator of PPARα, with selective binding affinity for PPARα (EC50=100 nM, compared to 120 nM for OEA). N-Octadecyl-N'-propyl-sulfamide (10 mg/kg; ip) inhibits food intake and reduces body weight gain in rats. At a dose of 1 mg/kg, N-Octadecyl-N'-propyl-sulfamide induces satiety, thereby reducing food intake, body weight, and plasma triglyceride concentrations in free-feeding Wistar rats and obese Zucker (fa/fa) rats.
|
-
- HY-119540
-
|
|
Fungal
|
Infection
|
|
Furametpyr is a fungicide used to control rice sheath blight. Furametpyr exhibits a wide variety of metabolites in rats, through recombinant human cytochrome P450 .
|
-
- HY-121417
-
|
|
Others
|
Metabolic Disease
|
|
Laserpitin, a coumarin, increases serum HDL levels, especially apoE-HDL, and decreases the hepatic triglyceride content in stroke-prone spontaneously hypertensive rats (SHRSP) .
|
-
- HY-D0256A
-
|
Chlorazol Black E free acid; Ferristatin II; C.I. 30235 free acid
|
DNA/RNA Synthesis
|
Others
|
|
Direct Black 38 free acid is an azo dye. Direct Black 38 induces unscheduled DNA synthesis in liver and micronucleus in bone marrow of rats in vivo .
|
-
- HY-N7515
-
|
2',4',6'-Trihydroxychalcone
|
Bacterial
|
Inflammation/Immunology
|
|
Pinocembrin chalcone (2',4',6'-Trihydroxychalcone) is an antibacterial compound from Helichrysum Trilineatum. Pinocembrin chalcone can prevent gastric ulcers in rats .
|
-
- HY-19259
-
|
|
Adenosine Kinase
|
Neurological Disease
|
|
GP3269 is a potent, selective, and orally active inhibitor of human adenosine kinase (AK) with an IC50 of 11 nM. GP3269 exhibits anticonvulsant activity in rats .
|
-
- HY-105127
-
|
CGP 11305A hydrochloride
|
Monoamine Oxidase
|
Neurological Disease
|
Brofaromine (hydrochloride) is a monoamine oxidase A (MAO-A) inhibitor and a 5-HT uptake inhibitor. Brofaromine (hydrochloride) shows antidepressant-like activity in the social conflict test in rats .
|
-
- HY-145713A
-
|
HBV-IN-19 TFA
|
HBV
|
Infection
|
|
GS-8873 TFA is the TFA salt form of GS-8873 (HY-145713). GS-8873 TFA is an orally active inhibitor for the production of hepatitis B virus (HBV) surface antigen (HBsAg) with an EC50 of 4 nM. GS-8873 TFA exhibits good pharmacokinetic characters in rats and metabolic stability in human hepatocytes. GS-8873 TFA causes neurofunctional deficits in rats and cynomolgus monkeys .
|
-
- HY-159115
-
|
|
FABP
|
Metabolic Disease
|
|
ART26.12 is an orally active and selective FABP5 inhibitor. ART26.12 has a high oral bioavailability in rats and dogs .
|
-
- HY-100174
-
|
NSC294836
|
Others
|
Neurological Disease
|
|
W-2429 (NSC294836) is considerably more effective than acetylsalicylic acid in inhibiting carrageenan-induced edema and in reducing brewer's yeast-induced fever in rats .
|
-
- HY-P1742
-
|
|
Opioid Receptor
|
Metabolic Disease
|
|
Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats .
|
-
- HY-121565
-
|
|
Others
|
Metabolic Disease
Endocrinology
|
|
SaRI 59-801 is an orally effective hypoglycemic compound. SaRI 59-801 decreases blood glucose in several species and to elevate plasma insulin in rats and mice .
|
-
- HY-145454
-
|
(+)-3-PPP
|
Dopamine Receptor
|
Neurological Disease
|
|
(R)-Preclamol is a dopamine (DA) agonist with autoreceptor as well as postsynaptic receptor stimulatory properties. (R)-Preclamol inhibits the locomotor activity of mice and rats in low doses .
|
-
- HY-117774
-
|
|
Others
|
Neurological Disease
|
|
AHR-2244 hydrochloride is a bioactive agent that acts against psychosis and anxiety. It selectively blocks CAR in mice, rats, and cats, and can reduce the lethality associated with amphetamine .
|
-
- HY-124393
-
|
|
mGluR
|
Neurological Disease
|
|
GRN-529 is a negative allosteric modulator (NAM) for mGluR5. GRN-259 modulates sleep-wake activity, and exhibits anxiolytic efficacy in rats .
|
-
- HY-126800
-
|
|
Others
|
Inflammation/Immunology
|
|
Glycotriosyl glutamine is a synthetic analogue of the Glycopeptide. Glycotriosyl glutamine induces focal glomerulonephritis (FGN) and the appearance of myeloid bodies in the epithelial cells of the podocytes in rats with nephritogenic activity .
|
-
- HY-105412A
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
RU 52583 is an oral bioactive antagonist of alpha 2-adrenergic receptor. RU 52583 possesses cognition-enhancing properties in rats with damage to the septohippocampal system .
|
-
- HY-N0157S1
-
|
6-Carboxyuracil-13C,15N2 monohydrate; Vitamin B13-13C,15N2 monohydrate
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Metabolic Disease
|
|
Orotic acid- 13C, 15N2 (monohydrate) is the 13C and 15N labeled Orotic acid[1]. Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats[2][3][4].
|
-
- HY-103424
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
A-412997 dihydrochloride is a selective dopamine D4 receptor agonist. A-412997 dihydrochloride improves cognitive performance in rats and can be used in the research of psychiatric diseases .
|
-
- HY-155042
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Antihypertensive agent 3 (compound 4a) is an antagonis of angiotensin II receptor 1. Antihypertensive agent 3 exhibits antihypertensive activity in a spontaneously hypertensive rats (SHRs) model .
|
-
- HY-14121
-
-
- HY-D0256
-
|
Chlorazol Black E; Ferristatin II disodium; C.I. 30235
|
DNA/RNA Synthesis
|
Others
|
|
Direct Black 38 (Chlorazol Black E) is an azo dye. Direct Black 38 induces unscheduled DNA synthesis in liver and micronucleus in bone marrow of rats in vivo .
|
-
- HY-130704
-
|
|
Calcium Channel
|
Metabolic Disease
|
|
Isotachysterol 3 is an analog of 1,25-dihydrox Vitamin D3. Isotachysterol 3 stimulates intestinal calcium transport and bone calcium mobilization in anephric rats .
|
-
- HY-133610
-
|
|
Others
|
Others
|
|
3,4,6-trichlorocatechol (TCC) is the metabolite produced by industrial pollutant through post-mitochondrial liver fraction from Aroclor-1254 induced rats .
|
-
- HY-W751152
-
|
|
Others
|
Cancer
|
|
α,β-Thujone is a component of the essential oils of some plants. α,β-Thujone causes cancers in male rats and induces seizures in the highest doses .
|
-
- HY-148226
-
-
- HY-164386
-
|
OM 174
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
Cancer
|
|
Defoslimod (OM 174) is an agonist for TLR4 receptor and acts as an immunomodulator. Defoslimod activates macrophages and dendritic cells, induces cytokines secretion, and exhibits antitumor efficacy in rats .
|
-
- HY-126826
-
-
- HY-118910
-
-
- HY-15023
-
|
PF-3274167
|
Oxytocin Receptor
|
Endocrinology
|
|
Cligosiban (PF-3274167) is an orally active, highly selective, and centrally permeable oxytocin receptor antagonist with good pharmacokinetics in rats and can inhibit physiological ejaculation in rodents [1][2].
|
-
- HY-D1163
-
|
Chromium acetate; Chromic acetate; Chromium triacetate
|
AMPK
|
Metabolic Disease
|
|
Chromium(III) acetate (Chromic acetate) is an AMPK inhibitor that promotes lipogenesis by inhibiting AMPK phosphorylation. Chromium(III) acetate has low toxicity in mammals, with an LD50 of 2365 mg/kg in rats .
|
-
- HY-118470
-
|
Butoxamin hydrochloride
|
Adrenergic Receptor
|
Endocrinology
|
|
Butaxamine (Butoxamin) hydrochloride is a specific β2-adrenergic receptor blocker. Butaxamine hydrochloride inhibits the decreases in urine volume in ethanol-anesthetized, water-diuretic rats .
|
-
- HY-103232
-
|
|
mGluR
|
Neurological Disease
|
IEM-1925 bromide is an orally active glutamate receptor antagonist, increases the latent period and decreases the duration of status epilepticus in rats in a lithium-pilocarpine model of epilepsy .
|
-
- HY-100987
-
|
|
Others
|
Others
|
|
Lauroylcarnitine chloride enhances the absorption of salmon calcitonin in rats. Also in determining in situ bioavailability, increased availability of Lucifer yellow and decreased expression of claudin-4 protein in the colon .
|
-
- HY-125610
-
-
- HY-129759
-
|
|
Cholecystokinin Receptor
|
Inflammation/Immunology
|
|
KSG-504 (anhydrous) is a CCK receptor antagonist. KSG-504 (anhydrous) inhibits the development of Ethionine-induced acute pancreatitis in rats and facilitates the regeneration of acinar cells .
|
-
- HY-122231
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
MRS3558 is a potent and selective A3AR agonist, with Ki values of 0.6 nM for humans and 0.9 nM for rats, making it suitable for research in the fields of neuropathic pain and anesthesia .
|
-
- HY-19061
-
|
|
Others
|
Neurological Disease
|
CGP 28014 is a catechol-O-methyltransferase inhibitor. CGP 28014 can lower HVA levels and increase DOPAC levels in the striatum of rats, making it useful for research on Parkinson's disease .
|
-
- HY-155297
-
|
FLA-136
|
Histamine Receptor
|
Cardiovascular Disease
|
|
Nebidrazine is a centrally-acting hypotensive agent compared to clonidine, demonstrating weaker cardiovascular effects in rats. It induces dose-dependent hypotension and bradycardia when administered intracerebroventricularly (i.c.v.), with significantly lower sedative potential than clonidine in conscious rats. Yohimbine attenuates the cardiovascular effects of both Nebidrazine and clonidine, suggesting involvement of central alpha-autoreceptors sensitive to yohimbine. Unlike clonidine, Nebidrazine does not affect peripheral alpha-adrenoceptors in pithed rats, indicating a selective central mechanism. Chemical sympathectomy reduces Nebidrazine's cardiovascular effects more than clonidine's, and metiamide diminishes responses to both drugs, implicating central histamine receptors. These findings highlight Nebidrazine's distinct pharmacological profile and potential therapeutic application in managing hypertension through central alpha-autoreceptor stimulation .
|
-
- HY-14923
-
|
AVE 7688
|
Angiotensin-converting Enzyme (ACE)
|
Metabolic Disease
|
|
Ilepatril, a vasopeptidase inhibitor, was investigated in obese Zucker diabetic fatty (ZDF) rats as a dual inhibitor of angiotensin converting enzyme and neutral endopeptidase for treating Type 2 diabetic nephropathy. Despite stable diabetes (HbA1c >12%), Ilepatril significantly reduced albuminuria in a dose-dependent manner compared to placebo. This study highlights Ilepatril's efficacy in ameliorating nephropathy symptoms in diabetic rats, suggesting its potential as a therapeutic strategy independent of metabolic control for Type 2 diabetic nephropathy .
|
-
- HY-N8931
-
|
Lithospermic acid monomethyl ester
|
Akt
|
Neurological Disease
|
|
Monomethyl lithospermate activates the PI3K/AKT pathway, which plays a protective role in nerve injury. Monomethyl lithospermate can improve the survival ability of SHSY-5Y cells, inhibit the breakdown of mitochondrial membrane potential (MMOP) and inhibit cell apoptosis. Monomethyl lithospermate also reduced the level of oxidative stress in the brain tissue of rats with middle artery occlusion (MCAO) and improved nerve damage in rats with ischemic stroke (IS) .
|
-
- HY-153369
-
|
|
Guanylate Cyclase
|
Cardiovascular Disease
Neurological Disease
|
|
BAY-747 is an orally active and brain-penetrant stimulator of soluble guanylate cyclase (sGC). BAY-747 reverses L-NAME induced memory impairments and enhances cognition of rats in the object location task (OLT). BAY-747 also decreases blood pressure in both conscious normotensive and spontaneously hypertensive rats (SHR). BAY-747 improves function of the skeletal muscle associated with Duchenne muscular dystrophy (DMD) in mdx/mTRG2 mice model .
|
-
- HY-143444
-
|
|
JAK
|
Inflammation/Immunology
|
|
JAK-IN-20 is a potent, pan and orally active JAK inhibitor with an IC50s of 7 nM, 5 nM, 14 nM for JAK1, JAK2, JAK3, respectively. JAK-IN-20 shows excellent pharmacokinetics and displays anti-inflammatory efficacy in vivo .
|
-
- HY-146429
-
|
|
Others
|
Metabolic Disease
|
|
NaPi2b-IN-3 (compound 5) is a potent sodium-dependent transport protein 2b (SLC34A2, NaPi2b) inhibitor with IC50s of 71 nM and 28 nM for human NaPi2b and rat NaPi2b, respectively. NaPi2b-IN-3 can be used for researching hyperphosphatemia .
|
-
- HY-P0048
-
|
Surfagon
|
GnRH Receptor
|
Others
|
|
(Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH (Surfagon, Mwt 1167.34 Da) is an agonist of gonadotropin-releasing hormone (GnRH). (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH can be used as an internal standard for the LC-MS analysis of leuprorelide acetate. (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH has potential applications in biochemical analysis and fertility .
|
-
- HY-128060
-
-
- HY-162398
-
|
|
CDK
|
Inflammation/Immunology
|
|
LQ23 is a selective inhibitor for CDC2-like kinase 2 (CLK2) with an IC50 of 1.4 nM. LQ23 exhibits anti-inflammatory activity .
|
-
- HY-162399
-
|
|
PD-1/PD-L1
STAT
|
Inflammation/Immunology
|
|
PD-L1-IN-6 (Compound 16) is an orally active inhibitor for PD-L1 expression in neutrophil by targeting STAT3 with KD of 90.5 nmol/L. PD-L1-IN-6 promotes neutrophil-mediated antifungal immunoresponse .
|
-
- HY-163443
-
|
|
PPAR
|
Others
|
|
PPAR agonist 4 (Compound 12) is an orally active agonist for peroxisome proliferator-activated receptor (PPAR), which activates PPARα, PPARδ and PPARγ with EC50s of 0.7, 0.7 and 1.8 μM, respectively. PPAR agonist 4 exhibits anti-liver fibrosis efficacy .
|
-
- HY-118383
-
-
- HY-164011
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
Alaproclate is an inhibitor for serotonin (5-HT) reuptake. Alaproclate affects mechanisms that related to cued navigation performance such as sensory, sensorimotor, or motivational factors, impairs spatial navigation ability of rats .
|
-
- HY-158556
-
|
2,3-Dmec hydrochloride
|
Others
|
Neurological Disease
|
|
2,3-Dimethylethcathinone (2,3-Dmec) hydrochloride, a cathinone, is an analog of Ethcathinone. Ethcathinone increases the peak dopamine efflux after electrical stimulation and slows dopamine reuptake in rats .
|
-
- HY-162662
-
|
|
Cytochrome P450
mAChR
|
Neurological Disease
|
|
VU6008677 is a positive allosteric modulator (PAM) for M4, with EC50 of 120 nM for hM4. VU6008677 inhibits cytochrome P450, exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-127152
-
|
Pratorine
|
Endogenous Metabolite
|
Cardiovascular Disease
|
|
Hippadine (Pratorine) is an alkaloid, which can be isolated from the plant Crinum macowanii. Hippadine exhibits heart-rate lowering and blood-pressure lowering effects in rats models with spontaneously hypertensive .
|
-
- HY-160857
-
|
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
TOP5668 is an orally active follicle-stimulating hormone receptor allosteric agonist. TOP5668 can induce the production of testosterone in stromal cells and promote follicular genesis and superovulation in rats .
|
-
- HY-160856
-
|
TOP05300
|
Estrogen Receptor/ERR
|
Endocrinology
|
|
TOP5300 is an orally active follicle-stimulating hormone receptor allosteric agonist. TOP5300 can induce the production of testosterone in stromal cells and promote follicular genesis and superovulation in rats .
|
-
- HY-119304
-
-
- HY-N9363
-
|
|
Others
|
Metabolic Disease
|
|
Corymbiferin is one of active constituents, responsible for anti-diabetic properties. Corymbiferin improves antioxidant capacity and carbohydrate metabolism in diabetic rats, along with the improvement of histopathology of livers and pancreatic β cells .
|
-
- HY-119953
-
|
|
mAChR
|
Neurological Disease
|
|
BIBN-99 is a selective, BBB-penetrable and competitive muscarinic M2 receptor antagonist. BIBN-99 improves cognitive performancein rats with traumatic brain injury .
|
-
- HY-P4201
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .
|
-
- HY-136880
-
|
Sgd 195/78
|
5-HT Receptor
|
Cardiovascular Disease
|
|
Flufylline shows antihypertensive properties in spontaneously hypertensive rats and display antagonism towards 5-HT receptors in various animal models. Flufylline can be used for cardiovascular disease research .
|
-
- HY-110270A
-
|
|
TRP Channel
|
Inflammation/Immunology
|
|
RN-9893 Hydrochloride is an orally active antagonist of transient receptor potential vanilloid 4 (TRPV4), with IC50 values of 0.42 and 0.66 μM, for humans and rats, respectively .
|
-
- HY-120076
-
|
|
Dopamine Receptor
|
Neurological Disease
|
CP-293019 is a dopamine D4 receptor antagonist, with a Ki value of 3.4 nM. CP-293019 can inhibit Apomorphine (HY-12723) induced hyperactivity in rats .
|
-
- HY-N6910
-
|
|
Others
|
Metabolic Disease
|
|
Pseudolaric Acid C2, a diterpenoid isolated from Pseudolarix kaempferi, is identified as the specific metabolite of Pseudolaric acid B in plasma, urine, bile and feces after both oral and intravenous administration to rats .
|
-
- HY-121401A
-
|
(1R)-(−)-Myrtenal; (−)-(1R,5S)-Myrtenal
|
Akt
|
Metabolic Disease
Cancer
|
|
(?)-Myrtenal ((1R)-(?)-Myrtenal) is an orally active terpene with antitumour activity. (?)-Myrtenal ameliorates hyperglycemia by enhancing GLUT2 through Akt in the skeletal muscle and liver of diabetic rats .
|
-
- HY-107176A
-
|
HS-25
|
Others
|
Metabolic Disease
|
|
Hyzetimibe is a cholesterol absorption inhibitor. Hyzetimibe blocks the intestinal absorption of cholesterol and phytol. Hyzetimibe is well tolerated in animal models, with an LDmax 2000 mg/kg in rats and an LDmax 500 mg/kg in rhesus monkeys .
|
-
- HY-130325
-
|
|
Others
|
Neurological Disease
|
|
α-Guanidinoglutaric acid is a guanidino compound first found in cobaltinduced epileptogenic focus tissue in the cerebral cortex of cats. α-Guanidinoglutaric acid induces epileptic seizures in rats after intraventricular administration .
|
-
- HY-165529
-
|
|
Others
|
Inflammation/Immunology
|
Camostat is an orally active trypsin inhibitor. Camostat can reduce pancreatic fibrosis induced by repeated administration of superoxide dismutase inhibitors in rats, and decrease the proliferation and activation of pancreatic stellate cells (PSCs) .
|
-
- HY-124521
-
|
LY163502 free base
|
Dopamine Receptor
|
Neurological Disease
|
|
Quinelorane (LY163502 free base) is a dopamine D2 receptor agonist. Quinelorane promotes semen ejaculation but inhibits penile erection in rats. Quinelorane can be used in the study of sexual dysfunction .
|
-
- HY-113840
-
|
Ro 14-9706
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
Sumarotene (Ro 14-9706), an arotinoid methyl sulfone, is a potent dermatologic agent for the repair of photodamage, antikeratinization, and antiproliferation. Sumarotene exhibits in rats a prolactin-suppressive activity which affects lactation .
|
-
- HY-161784
-
|
|
GABA Receptor
|
Neurological Disease
|
|
GABAA receptor modular-3 (Compound S28) is a modulator for (γ-aminobutyric acid)A receptor (GABAA receptor), with EC50 of 56 nM and 10 nM, for α1β2γ2 and α4β3δ subtype. GABAA receptor modular-3 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modular-3 is slightly toxic toxicity in rats with a loss of rollover reflex (LORR) threshold dose of 23.3 μmol/kg, and exhibits potential ameliorating the postpartum depression .
|
-
- HY-117792
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
LY314228 is an aminoguanidine 5-HT2 antagonist with relative selectivity for 5-HT2A receptors (IC50: 147.9 nM). The Ki values ??of LY314228 targeting different 5-HT subtypes are 65 nM (5-HT 2A), 1214 nM (5-HT 2B), and 168 nM (5-HT 2C), respectively. LY314228 is an effective inhibitor of 5-HT-induced paw edema in rats with an ED50 of 6.4 mg/kg in ovariectomized female rats. .
|
-
- HY-129207
-
|
|
GHSR
|
Endocrinology
|
|
Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro. 80 μg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats. JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 μg/kg.
|
-
- HY-158030
-
|
|
HDAC
|
Neurological Disease
|
|
HDAC6-IN-37 (compound W5) is an inhibitor of HDAC6 and has neuroprotective effects. HDAC6-IN-37 can restore the morphology of hippocampal neurons, reduce the expression of Aβ, Tau, and p-Tau proteins in the hippocampus of AD rats, and inhibit the formation of senile plaques and neurofibrillary tangles. Thus, HDAC6-IN-37 improves the Aβ/Cu 2+-induced AD model in rats, regulates oxidative stress status, and balances neurotransmitter disorders in brain tissue .
|
-
- HY-A0139
-
|
NSC 108165; Navan; Navane
|
Others
|
Others
|
|
Thiothixene is a typical antipsychotic. It selectively binds to dopamine D2 over D1, D3, and D4 receptors (Kis=0.417, 338, 186.2, and 363.1 nM, respectively). Thiothixene also binds to various serotonin (5-HT), histamine H1, α1- and α2-adrenergic, muscarinic acetylcholine, and sigma receptors (Kis=15-5,754 nM) as well as the dopamine, norepinephrine, and serotonin transporters (Kis=3.16-30 μM). In vivo, thiothixene reduces spontaneous and amphetamine-induced locomotor activity in rats. It enhances latent inhibition, as measured by a decreased lick latency in response to light and foot shock stimuli, which is a measure of selective attention in rats.3 Thiothixene also increases competitive behavior in submissive mice, indicating antidepressant-like behavior.
|
-
- HY-161835
-
-
- HY-106246
-
|
EMD 281014 free acid; LY 2422347
|
5-HT Receptor
|
Neurological Disease
Metabolic Disease
|
|
Pruvanserin (EMD 281014 free acid) is a selective 5-HT2A receptor antagonist. Pruvanserin alleviates tactile allodynia in diabetic rats. Pruvanserin can also be used for research of insomnia .
|
-
- HY-B1971S
-
|
Decamethrin-d5
|
Isotope-Labeled Compounds
Endogenous Metabolite
|
Cancer
|
|
Deltamethrin-d5 is the deuterium labeled Deltamethrin. Deltamethrin (Decamethrin), a neurotoxic pyrethroid insecticide, produces a reversible sequence of motor symptoms in rats involving hind limb rigidity and choreoathetosis[1][2].
|
-
- HY-B1301
-
|
|
Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Triprolidine hydrochloride monohydrate, a first-generation antihistamine, is an oral active histamine H1 antagonist. Triprolidine hydrochloride monohydrate can be used for the research of allergic rhinitis. Triprolidine hydrochloride monohydrate exhibits spinal motor and sensory block in rats .
|
-
- HY-135761
-
|
|
Fungal
Cholinesterase (ChE)
|
Infection
Neurological Disease
|
|
Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats .
|
-
- HY-P2497
-
|
|
GCGR
|
Neurological Disease
|
|
Exendin (5-39) is a potent glucagon-like peptide 1 (GLP-1) receptor antagonist. Exendin (5-39) improves memory impairment in β-amyloid protein-treated rats .
|
-
- HY-108038
-
|
|
nAChR
|
Neurological Disease
|
|
ABT-107 is a selective α7 neuronal nicotinic receptor agonist. ABT-107 protects against nigrostriatal damage in rats with unilateral 6-hydroxydopamine lesions .
|
-
- HY-103510
-
|
|
GABA Receptor
|
Neurological Disease
|
|
TB-21007 is an inverse agonist of α5β3γ2 subunit-containing GABAA receptor with a Ki of 1.6 nM. TB-21007 enhanced spatial memory in rats .
|
-
- HY-111130
-
|
|
Histamine Receptor
mAChR
|
Neurological Disease
Cancer
|
Methapyrilene is a histamine antagonist, a pyridine chemical with anticholinergic activity. Methapyrilene can cause target organ-specific epigenetic alterations, such as a decrease in DNA methylation levels. Methapyrilene induces hepatocellular carcinoma in rats .
|
-
- HY-118388
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
AS604872 is an orally active, potent and selective prostaglandin F2α receptor (FP) antagonist with a Ki of 35 nM in humans, 158 nM in rats and 323 nM in mice. AS604872 inhibits contractions and delays labour .
|
-
- HY-129315
-
|
N-Deacetylketoconazole; R-39519
|
Bacterial
Fungal
|
Infection
|
|
Deacylketoconazole (N-Deacetylketoconazole; R-39519) is an orally active metabolite of Ketoconazole (HY-B0105). Deacylketoconazole exhibits antifungal and antibacterial activity. Deacylketoconazole is cytotoxic in rats hepatocyte .
|
-
- HY-N0300R
-
|
|
Dopamine Receptor
Apoptosis
|
Neurological Disease
|
|
Tetrahydropalmatine (Standard) is the analytical standard of Tetrahydropalmatine. This product is intended for research and analytical applications. Tetrahydropalmatine possesses analgesic effects. Tetrahydropalmatine acts through inhibition of amygdaloid release of dopamine to inhibit an epileptic attack in rats .
|
-
- HY-123239
-
|
|
GPR55
|
Neurological Disease
|
|
KLS-13019 is an orally active GPR55 receptor antagonist and a structural analogue of cannabidiol (CBD). It can prevent and reverse chemotherapy-induced peripheral neuropathy (CIPN) in a dose-dependent manner in rats .
|
-
- HY-110161
-
|
|
Somatostatin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
sst2 Receptor agonist-1 is a potent somatostatin receptor subtype 2 (sst2) agonist with a Ki value of 0.025 nM and a cAMP IC50 value of 4.8 nM. sst2 Receptor agonist-1 can inhibit rat growth hormone (GH) secretion and ocular neovascular lesion formation. Antiangiogenic effect .
|
-
- HY-14127
-
R121919
4 Publications Verification
NBI30775
|
CRFR
|
Neurological Disease
Endocrinology
|
|
R121919 (NBI30775) is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 has antidepressant and anxiolytic effects. R121919 alleviates defensive withdrawal in rats .
|
-
- HY-P1236
-
|
Atrial natriuretic factor (1-28) (rat, mouse)
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
|
-
- HY-107248
-
|
|
Others
|
Inflammation/Immunology
|
|
Escin IIa, isolated from horse chestnut, the seeds of Aesculus hippocastanum L., has positive effects on acute inflammation in animals. Escin IIa has gastroprotections on ethanol-induced gastric mucosal lesions in rats .
|
-
- HY-119061
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-357134 is a potent, selective, brain penetrant, and orally active 5-HT6 receptor antagonist. SB-357134 enhances memory and learning and increases seizure threshold in rats .
|
-
- HY-156972
-
|
|
Opioid Receptor
|
Metabolic Disease
|
|
NOP agonist-1(compound 4) is a nociceptin opioid receptor (NOP) partial agonist. NOP agonist-1attenuate parkinsonian disabilities in 6-OHDA hemilesioned rats .
|
-
- HY-115645
-
|
NBI30775 hydrochloride
|
CRFR
|
Neurological Disease
Metabolic Disease
|
|
R121919 (NBI30775) hydrochloride is a potent and selective CRF1R antagonist with a Ki of 2 to 5 nM. R121919 hydrochloride has antidepressant and anxiolytic effects. R121919 hydrochloride alleviates defensive withdrawal in rats .
|
-
- HY-W037282
-
|
Cupreidine
|
Others
|
Neurological Disease
|
|
O-Desmethyl quinidine (Cupreidine) is an orally active metabolite of Quinine (HY-D0143). O-Desmethyl quinidine reduces frequency of cramps in rats with spinal cord injury and shows low blood toxicity .
|
-
- HY-117443
-
|
|
Guanylate Cyclase
|
Cardiovascular Disease
|
|
IWP-051 is an agonist for soluble guanylate cyclase with an EC50 of 290 nM. IWP-051 stimulates the generation of cGMP, and exhibits the synergistic effect with NO. IWP-051 exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-161993
-
|
|
Ketohexokinase
|
Metabolic Disease
|
|
BI-9787 is a zwitterionic inhibitior for ketohexokinase, with an IC50 of 12 and 12.8 nM for hKHK-A and hKHK-C. BI-9787 exhibits good metabolic stability in rat hepatocyte and good pharmacokinetic characteristics in rats .
|
-
- HY-106281
-
|
PPD 10558
|
HMG-CoA Reductase (HMGCR)
|
Cardiovascular Disease
Metabolic Disease
|
|
Bemfivastatin (PPD 10558) is an orally active, HMG-CoA Reductase (HMGCR) inhibitor, also known as Statin. Bemfivastatin enhances the activity of liver extraction. Bemfivastatin exhibits little developmental toxicity effects in pregnant rats and rabbits via daily oral doses during organogenesis period. The no observed adverse effect level (NOAEL) are ≥320 mg/kg/day for rats developmental toxicity, 12.5 mg/kg/day for rabbits maternal toxicity, and 25 mg/kg/day for rabbits developmental toxicity, respectively. Bemfivastatin can be used for research on Statin-related hypercholesterolemic myalgia with inability to tolerate statins .
|
-
- HY-15543A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
CP-809101 hydrochloride is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 hydrochloride inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 hydrochloride also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence .
|
-
- HY-15543
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
CP-809101 is a potent and highly selective 5-HT2C receptor agonist, with pEC50s of 9.96, 7.19 and 6.81 M for human 5HT2C, 5HT2B and 5HT2A receptor. CP-809101 inhibits conditioned avoidance responding in rats and antagonizes both PCP (phencyclidine hydrochloride)- and d-amphetamine-induced hyperactivity. CP-809101 also reduces food and nicotine dependence in rats, can be used in studies of antipsychotic and nicotine dependence .
|
-
- HY-162586
-
|
|
Others
|
Cancer
|
|
PDHK-IN-7 (compound 32) is an inhibitor of pyruvate dehydrogenase kinase with an IC50 value of 17 nM.PDHK-IN-7 activates PDH in rat livers and has a glucose-lowering effect in Zucker fatty rats .
|
-
- HY-118033
-
|
|
Renin
|
Cardiovascular Disease
|
|
SQ 30774 is a renin (renin) inhibitor. SQ 30774 has potent in vitro inhibitory effects in primates but not in rats, pigs, or dogs. And imidazolinol renin inhibitors also inhibit PRA and reduce arterial blood pressure in vivo .
|
-
- HY-102092
-
|
PD 147953
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
FR139317 (PD 147953) is a selective ETA receptor antagonist. FR139317 inhibits cerebral activation by intraventricular endothelin-1 in conscious rats. FR139317 also ameliorates cerebral vasospasm in dogs .
|
-
- HY-105454A
-
|
Wy-42362 hydrochloride
|
Others
|
Cardiovascular Disease
|
|
Recainam (Wy-42362) hydrochloride is an orally active anti-arrhythmic agent with Class I electrophysiological properties. Recainam suppresses complex ventricular arrhythmias. Racainam hydrochloride exhibits a good pharmacokinetic character in Sprague Dawley rats .
|
-
- HY-121827
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
LH-21 is a potent in vivo neutral cannabinoid CB1 receptor antagonist. LH-21 reduces food intake and body weight gain in obese Zucker rats.
, and displays efficacy as a feeding inhibitor .
|
-
- HY-B0235
-
|
|
Others
|
Metabolic Disease
|
|
Trichlormethiazide is an orally active thiazide diuretic, with antihypertensive effect. Trichlormethiazide increases urine volume (UV), Na and K excretion and tends to improve the depressed creatinine clearance (CCRE) in acute renal failure rats model .
|
-
- HY-P1236A
-
|
Atrial natriuretic factor (1-28) (rat, mouse) TFA
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse (TFA) is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
|
-
- HY-108582
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
Y-27152, a proagent of the KATP (Kir6) channel opener Y-26763, is a long-acting K+ channel opener with less tachycardia: antihypertensive effects in hypertensive rats and dogs in conscious state .
|
-
- HY-N0723
-
|
|
Others
|
Metabolic Disease
|
|
Neomangiferin is a natural C-glucosyl xanthone isolated from m the dried rhizome of Anemarrhena asphodeloides. Neomangiferin has significant therapeutic effects on high-fat diet-induced nonalcoholic fatty liver disease (NAFLD) in rats .
|
-
- HY-N2531
-
|
|
Autophagy
|
Cardiovascular Disease
|
|
Notoginsenoside Fc, a protopanaxadiol- (PPD-) type saponin isolated from the leaves of Panax notoginseng, effectively counteracts platelet aggregation. Notoginsenoside Fc can accelerate reendothelialization following vascular injury in diabetic rats by promoting autophagy .
|
-
- HY-B0235A
-
|
|
Others
|
Metabolic Disease
|
|
Trichlormethiazide sodium is an orally active thiazide diuretic, with antihypertensive effect. Trichlormethiazide sodium increases urine volume (UV), Na and K excretion and tends to improve the depressed creatinine clearance (CCRE) in acute renal failure rats model .
|
-
- HY-107644
-
|
|
mAChR
|
Cardiovascular Disease
|
|
AQ-RA 741 is a potent and selective M 2 antagonist. AQ-RA 741 inhibits the vagally or agonist-induced bradycardia in rats, cats and guinea-pigs. AQ-RA 741 is used in bradycardiac disorders research .
|
-
- HY-131542
-
|
|
Aldose Reductase
Apoptosis
|
Metabolic Disease
|
|
APPA is an aldose reductase inhibitor. APPA can effectively prevent apoptosis and the symptoms of Streptozotocin (HY-13753)-induced diabetes by inhibiting the polyol pathway in rats. APPA has the potential for diabetic nephropathy (DN) research .
|
-
- HY-W102714
-
|
CDTA
|
Others
|
Metabolic Disease
|
|
1,2-Cyclohexylenedinitrilotetraacetic acid (CDTA) is a chelating agent. 1,2-Cyclohexylenedinitrilotetraacetic acid has an ability to remove manganese from brain and liver (in vivo) and their sub-cellular fractions (in vitro), of rats pretreated with manganese sulphate .
|
-
- HY-121775
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
F-00217830 is an agonist ofDopamine D2 receptor. PF-00217830 inhibits of spontaneous locomotor activity and 2,5-dimethoxy-4-iodoamphetamine-induced head twitches in rats .
|
-
- HY-127166
-
|
O10-Demethylcolchicine
|
Microtubule/Tubulin
|
Inflammation/Immunology
|
|
Colchiceine is one of several metabolites of the anti-gout medication Colchicine (HY-16569). Colchicine is a tubulin inhibitor and a microtubule disrupting agent, and may protect rats from developing liver injury and fibrosis .
|
-
- HY-105454
-
|
Wy-42362
|
Others
|
Cardiovascular Disease
|
|
Recainam (Wy-42362) is an orally active anti-arrhythmic agent with Class I electrophysiological properties. Recainam suppresses complex ventricular arrhythmias. Racainam exhibits a good pharmacokinetic character in Sprague Dawley rats .
|
-
- HY-106424
-
|
|
Others
|
Neurological Disease
|
|
Soretolide is an antiepileptic agent. Soretolide is effective in maximal electroshock-induced seizure (MES) test in rodents. Soretolide inhibits metabolism of Phenytoin (HY-B0448). Soretolide exhibits a good pharmacokinetic character in rats model .
|
-
- HY-116507
-
|
|
nAChR
|
Neurological Disease
|
|
AZD0328 is a selective α7 nAChR partial agonist. AZD0328 selectively enhances midbrain dopaminergic neuronal activity and enhances cortical dopamine levels in rats. AZD0328 improves cognitive performance .
|
-
- HY-107593
-
|
|
IKK
|
Inflammation/Immunology
|
|
PS-1145 (dihydrochloride) is a potent IκB kinase-2 inhibitor with an IC50 value of 88 nM. PS-1145 (dihydrochloride) inhibits activity of NF-κB by blocking IκB kinase phosphorylation in tumor-bearing rats .
|
-
- HY-10900
-
-
- HY-N0691
-
|
Schizandrin; Schizandrol; Schizandrol-A
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Schisandrin (Schizandrin), a dibenzocyclooctadiene lignan, is isolated from the fruit of Schisandra chinensis Baill. Schisandrin exhibits antioxidant, hepatoprotective, anti-cancer and anti-inflammatory activities. Schisandrin also can reverses memory impairment in rats .
|
-
- HY-112612
-
|
|
GPR88
|
Neurological Disease
|
|
RTI-13951-33 is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 reduces alcohol reinforcement and intake behaviors in rats .
|
-
- HY-75087
-
|
(+)-(R)-Proline; (R)-(+)-Proline; (R)-2-Carboxypyrrolidine; (R)-Proline
|
Endogenous Metabolite
|
Metabolic Disease
|
|
(R)-pyrrolidine-2-carboxylic acid ((+)-(R)-Proline) is a proline isomer that exhibits high renal and hepatotoxicity in rats. (R)-pyrrolidine-2-carboxylic acid can be used to study amino acid metabolism and toxicity mechanisms .
|
-
- HY-112612A
-
|
|
GPR88
|
Neurological Disease
|
|
RTI-13951-33 hydrochloride is a potent, selective, and brain-penetrant GPR88 agonist, with an EC50 of 25 nM in GPR88 cAMP functional assay. RTI-13951-33 hydrochloride reduces alcohol reinforcement and intake behaviors in rats .
|
-
- HY-N2196
-
|
|
Others
|
Inflammation/Immunology
|
|
Ajugasterone C is an ecdysteroid isolated from Leuzea carthamoides. Ajugasterone C shows significant inhibitory effect at 100 mg/kg dose on rat paw oedema development due to Carrageenan-induced inflammation in Sprague Dawley rats .
|
-
- HY-N9113
-
|
|
Others
|
Cardiovascular Disease
|
|
1,3,5,6-Tetrahydroxyxanthone is a natural xanthone that can be isolated from Garcinia achachairu Rusby (Clusiaceae) branches. 1,3,5,6-Tetrahydroxyxanthone induces diuresis and saluresis in normotensive and hypertensive rats .
|
-
- HY-148558
-
|
|
P2X Receptor
|
Neurological Disease
|
|
P2X7 receptor antagonist-3 is a potent P2X7 receptor antagonist with P2X7R IC50 values of 4.2 nM in humans and 6.8 nM in rats .
|
-
- HY-119594
-
|
|
Parasite
|
Infection
|
|
Melarsoprol, a melaminophenylarsine-type trivalent organic arsenical, is an important drug for African trypanosomiasis. Melarsoprol is also active against leukemia cell lines and plasma cells from myeloma patients. Melarsoprol increases the biliary output of GSH in rats .
|
-
- HY-162325
-
-
- HY-B0099R
-
|
|
MMP
Apoptosis
|
Neurological Disease
|
|
Edaravone (Standard) is the analytical standard of Edaravone. This product is intended for research and analytical applications. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator.
|
-
- HY-163378
-
|
|
Complement System
|
Inflammation/Immunology
|
|
C5aR1 antagonist 1 (Compound 7e) is an orally active C5a receptor 1 (C5aR1) antagonist. C5aR1 antagonist 1 is active in DISCO and migration assays, with IC50 values of 38 nM and 17 nM, respectively. C5aR1 antagonist 1 can be used for the research of acute and chronic inflammatory diseases .
|
-
- HY-108381
-
|
LCB29
|
Others
|
Others
|
|
Idrocilamide (LCB29) exhibits a muscle relaxing effect, that inhibits muscle twitch, tetanic tension, K +-induced as well as voltage clamp-induced contraction of rat soleus muscle fibers .
|
-
- HY-N2388
-
-
- HY-W009724
-
|
2-APB
|
Calcium Channel
TRP Channel
CRAC Channel
|
Inflammation/Immunology
|
|
2-Aminoethyl diphenylborinate (2-APB) is a cell-permeable inhibitor of Inositol triphosphate receptor (IP3R). 2-Aminoethyl diphenylborinate also inhibits the store-operated Ca 2+ (SOC) channel and activates some TRP channels (V1, V2 and V3). Additionally, 2-Aminoethyl diphenylborinate has inhibitory effects on vasospasm. At high concentrations, it exhibits specific anti-inflammatory and antioxidant effects in neural tissue .
|
-
- HY-121469
-
|
|
Others
|
Neurological Disease
|
|
Dioxone is a substance possessing convulsant properties qualitatively similar to leptazol and bemegride. Dioxone is orally active .
|
-
- HY-151927
-
-
- HY-149212
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
SD-6 is an orally active inhibitor of hAChE and hBChE with IC50 values of 0.907 µM and 1.579 µM, respectively. SD-6 has excellent blood-brain barrier (BBB) permeability and no neurotoxicity, which can be used for research on Alzheimer's disease .
|
-
- HY-14922
-
|
|
Reverse Transcriptase
HIV
|
Infection
|
|
Fosalvudine tidoxil is an orally active nucleoside reverse transcriptase inhibitor (NRTI). Fosalvudine tidoxil is a prodrug derived from Alovudine (HY-B1516). Fosalvudine tidoxil is less toxic than Alovudine and can be used for the research of HIV-1 infection .
|
-
- HY-N3202
-
|
(+)-Neolitsine
|
Others
|
Cardiovascular Disease
|
|
Neolitsine ((+)-Neolitsine) is a vasodilator. Neolitsine can be isolated from the herb Cassytha filiformis. Neolitsine exhibits significant vasodilatory effects on precontracted rat aortic preparations with an IC50 of 0.29 μM .
|
-
- HY-106356
-
|
|
Others
|
Others
|
|
GV-150013 is a selective CCK-B receptor antagonist. GV-150013 has sleep aid effect .
|
-
- HY-17011
-
|
|
Others
|
Metabolic Disease
|
|
Croconazole is an antifungal agent containing imidazole rings. Croconazole has a unique structural feature of aryl vinyl at the imidazole ring N-1. Croconazole can be used for the identification and quantitative study of major metabolites in rat urine and bile .
|
-
- HY-116431
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
I-BOP is an agonist for thromboxane A2 receptor (TP) with a KD of 0.61 nM. I-BOP promotes proliferation through activation of PI3K pathway in vascular smooth muscle . I-BOP dose-dependently biphasicly affects the excitatory postsynaptic potential (e.p.s.p.) in hippocampal neurons .
|
-
- HY-162482
-
|
|
EGFR
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
EGFR kinase inhibitor 5 (Compound 4c) is an orally active inhibitor for epidermal growth factor receptor (EGFR) kinase, with IC50 of 18.35 μM. EGFR kinase inhibitor 5 induces apoptosis. EGFR kinase inhibitor 5 exhibits anticancer and anti-inflammatory activity with low toxicity (LD50 range: 500-2000 mg/kg) .
|
-
- HY-162483
-
|
|
EGFR
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
EGFR kinase inhibitor 6 (Compound 4b) is an orally active inhibitor for epidermal growth factor receptor (EGFR) kinase, with IC50 of 24.34 μM. EGFR kinase inhibitor 6 induces apoptosis. EGFR kinase inhibitor 6 exhibits anticancer and anti-inflammatory activity with low toxicity (LD50 range: 500-2000 mg/kg) .
|
-
- HY-160932
-
|
|
Others
|
Endocrinology
|
|
RS-15385-198 is the enantiomer of Delequamine (RS-15385-197) (HY-106874). RS-15385-198 exhibits a pKi of 6.32 for α2-adrenoceptors in the rat cortex. RS-15385-198 is an antagonist for UK-14304 (HY-B0659) in the rat vas deferens and in the guinea-pig ileum .
|
-
- HY-P10320
-
|
Tumstatin (69-88), human
|
PI3K
Akt
|
Cardiovascular Disease
|
|
T3 Peptide is an active fragment of tumstatin. T3 Peptide binds integrin αvβ3/αvβ5, activates the PI3K/Akt/p70S6K signaling pathway, and thus stimulates the proliferation and migration of rat cardiac fibroblasts .
|
-
- HY-163832
-
|
|
Others
|
Metabolic Disease
|
|
FPPS-IN-2 (compound 4a) is a potent and orally active HFPPS inhibitor with an IC50 value of 1.108 µM. FPPS-IN-2 has the potential for the research of osteoporosis .
|
-
- HY-N2388R
-
|
|
MMP
PPAR
Bacterial
|
Cardiovascular Disease
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Auraptene (Standard) is the analytical standard of Auraptene. This product is intended for research and analytical applications. Auraptene is an orally active geranyloxycoumarin that can be isolated from plants in the Brassicaceae family, antibacterial, anti-pathogen, antioxidant, anti-tumor, and neuroprotective effects. Auraptene plays an important role in the treatment of various chronic diseases such as hypertension and cystic fibrosis .
|
-
- HY-117466
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
FR186054 is an oral active acyl-Coenzyme A:cholesterol acyltransferase (ACAT) inhibitor with the IC50 of 99 nM. FR186054 shows hypocholesterolemic effect and can be used for study of hypercholesterolemia and atherosclerosis .
|
-
- HY-B0476
-
|
Acetophenetidin
|
COX
|
Inflammation/Immunology
|
|
Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
|
-
- HY-W012946
-
-
- HY-113986
-
|
(R)-Fadrozole; (R)-CGS 16949A free base; FAD286
|
Others
|
Cardiovascular Disease
|
|
Dexfadrostat ((R)-Fadrozole) is a potent nonsteroidal inhibitor . Dexfadrostat also inhibits human placental aromatase (pIC50 = 6.17) and aldosterone biosynthesis. Dexfadrostat reverses cardiac fibrosis in spontaneously hypertensive heart failure rats. .
|
-
- HY-W014941
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
(R)-(-)-α-Methylhistamine dihydrochloride is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM . (R)-(-)-α-Methylhistamine dihydrochloride can enhance memory retention, attenuates memory impairment in rats .
|
-
- HY-N10226
-
|
|
Prostaglandin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Thielavin B is an inhibitor of prostaglandin biosynthesis produced by Thielavia terricola. Thielavin B effectively influences the prostaglandin E2 synthesis from the endoperoxide. Thielavin B is significantly effective on carrageenan-induced oedema of rats when administered intravenously .
|
-
- HY-N4009
-
|
|
Others
|
Others
|
|
Iriflophenone 2-O-α-rhamnoside can be isolated from the leaves of Aquilaria sinensis. Iriflophenone 2-O-α-rhamnoside has a half-life value of 2.44 min in rats at the administration of 25 mg/kg .
|
-
- HY-B0770
-
|
β-Arteether; (+)-Arteether; Arteether
|
CXCR
Parasite
|
Infection
Cancer
|
|
Artemotil (β-Arteether) has antimalarial activity for the treatment of chloroquine-resistant Plasmodium falciparum malaria with an IC50 of 1.61 nM. Artemotil also has central nervous system (CNS) neurotoxicity and anorectic toxicity in rats, dogs and monkeys .
|
-
- HY-B0099S
-
|
MCI-186-d5
|
MMP
Apoptosis
|
Neurological Disease
|
|
Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
|
-
- HY-120813
-
|
URB913
|
Others
|
Inflammation/Immunology
|
|
ARN 077 is a potent and selective N-acylethanolamine acid amidase (NAAA) inhibitor with an IC50 of 7 nM for human NAAA . ARN 077 significantly increases palmitoyl ethanolamine (PEA) levels within the CNS and has broad antinociceptive activity in mice and rats .
|
-
- HY-100164
-
|
MKS 492
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
SDZ-MKS 492 (MKS 492) is a selective inhibitor of cyclic GMP-inhibited phosphodiesterase (type III PDE). SDZ-MKS 492 inhibits antigen- or platelet activating factor (PAF)-induced bronchoconstriction and allergic reactions in guinea pigs and rats .
|
-
- HY-P1338
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats .
|
-
- HY-120380
-
|
|
Autophagy
|
Inflammation/Immunology
|
|
FeTMPyP is an orally active peroxynitrite (ONOO ?) scavenger. FeTMPyP reduces nitrative stress and increases autophagy. FeTMPyP reduces PARP over-activation and neuroinflammation in chronic constriction injury (CCI)-induced rats, and ameliorates functional, behavioral and biochemical deficits .
|
-
- HY-135319
-
|
|
Others
|
Infection
|
|
Strictinin is a phenolic compound isolated from Pu'er teas. Strictinin has potential antiviral, antibacterial and laxative activities. Strictinin occurs by accelerating intestinal transit rather than enhancing gastric emptying, increasing food intake, or inducing diarrhea in rats.
|
-
- HY-121025
-
|
|
TGF-β Receptor
|
Others
|
|
BUR1 is a BMP upregulator (EC50: 98 nM) and activates BMPRII signalling. BUR1 induces BMP2 and PTGS2 expression. BUR1 reversed pulmonary arterial pressure in Monocrotaline (HY-N0750) induced rats .
|
-
- HY-19656
-
|
|
Others
|
Metabolic Disease
|
|
HMR1426 is an orally active, potent gastric emptying inhibitor. HMR1426 reduces food intake and the rate of gastric emptying, decreases body weight and fat mass and shows an anorectic potential in rats. HMR1426 has the potential for obesity research .
|
-
- HY-10655
-
|
ACT-058362
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
Palosuran (ACT-058362) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran can improves pancreatic and renal function in diabetic rats .
|
-
- HY-N2086
-
-
- HY-N1131
-
|
2,2,6,6-Tetramethyl-4-piperidone
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
Triacetonamine (2,2,6,6-Tetramethyl-4-piperidone) is used as an intermediate for the synthesis of pharmaceutical products, pesticides and photostabilizers for polymers. Triacetonamine has oral activity and can induce acute liver failure (ALF) in rats .
|
-
- HY-100999
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
(R)-(-)-α-Methylhistamine dihydrobromide is a potent, selective and brain-penetrant agonist of H3 histamine receptor, with a Kd of 50.3 nM . (R)-(-)-α-Methylhistamine dihydrobromide can enhance memory retention, attenuates memory impairment in rats .
|
-
- HY-10655A
-
|
ACT-058362 hydrochloride
|
Urotensin Receptor
|
Cardiovascular Disease
|
|
Palosuran hydrochloride (ACT-058362 hydrochloride) is a potent, selective, and orally active antagonist of urotensin II receptor, with an IC50 of 3.6 nM for CHO cell membranes expressing human recombinant receptors. Palosuran hydrochloride can improves pancreatic and renal function in diabetic rats .
|
-
- HY-N1131B
-
|
2,2,6,6-Tetramethyl-4-piperidone monohydrate
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
Triacetonamine (2,2,6,6-Tetramethyl-4-piperidone) monohydrate is used as an intermediate for the synthesis of pharmaceutical products, pesticides and photostabilizers for polymers. Triacetonamine hydrochloride has oral activity and can induce acute liver failure (ALF) in rats .
|
-
- HY-114538
-
|
|
Others
|
Cardiovascular Disease
Inflammation/Immunology
|
|
Asobamast is a potent, orally active antiallergic agent that inhibits ige mediated passive pulmonary allergic responses in rats (ED50=4.7 mg/kg) and inhibits antigen-induced mediator release from sensitized guinea pig lung fragments .
|
-
- HY-115447
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Clobenpropit is a potent histamine H3-receptor antagonist. Clobenpropit decreases dopamine release and increases histamine levels in the hypothalamus. Clobenpropit shows antipsychotic-like activities. Clobenpropit causes a resuscitating effect in rats subjected to the hemorrhagic shock .
|
-
- HY-N1131A
-
|
2,2,6,6-Tetramethyl-4-piperidone hydrochloride
|
Biochemical Assay Reagents
|
Metabolic Disease
|
|
Triacetonamine (2,2,6,6-Tetramethyl-4-piperidone) hydrochloride is used as an intermediate for the synthesis of pharmaceutical products, pesticides and photostabilizers for polymers. Triacetonamine hydrochloride has oral activity and can induce acute liver failure (ALF) in rats .
|
-
- HY-111314
-
|
5-Hydroxy-1-methylhydantoin
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
NZ 419 (5-Hydroxy-1-methylhydantoin) is a metabolite of creatinine and an antioxidant with oral activity, which has the ability to scavenge hydroxyl radicals (•OH). NZ 419 can inhibit the progression of chronic kidney disease (CKD) in rats .
|
-
- HY-120329
-
|
|
mAChR
|
Others
|
|
Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .
|
-
- HY-114941
-
|
BP1137
|
Angiotensin-converting Enzyme (ACE)
Neprilysin
|
Cardiovascular Disease
|
|
Aladotril (BP1137) is the inhibitor for neutral endopeptidase (NEP) and angiotensin-converting enzyme (ACE), that ameliorates the cardiac hypertrophy in rats, without decreasing the blood pressure. Aladotril can be used in research about heart failure and cardiac remodeling after myocardial infarction .
|
-
- HY-Z0478
-
|
(S)-(-)-Limonene
|
Bacterial
Antibiotic
CaMK
|
Infection
Cardiovascular Disease
Metabolic Disease
|
|
(-)-Limonene ((S)-(-)-Limonene) is orally active and can cause mild bronchoconstriction. (-)-Limonene alleviates cytosolic and mitochondrial oxidative stress by inhibiting the increase of calcium ions (Ca 2+) and Ca 2+/calmodulin-dependent protein kinase II (CaMKII). It also exerts anti-stress effects by inhibiting the activity of the hypothalamic-pituitary-adrenal (HPA) axis. Additionally, (-)-Limonene can be used as an antibacterial agent in aquaculture .
|
-
- HY-149316
-
|
|
E1/E2/E3 Enzyme
|
Cardiovascular Disease
|
|
Smurf1-IN-1 is an orally active and selective inhibitor of specific E3 ubiquitin protein ligase 1 (SMURF1) with an IC50 of 92 nM. Smurf1-IN-1 has significant efficacy in rats model of pulmonary hypertension .
|
-
- HY-16983
-
|
|
ROR
|
Inflammation/Immunology
|
|
GNE-3500 is a selective, orally active antagonist for Retinoic Acid Receptor-Related Orphan Receptor C (RORc, also known as RORγ or NR1F3) with an EC50 of 12 nM. GNE-3500 exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-B1448
-
|
KW-3049
|
Calcium Channel
Apoptosis
|
Cardiovascular Disease
|
|
Benidipine hydrochloride is an orally active calcium channel antagonist. Benidipine hydrochloride can inhibit cell proliferation and apoptosis. Benidipine hydrochloride has antioxidant activity and can increase nitric oxide synthase activity and improve coronary circulation in hypertensive rats .
|
-
- HY-P1338A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats .
|
-
- HY-B1448A
-
|
KW-3049 free base
|
Apoptosis
Calcium Channel
|
Cardiovascular Disease
|
|
Benidipine is a potent and orally active calcium channel antagonist . Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells . Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats .
|
-
- HY-106364
-
|
Bleomycin PEP; Pepleomycin
|
Antibiotic
|
Cancer
|
|
Peplomycin (Bleomycin PEP; Pepleomycin) is an antibiotic analogue of Bleomycin (HY-108345), with high antitumor effect and less pulmonary toxicity. Peplomycin induce apoptosis in oral squamous carcinoma cell line SSCKN cells and pulmonary fibrosis in rats .
|
-
- HY-148565
-
|
|
Serotonin Transporter
|
Neurological Disease
|
|
SERT-IN-2 is a potent SERT inhibitor (IC50=0.58 nM) with promising anti-depression efficacy. SERT-IN-2 shows good bioavailability of 83.28% in rats. SERT-IN-2 can cross the blood-brain barrier .
|
-
- HY-107565
-
|
|
Others
|
Inflammation/Immunology
|
|
2-Pyridylethylamine is a histamine-1 (H1R) receptor agonist. 2-Pyridylethylamine can reduce the joint injury induced by formalin in rats. 2-Pyridylethylamine can be used to study the spinal cord release of neuropeptide (NPY) .
|
-
- HY-112528
-
|
GP-NPEA
|
Others
|
Metabolic Disease
|
|
Glycerophospho-N-palmitoyl ethanolamine (GP-NPEA) is a metabolic precursor of palmitoyl ethanolamide PEA (HY-157829). Glycerophospho-N-palmitoyl ethanolamine decreases in the cortex of CUMS rats, which may be related to a disorder in the endocannabinoid system arising after the onset of depression .
|
-
- HY-106874
-
|
RS-15385-197
|
Adrenergic Receptor
|
Others
|
|
Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist. Delequamine can increase the sexual behavior score of both male and female rats and can be used in the research of sexual dysfunction .
|
-
- HY-A0148B
-
|
(-)-SKF-102886 free base; (-)-WR-171669
|
Parasite
|
Infection
|
|
(-)-Halofantrine ((-)-SKF-102886 free base; (-)-WR-171669) is an inhibitor of the malignant malaria parasite (P. falciparum) and targets multidrug-resistant P. falciparum. The pharmacokinetic parameters of (-)-Halofantrine in rats vary depending on the route of administration, distinguishing it from other isomers .
|
-
- HY-123294
-
|
YRC 2388; BAY-YRC 2388; NBA 061
|
Others
|
Neurological Disease
Metabolic Disease
|
|
Fentrazamide (YRC 2388) is a herbicide. Fentrazamide has specific toxic effects on the nervous system and erythrocytes in rats, affecting the energy supply of cells mainly by interfering with the glycolysis process. Fentrazamide can be used as a useful tool to study the mechanisms of neurodegenerative diseases and erythrocyte dysfunction .
|
-
- HY-105485
-
|
|
Others
|
Neurological Disease
Metabolic Disease
|
|
FR-62765 is a derivative of WF-3681. FR-62765 can significantly inhibit the accumulation of sorbitol in the sciatic nerve and the decrease of motor nerve conduction velocity in the tail of diabetic neuropathy rats, which can be used in the research of diabetic neuropathy .
|
-
- HY-19136
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
WAY-100289 is an orally active antagonist for 5-HT3 receptor, that exhibits high affinity to the isolated rat vagus nerves with pA2 of 8.9. WAY-100289 inhibits the Bezold-Jarisch reflex in anesthetized and awake rats .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-123284
-
|
|
Others
|
Others
|
|
LY137150 (2) and LY163252 (4) are products of LY175326 metabolism in rats or dogs. The preparation of LY175326 labeled with 14C at the methylthiol group provides a sensitive method to determine whether the metabolically produced LY137150 (2) is further metabolized by S-demethylation.
|
-
- HY-15066
-
|
FG9065
|
iGluR
|
Neurological Disease
|
|
CNQX (FG9065) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX is a competitive non-NMDA receptor antagonist . CNQX blocks the expression of fear-potentiated startle in rats .
|
-
- HY-111583
-
|
|
RXFP Receptor
|
Metabolic Disease
|
|
RXFP3/4 agonist 1 is an agonist of relaxin family peptide 3/4 receptor (RXFP3/4), with EC50s of 82/2 nM, respectivley. RXFP3/4 agonist 1 increases food intake in rats .
|
-
- HY-N3015
-
|
|
Others
|
Metabolic Disease
|
|
Bruceine E is a quassinoid from seeds of Brucea javanica (L.) Merr, exhibiting hypoglycemia effect . Bruceine E exhibits blood glucose lowering effect in both nondiabetic mice and Streptozotocin (STZ (HY-13753))-induced diabetic rats at lower dose .
|
-
- HY-N0495
-
|
Aloenin A
|
Beta-secretase
|
Neurological Disease
|
|
Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitory activity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release.
|
-
- HY-108295
-
|
CXB-722
|
GABA Receptor
|
Neurological Disease
|
|
Pivagabine (CXB 722) is a hydrophobic 4-aminobutyric acid derivative with neuromodulatory activity. Pivagabine penetrates the blood-brain barrier in rats. Pivagabine antagonizes the effects of foot shock on both GABAA receptor function and corticotropin-releasing factor (CRF) concentrations in rat brain .
|
-
- HY-121149
-
|
3-Hydroxytamoxifen
|
Estrogen Receptor/ERR
Apoptosis
|
Cancer
|
|
Droloxifene, a Tamoxifen derivative, is an orally active and selective estrogen receptor modulator. Droloxifene shows antiestrogenic and anti-implantation effects. Droloxifene induces p53 expression and apoptosis in MCF-7 cells. Droloxifene prevents bone loss in ovariectomized rats .
|
-
- HY-131034
-
|
|
Wnt
|
Others
|
|
LP-922056 is an orally active, highly potent Notum Pectinacetylesterase inhibitor with EC50s of 21 nM, 55 nM in human and mouse cellular assay, respectively. LP-922056 significantly increases midshaft femur cortical bone thickness in mice and rats .
|
-
- HY-145633
-
|
OPT 302; VGX-300
|
VEGFR
|
Cardiovascular Disease
|
|
Sozinibercept (OPT 302; VGX-300) is a soluble form of VEGFR-3, potently inhibits the activity of VEGF-C/D, which are the proangiogenic factors, inhibiting angiogenesis and vascular leakage. Sozinibercept also inhibits diabetic retinal edema in rats .
|
-
- HY-N1131S
-
-
- HY-107055
-
|
|
Dopamine Transporter
|
Neurological Disease
|
|
RTI 336 is a phenyltropane analog, as well as a potent and selective dopamine transporter (DAT) inhibitor. RTI 336 inhibits addictive agent induced locomotor activity and self-administration in Lewis rats. RTI 336 exhibits inhibitory effects depending on inherent NAc DAT levels .
|
-
- HY-110116
-
|
|
MMP
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
SD-2590 hydrochloride is a potent MMP inhibitor with IC50 values of ﹤0.1, ﹤0.1, 0.18, and 1.7 nM for MMP2, MMP13, MMP9, and MMP8, respectively. SD-2590 hydrochloride inhibits dilation of the left ventricle in rats .
|
-
- HY-W010655
-
|
TAK-875 hemihydrate
|
Free Fatty Acid Receptor
|
Metabolic Disease
|
|
Fasiglifam (TAK-875) hemihydrate is a potent, selective and orally active GPR40 agonist with EC50 of 72 nM. Fasiglifam enhances glucose-dependent insulin secretion and improves hyperglycemia in type 2 diabetic rats. Fasiglifam can induce liver injury .
|
-
- HY-P10148
-
|
Ac-[Leu28,31]-NPY (24-36)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) attenuates cardiac vagal action in anaesthetised rats .
|
-
![N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36)](//file.medchemexpress.eu/product_pic/hy-p10148.gif)
- HY-126907
-
-
- HY-135026
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
DL-Norepinephrine tartrate is a neurotransmitter, which targets adrenergic receptors, and causes large-amplitude sleep-like electrical activity in the neocortex and suppresses electroencephalography (EEG) activity in the hippocampus. DL-Norepinephrine tartrate results in head shake, difficulty walking, and frequent posture changes in rats model .
|
-
- HY-147152
-
|
|
Others
|
Others
|
|
1-Myristoyl-3-chloropropanediol is a 3-monochloropropanediol (3-MCPD) fatty acid ester. 3-MPCD causes nephropathy and tubular hyperplasia and adenomas by chronic oral administration; also reduces fertility, or provokes infertility in rats and suppresses the immune function .
|
-
- HY-101679
-
|
|
mAChR
|
Neurological Disease
|
|
YM-58790 is a potent antagonist of mAChR. YM-58790 binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
|
-
- HY-100287
-
|
|
Prostaglandin Receptor
Phospholipase
|
Endocrinology
|
|
2-(E-2-decenoylamino)ethyl 2-(cyclohexylethyl) sulfide is a compound that inhibits stress-induced ulcer and low toxicity, and can maintain the content of phospholipase A2 and prostaglandin E2 in ulcerated rats induced by water immersed restrained stress.
|
-
- HY-109897
-
-
- HY-157495
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
EP3 antagonist 6 (compound 5) is a potent, orally and selective EP3 receptor antagonist, with an IC50 of 1.9 nM. EP3 antagonist 6 can inhibits PGE2-induced (HY-101952) uterine contraction in pregnant rats .
|
-
- HY-118706
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
PD 118440 is an orally active dopamine (DA) agonist. PD 118440 has significant central nervous system effects, including inhibition of striatal DA synthesis, suppression of DA neuron firing, and reversal of Reserpine (HY-N0480)-induced depression in rats .
|
-
- HY-12159
-
|
|
Integrin
|
Inflammation/Immunology
|
|
MK-0668 is an amino acid-based, potent antagonist of unactivated VLA-4, with an IC50) of 0.13 nM in human whole blood. And MK-0668 exhibits IC50s of 0.19 nM in dogs, 0.21 nM in rhesus monkeys, and 0.4 nM in rats .
|
-
- HY-116930
-
|
|
Melatonin Receptor
|
Metabolic Disease
|
|
S-20928 is an antagonist for melatonin receptor through inhibition of binding of melatonin to its receptors. S-20928 enhances the 2-Deoxy-D-glucose (2DG) (HY-13966)-induced increase in blood glucose and glucagon levels in rats brain .
|
-
- HY-116625
-
|
|
GHSR
|
Neurological Disease
|
|
PF-04628935 (compound 10n) is a potent ghrelin receptor inverse agonist, with an IC50 of 4.6 nM. PF-04628935 exhibits oral bioavailability of 43% in rats and shows reasonable penetration into the brain. PF-04628935 can be used for stress and anxiety research .
|
-
- HY-109058
-
|
QGC001; RB150
|
Aminopeptidase
|
Cardiovascular Disease
|
|
Firibastat (QGC001), an orally active brain penetrating proagent of EC33, is a first-in-class brain aminopeptidase A (APA) inhibitor (Ki=200 nM). Firibastat selectively and specifically inhibits conversion of brain angiotensin-II into angiotensin-III and decreases blood pressure in hypertensive rats .
|
-
- HY-B1869
-
|
|
Others
|
Others
|
|
Metsulfuron-methyl is a systemic sulfonylurea herbicide that has been widely used to control broadleaf weeds and annual grasses in rice, corn, wheat, and barley. Metsulfuron-methyl exhibits high herbicidal activity and low mammalian toxicity, with an LD50 for rats exceeding 5000 mg/kg .
|
-
- HY-111475
-
|
|
Mitochondrial Metabolism
|
Cardiovascular Disease
|
|
Mitochondrial fusion promoter M1 is a mitochondrial dynamic modulator. Mitochondrial fusion promoter M1 preserves the mitochondrial function and promotes cellular respiration. Mitochondrial fusion promoter M1 alleviates cardiac and brain damage in rats with cardiac ischemia/reperfusion injury .
|
-
- HY-13964A
-
|
|
GHSR
|
Metabolic Disease
|
|
YIL781 hydrochloride is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 hydrochloride produces a greater improvement in glucose homeostasis in rats. YIL781 hydrochloride inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively .
|
-
- HY-154829A
-
|
|
Others
|
Inflammation/Immunology
|
|
AC-099 hydrochloride (compound 3) is a selective NPFF2R full agonist (EC50=1189 nM) and NPFF1R partial agonist (EC50=2370 nM). AC-099 hydrochloride attenuates spinal nerve ligation-induced hypersensitivity in rats .
|
-
- HY-13964
-
|
|
GHSR
|
Metabolic Disease
|
|
YIL781 is a potent and orally active ghrelin receptor (GHSR) antagonist. YIL781 produces a greater improvement in glucose homeostasis in rats. YIL781 inhibits the calcium response induced by ghrelin with pIC50 values of 7.90 and 8.27, respectively .
|
-
- HY-154829
-
|
|
Others
|
Inflammation/Immunology
|
|
AC-099 (compound 3) is a selective NPFF2R full agonist (EC50=1189 nM) and NPFF1R partial agonist (EC50=2370 nM). AC-099 attenuates spinal nerve ligation-induced hypersensitivity in rats .
|
-
- HY-P2046
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
β-Endorphin (rat) is an endogenous opioid neuropeptide and peptide hormone. β-Endorphin (rat) has analgesic activity and also contributes to food intake in satiated rats. β-Endorphin (rat) can be used in the research of neurological diseases such as analgesia and drug addiction .
|
-
- HY-135761R
-
|
|
Fungal
Cholinesterase (ChE)
|
Infection
Neurological Disease
|
|
Penconazole (Standard) is the analytical standard of Penconazole. This product is intended for research and analytical applications. Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats .
|
-
- HY-B1301R
-
|
|
Histamine Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Triprolidine (hydrochloride monohydrate) (Standard) is the analytical standard of Triprolidine (hydrochloride monohydrate). This product is intended for research and analytical applications. Triprolidine hydrochloride monohydrate, a first-generation antihistamine, is an oral active histamine H1 antagonist. Triprolidine hydrochloride monohydrate can be used for the research of allergic rhinitis. Triprolidine hydrochloride monohydrate exhibits spinal motor and sensory block in rats .
|
-
- HY-118751
-
|
Bancol
|
nAChR
|
Others
Neurological Disease
|
|
Bensultap (Bancol) is an insecticide, which can control Colorado beetle and some other insect pests. Bensultap is a modulator for nicotinic acetylcholine receptor (nAChR), and exhibits mild and temporary neuromodulatory efficacy on rat nervous system .
|
-
- HY-14542A
-
|
CP-88059 hydrochloride
|
5-HT Receptor
Dopamine Receptor
|
Neurological Disease
|
|
Ziprasidone (CP-88059) hydrochloride is an orally active combined 5-HT and dopamine receptor antagonist . Ziprasidone hydrochloride has affinities for Rat D2 (Ki=4.8 nM), 5-HT2A (Ki=0.42 nM) and 5-HT1A (Ki=3.4 nM) .
|
-
- HY-12402
-
|
|
PCSK9
|
Cardiovascular Disease
|
|
SBC-115076 is a potent proprotein convertase subtilisin/kexin type 9 (PCSK9) inhibitor. PCSK9 is a proprotein convertase, which plays a crucial role in LDL receptor metabolism .
|
-
- HY-P1025
-
-
- HY-N8196
-
|
Isorhamnetin-3,7-diglucoside; Isorhamnetin diglucoside
|
Others
|
Metabolic Disease
|
|
Isorhamnetin 3,7-di-O-β-D-glucopyranoside, a major flavonoid compound, is metabolized in vivo by intestinal bacteria to isorhamnetin and that isorhamnetin plays an important role as an antioxidant .
|
-
- HY-19431
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
Ro 46-8443 is the first non-peptide endothelin ETB receptor selective antagonist. Ro 46-8443 displays an at least 100-fold selectivity for ETB (IC50: 34-69 nM) over ETA receptors (IC50: 6800 nM) .
|
-
- HY-P3064
-
|
Leiurotoxin I
|
Potassium Channel
|
Neurological Disease
|
|
Scyllatoxin (Leiurotoxin I) is a peptide toxin, it can be isolated from the venom of the scorpion (Leiurus quinquestriatus hebraeus). Scyllatoxin is a blocker of small-conductance KCa (SK) channel. Scyllatoxin enhances both norepinephrine (NE) and epinephrine (Epi) release in vivo .
|
-
- HY-107398
-
|
|
Others
|
Cardiovascular Disease
|
|
1-(2,3-Dichlorophenyl)ethanamine hydrochloride is a phenylethanolamine N-methyltransferase (PNMT) inhibitor. 1-(2,3-Dichlorophenyl)ethanamine hydrochloride effectively reduces blood pressure of spontaneously hypertensive. 1-(2,3-Dichlorophenyl)ethanamine hydrochloride can be used for the research of blood pressure .
|
-
- HY-106816
-
-
- HY-153192A
-
|
BI 1015550 dihydrate
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Nerandomilast (BI 1015550) dihydrate is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast (dihydrate) has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-153192
-
|
BI 1015550
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
Nerandomilast (BI 1015550) is an orally active inhibitor of PDE4B with an IC50 value of 7.2 nM. Nerandomilast has good safety and potential applications in inflammation, allergic diseases, pulmonary fibrosis, and chronic obstructive pulmonary disease (COPD) .
|
-
- HY-100356
-
|
CNS 1102 free base
|
iGluR
|
Neurological Disease
|
|
Aptiganel (CNS 1102 (free base)), peptide, is a noncompetitive NMDA antagonist with cerebroprotective effects. Aptiganel can be used for the research of stroke .
|
-
- HY-122076
-
|
|
Antibiotic
Bacterial
Fungal
|
Infection
|
|
A-26771B is an antibiotic can be obtained from Penicillium turbatum. A-26771B exhibits moderate antimicrobial activity against Gram-positive bacteria, mycoplasma, and fungi. A-26771B also inhibits potassium-dependent ATPase in rat liver mitochondria .
|
-
- HY-131696
-
|
11-deoxy PGF1α
|
Others
|
Cardiovascular Disease
Others
|
|
11-deoxy Prostaglandin F1α (11-deoxy PGF1α) is an analog of prostaglandin F1α, exhibits side effects on intestines and causes the uterine contraction. 11-deoxy Prostaglandin F1α exhibits activity as vasopressor and bronchoconstrictor .
|
-
- HY-P1025A
-
-
- HY-163536
-
|
|
TGF-beta/Smad
|
Inflammation/Immunology
|
|
TGF-β1/Smad3-IN-1 (Compound 5aa) is an inhibitor of the TGF-β1/Smad3 signaling pathway(IC50=1.07 μM). TGF-β1/Smad3-IN-1 possesses antifibrotic activity and oral potency .
|
-
- HY-129415
-
|
Hexaprazole
|
Others
|
Others
|
|
Esaprazole (Hexaprazole) is an antiulcer agent that has the effect of promoting the healing of peptic ulcer. Esaprazole can inhibit the secretion of gastric acid and pepsin .
|
-
- HY-161512
-
|
|
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
hAChE/hBACE-1-IN-4 (compound AK-2) is a quinazoline derivative. hAChE/hBACE-1-IN-4 shows significant inhibitory activity against hAChE and hBACE-1 enzymes (hAChE, IC50=0.283 μM; hBACE-1, IC50=0.231 μM). hAChE/hBACE-1-IN-4 has the potential to inhibit Aβ aggregation. hAChE/hBACE-1-IN-4 has non-neurotoxicity , blood-brain barrier permeability and oral activity. hAChE/hBACE-1-IN-4 can be used in Alzheimer's disease research .
|
-
- HY-121678
-
|
POLI-67
|
Others
|
Inflammation/Immunology
|
|
Tetridamine is a non-steroidal anti-inflammatory agent and shows a marked reduction of paw swelling and pain sensibility .
|
-
- HY-P3429
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-100986B
-
|
|
NO Synthase
|
Cardiovascular Disease
|
|
L-NIO is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively . L-NIO induces a consistentfocal ischemic infarctin rats .
|
-
- HY-100986
-
|
|
NO Synthase
|
Cardiovascular Disease
|
|
L-NIO dihydrochloride is a potent, non-selective and NADPH-dependent nitric oxide synthase (NOS) inhibitor, with Kis of 1.7, 3.9, 3.9 μM for neuronal (nNOS), endothelial (eNOS), and inducible (iNOS), respectively . L-NIO dihydrochloride induces a consistentfocal ischemic infarctin rats .
|
-
- HY-18332C
-
|
|
Serotonin Transporter
Dopamine Transporter
|
Neurological Disease
|
|
DOV-216,303 (Free Base) is a potent triple serotonin, norepinephrine, and dopamine reuptake inhibitor, with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively . Has antidepressant-like effects and increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats .
|
-
- HY-14858
-
|
SLV 320
|
Adenosine Receptor
|
Cardiovascular Disease
|
|
Derenofylline (SLV 320) is a potent, selective and orally active adenosine A1 receptor antagonist, with Ki values of 1 nM, 200 nM and 398 nM for human A1, A3 and A2A receptors respectively. Derenofylline suppresses cardiac fibrosis and attenuates albuminuria without affecting blood pressure in rats .
|
-
- HY-103460
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
IRL 2500 is a potent Endothelin receptor antagonist. IRL 2500 shows IC50 values of 1.3 and 94 nM for ETB and ETA receptors, respectively. IRL 2500 inhibits ETB receptor-mediated blood pressure increase and renal vascular resistance in rats in vivo .
|
-
- HY-122666
-
|
|
GlyT
|
Metabolic Disease
|
|
Org 25935 is a potent and selective glycine transporter 1 protein (GlyT1) inhibitor with an IC50 value of 100 nM. Org 25935 can decrease ethanol (EtOH) intake and EtOH preference in rats, whereas water intake is unaffected. Org 25935 can be used for researching alcohol dependence or abuse .
|
-
- HY-P10039
-
|
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-16) rat is a β-amyloid peptide (Abeta), a metal-binding domain fragment of amyloid. Three amino acid substitutions in β-Amyloid (1-16) rat that differ from humans render rats and mice less susceptible to AD-like neurodegeneration .
|
-
- HY-D1005A16
-
|
PEG-PPG-PEG, 4600 (Averag)
|
Biochemical Assay Reagents
|
Others
|
|
Poloxamer 235 P85 is block polymer of polyoxyethylene and polyoxypropylene with average molecular mass of 4600. Poloxamer 235 P85 exhibits acute and subchronic toxicity in albino rats with an oral LD50 of >34.6 g/kg. Poloxamer 235 P85 induces ocular irritation in rabbits .
|
-
- HY-120381
-
|
CAM 1189
|
Cholecystokinin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
PD 136450 (CAM 1189) is an antagonist for cholecystokinin 2 (CCK2). PD 136450 exhibits anti-secretory, anxiolytic and anti-ulcer activities, inhibits gastric acid secretion (IC50=1 mg/kg), and ameliorates the haemorrhagic lesions (IC50=4.7 mg/kg) in rats .
|
-
- HY-112746
-
|
DPC974; GW5638
|
Estrogen Receptor/ERR
|
Cancer
|
|
Etacstil (GW5638) is a estrogen receptor antagonist that displays minimal uterotropic activity in ovariectomized rats and inhibits the agonist activity of Estradiol (HY-B0141), Tamoxifen (HY-13757A) and Raloxifene (HY-13738) in the environment. Etacstil is promising for research of breast cancer and bone protection .
|
-
- HY-D1056
-
|
LPS
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Lipopolysaccharides, from E. coli O55:B5 is an endotoxin extracted from E. coli O55:B5, consisting of an antigen-specific chain, A core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O55:B5 activates TLR-4 of immune cells. Lipopolysaccharides, from E. coli O55:B5 can induce the change of body temperature in rats with dose and serotype specificity. Lipopolysaccharides, from E. coli O55:B5 caused a heterogeneous and dose-independent increase in body temperature in rats .
|
-
- HY-155553
-
|
|
GPR119
|
Metabolic Disease
|
|
GPR119 agonist 2 (compound 43) is an orally active GPR119 agonist. GPR119 agonist 2 shows good pharmacokinetic characteristics in rodents and can effectively improve glucose tolerance in mice and rats. GPR119 agonist 2 has the potential to study type 2 diabetes .
|
-
- HY-113854
-
|
|
Glucocorticoid Receptor
|
Cardiovascular Disease
Endocrinology
|
|
AZD2906 is a selective glucocorticoid receptor (GR) agonist, increases micronucleated immature erythrocytes in the bone marrow of rats. AZD2906 shows IC50s of 2.2, 0.3, 41.6 and 7.5 nM at GR in human, rat PBMC and human, rat whole blood, respectively .
|
-
- HY-103023
-
CLP290
1 Publications Verification
|
Potassium Channel
|
Neurological Disease
|
|
CLP290 is an orally available activator of the neuron-specific K +-Cl ? cotransporter KCC2, displays potential for treatment of a wide range of neurological and psychiatric indications. CLP290 can significantly lower blood arginine-vasopressin (AVP) and glucose levels in STZ (HY-13753) rats .
|
-
- HY-15066A
-
|
FG9065 disodium
|
iGluR
|
Neurological Disease
|
|
CNQX disodium (FG9065 disodium) is a potent and competitive AMPA/kainate receptor antagonist with IC50s of 0.3 μM and 1.5 μM, respectively. CNQX disodium is a competitive non-NMDA receptor antagonist . CNQX disodium blocks the expression of fear-potentiated startle in rats .
|
-
- HY-19037
-
|
|
Adrenergic Receptor
|
Neurological Disease
Metabolic Disease
|
|
SM-2470 is a potent α1-adrenoceptor antagonist, has sympathetic nerve activity in anesthetized rats . SM-2470 is an antihypertensive agent. SM-2470 exhibits hypocholesterolaemic effect by the inhibition of cholesterol absorption related to the reduction of cholesterol solubilization .
|
-
- HY-137976
-
|
Penequinine hydrochloride
|
mAChR
NF-κB
|
Inflammation/Immunology
|
|
Penehyclidine (Penequinine) hydrochloride, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine hydrochloride activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine hydrochloride can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation .
|
-
- HY-144303
-
|
|
Xanthine Oxidase
|
Metabolic Disease
|
|
Xanthine oxidase-IN-4 (compound 19a) is an orally active and potent xanthine oxidase (XO) inhibitor, with an IC50 of 0.039 μM. Xanthine oxidase-IN-4 exhibits hypouricemic potency in potassium oxonate induced hyperuricemia rats. Xanthine oxidase-IN-4 can be used for hyperuricemia and gout research .
|
-
- HY-142119
-
|
|
mAChR
NF-κB
|
Inflammation/Immunology
|
|
Penehyclidine, a anticholinergic agent, is a selective antagonist of M1 and M3 receptors. Penehyclidine activates NF-kβ in lung tissue and inhibits the release of inflammatory factors. Penehyclidine can alleviate the pulmonary inflammatory response in rats with chronic obstructive pulmonary disease (COPD) undergoing mechanical ventilation .
|
-
- HY-100812
-
|
|
GABA Receptor
|
Neurological Disease
Endocrinology
|
|
2-Hydroxysaclofen is a potent γ-amino-butyric-acid-B (GABAB) receptor antagonist. 2-Hydroxysaclofen can abolish nicotine-induced hypolocomotor effects and increases the antinociceptive effects. 2-Hydroxysaclofen can stimulate luteinizing hormone (LH) secretion in female rats .
|
-
- HY-152927
-
|
|
Biochemical Assay Reagents
|
Others
|
|
Hydroxypropylmethyl cellulose acetate succinate (Mw: 20-100k Da) is a cosolvent for preparing SDDs of low-solubility agents. Hydroxypropylmethyl cellulose acetate succinate (Mw: 20-100k Da) exhibits no acute/subchronic/chronic toxicity in rats, with oral activity and LD50 >2.5 g/kg .
|
-
- HY-118497
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
Metabolic Disease
|
|
BMS 182874 is an orallyactive, highly selective endothelin receptor (ETA receptor) antagonist, with IC50 value of 0.150 μM, Ki of 0.055 μM. BMS 182874 reduces the arterial pressure of Deoxycorticosterone acetate (HY-B1472) induced hypertension model in rats, and can be used for cardiovascular disease research .
|
-
- HY-B0235R
-
|
|
Others
|
Metabolic Disease
|
|
Trichlormethiazide (Standard) is the analytical standard of Trichlormethiazide. This product is intended for research and analytical applications. Trichlormethiazide is an orally active thiazide diuretic, with antihypertensive effect. Trichlormethiazide increases urine volume (UV), Na and K excretion and tends to improve the depressed creatinine clearance (CCRE) in acute renal failure rats model .
|
-
- HY-N0723R
-
|
|
Others
|
Metabolic Disease
|
|
Neomangiferin (Standard) is the analytical standard of Neomangiferin. This product is intended for research and analytical applications. Neomangiferin is a natural C-glucosyl xanthone isolated from m the dried rhizome of Anemarrhena asphodeloides. Neomangiferin has significant therapeutic effects on high-fat diet-induced nonalcoholic fatty liver disease (NAFLD) in rats .
|
-
- HY-116211
-
|
WIN-25978
|
Biochemical Assay Reagents
|
Neurological Disease
|
|
Amfonelic acid (WIN-25978) is a highly selective dopamine reuptake inhibitor. Amfonelic acid interferes with the in vitro neuronal uptake of norepinephrine in the iris of rats, but does not alter the concentrations of norepinephrine or dopamine in the whole mouse brain. Amfonelic acid can be used as a pharmacological tool to study the brain reward system, dopamine pathway and dopamine transporter .
|
-
- HY-156684
-
|
|
TRP Channel
|
Neurological Disease
|
|
GDC-6599 is an orally active TRPA1 inhibitor, with IC50 values of 5.3 nM in humans, 6.6 nM in rats, 9.3 nM in dogs, 7.2 nM in monkeys, and 15 nM in guinea pigs. GDC-6599 can be used in the research of neuropathic pain and respiratory diseases such as asthma and chronic cough .
|
-
- HY-100968
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
GBR 12783 dihydrochloride is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 dihydrochloride can improve memory performance and increase hippocampal acetylcholine release in rats .
|
-
- HY-W008610
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
GBR 12783 is a specific, potent and selective dopamine uptake inhibitor that inhibits the [ 3H]dopamine uptake by rat and mice striatal synaptosomes with IC50s of 1.8 nM and 1.2 nM, respectively. GBR 12783 can improve memory performance and increase hippocampal acetylcholine release in rats .
|
-
- HY-16100
-
|
|
Fatty Acid Synthase (FASN)
|
Metabolic Disease
Cancer
|
|
BI 99179 is a potent and selective type I fatty acid synthase (FAS) inhibitor with an IC50 of 79 nM. BI 99179 is a tool compound suitable for the in vivo validation of FAS as a target for lipid metabolism related diseases. BI 99179 exhibits significant exposure (both peripheral and central) upon oral administration in rats .
|
-
- HY-110184
-
|
|
Potassium Channel
|
Neurological Disease
|
|
PK-THPP is a potent TWIK-related acid-sensitive K(+) ion channel (TASK-3 ion channel) blocker (IC50s are 35 nM and 300 nM for TASK-3 and TASK-1, respectively) . PK-THPP increases breathing rate and induces respiratory alkalosis in rats .
|
-
- HY-157931
-
|
|
Histamine Receptor
|
Neurological Disease
|
|
Anticancer agent 192 (compound XXI) is a steroid-based histamine H3 receptor antagonist with no affinity for muscarinics and hERG. Anticancer agent 192 is quite stable in human and rat liver microsomes. Anticancer agent 192 can improve the cognitive level and reduce the degree of addiction in rats in the in vivo addiction test .
|
-
- HY-14466
-
|
|
Prostaglandin Receptor
|
Endocrinology
|
|
GW 848687X is a selective, orally active prostaglandin EP1 receptor antagonist for the inhibition of inflammatory pain. The oral bioavailability of GW 848687X was 54% in rats and 53% in dogs. GW 848687X has a half-life of 2 hours and has inhibitory potential for both acute and chronic pain .
|
-
- HY-162459
-
|
|
Cyclic GMP-AMP Synthase
|
Inflammation/Immunology
|
|
cGAS-IN-3 (compound 30d-S) is an orally active cyclic GMP-AMP synthase (Cyclic GMP-AMP Synthase/cGAS) inhibitor with good plasma exposure and low clearance. cGAS-IN-3 has anti-inflammatory activity and can significantly reduce lung inflammation in rats .
|
-
- HY-120820
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
LY320954 is a selective 5-HT2A receptor antagonist, with a Ki of 96 nM. LY320954 potently inhibits Ca 2+ influx in the functional assay (EC50 of 35.5 nM). LY320954 inhibits 5-HT-induced paw swelling in rats, with ED50 of 4.8 mg/kg .
|
-
- HY-N0691R
-
|
|
Autophagy
|
Inflammation/Immunology
Cancer
|
|
Schisandrin (Standard) is the analytical standard of Schisandrin. This product is intended for research and analytical applications. Schisandrin (Schizandrin), a dibenzocyclooctadiene lignan, is isolated from the fruit of Schisandra chinensis Baill. Schisandrin exhibits antioxidant, hepatoprotective, anti-cancer and anti-inflammatory activities. Schisandrin also can reverses memory impairment in rats .
|
-
- HY-134221
-
|
|
Others
|
Cardiovascular Disease
|
S-Nitroso-N-acetylcysteine is a nitric oxide donor. S-Nitroso-N-acetylcysteine has a tissue vascular dilation effect, which can enhance liver microcirculation and effectively prevent ischemia-reperfusion injury in fatty liver. S-Nitroso-N-acetylcysteine can reduce liver fibrosis in rats with cirrhosis .
|
-
- HY-119741
-
|
|
Lipase
|
Metabolic Disease
|
|
Salacinol can be isolated from the roots of the plant Salacia reticulata. Salacinol inhibits fat metabolizing enzymes, such as pancreatic lipase (PL, IC50=12.6 mg/L), lipoprotein lipase (LPL, IC50=13.6 mg/L), and glycerophosphate dehydrogenase (GPDH), enhances the lipolysis, and exhibits antiobesity efficacy in rats .
|
-
- HY-124668
-
|
|
CCR
|
Inflammation/Immunology
|
|
CCR1 antagonist 12 (Compound 12) is an antagonist for CCR1 with IC50 of 3 nM for human CCR1. CCR1 antagonist 12 inhibits CCL3-induced transwell chemotaxis with an IC50 of 0.009 µM. CCR1 antagonist 12 exhibits good pharmacokinetic characters in rats model .
|
-
- HY-115357
-
|
|
PPAR
|
Metabolic Disease
|
|
BMS711939 is a selective agonist for peroxisome proliferator-activated receptor α (PPAR α), with EC50 of 4 nM and 4.5 μM, for human PPARα and human PPARγ. BMS711939 exhibits good pharmacokinetic characters in rats models. BMS711939 increases HDL cholesterol, reduces LDL cholesterol and triglycerides .
|
-
- HY-144110
-
|
|
HCV
|
Infection
|
|
HCV-IN-37 (Compound 3d) is a potent inhibitor of HCV. HCV-IN-37 is orally available and long-lasting in rat plasma after oral administration to rats by a single dose of 15 mg/kg. The high potency of active derivative HCV-IN-37 is primarily driven by the inhibitory effect on the virus entry stage .
|
-
- HY-B0476R
-
|
Acetophenetidin (Standard)
|
COX
|
Inflammation/Immunology
|
|
Phenacetin (Standard) is the analytical standard of Phenacetin. This product is intended for research and analytical applications. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats .
|
-
- HY-N0157
-
|
6-Carboxyuracil; Vitamin B13
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Metabolic Disease
|
|
Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats .
|
-
- HY-N2026
-
|
Propyl parahydroxybenzoate; Propyl 4-hydroxybenzoate
|
Endogenous Metabolite
Bacterial
Apoptosis
|
Infection
|
|
Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods. Propylparaben disrupts follicular growth and steroidogenic function by altering cell cycle, apoptosis and steroidogenic pathways. Propylparaben also reduced sperm count and motility in rats .
|
-
- HY-N0157A
-
|
6-Carboxyuracil zinc; Vitamin B13 zinc
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Metabolic Disease
|
|
Orotic acid (zinc), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid (zinc) is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid (zinc) can induce hepatic steatosis and hepatomegaly in rats .
|
-
- HY-111615
-
|
|
Somatostatin Receptor
|
Neurological Disease
|
|
J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
|
-
- HY-130208
-
|
TDG
|
Galectin
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Thiodigalactoside (TDG) is an orally active and potent galectin (GAL) inhibitor with Kd values of 24 μM, 49 μM for GAL1 and GAL3, respectively . Thiodigalactoside, a non-metabolizable disaccharide, has anti-inflammatory and anti-cancer activity. Thiodigalactoside dramatically reduces body weight gain in diet-induced obese rats .
|
-
- HY-12598
-
|
|
mGluR
|
Neurological Disease
|
|
(S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with Ki values of 0.9 μM and 3.9 μM for mGluR1a and mGluR5a, respectively . (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia .
|
-
- HY-B0816
-
|
|
Others
|
Others
|
|
Etofenprox is an orally active non-ester pyrethroid insecticide. Etofenprox induces toxicity against many pest insects, including Diptera rather than mammalian and fish. Etofenprox has a liver tumor-promoting activity in rats accompanied with microsomal ROS production increase. Etofenprox can be used in agricultural pest control and malaria research .
|
-
- HY-P1216A
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA increases food intake in free-feeding rats .
|
-
- HY-N2026A
-
|
Propyl parahydroxybenzoate sodium; Propyl 4-hydroxybenzoate sodium
|
Endogenous Metabolite
Bacterial
Apoptosis
|
Infection
|
|
Propylparaben sodium (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben sodium is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben sodium disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben sodium also decreases sperm number and motile activity in rats .
|
-
- HY-112257
-
S-23
1 Publications Verification
|
Androgen Receptor
|
Metabolic Disease
|
|
S-23 is an orally active selective androgen receptor modulator (SARM) with a Ki of 1.7 nM. S-23 induces androgen receptor (AR)-mediated transcriptional activation in CV-1 cells. S-23 increases prostate, seminal vesicle, and levator ani muscle weights in castrated rats .
|
-
- HY-118543
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
TM6089 is a unique Prolyl Hydroxylase (PHD) inhibitor which stimulates HIF activity without iron chelation and induces angiogenesis and exerts organ protection against ischemia. Local administration of TM6089 enhances angiogenesis, and oral administration stimulates HIF activity in transgenic rats expressing a hypoxia-responsive reporter vector .
|
-
- HY-103327
-
|
|
Cannabinoid Receptor
|
Metabolic Disease
|
|
MJ15 is a potent and selective CB1 receptor antagonist with a Ki of 27.2 pM and an IC50 of 118.9 pM for rat CB1 receptors. MJ15 exhibits potency in obesity and hyperlipidemia models. MJ15 inhibits food intake and increases in body weight in diet-induced obese rats and mice .
|
-
- HY-100851A
-
|
|
5-HT Receptor
|
Cardiovascular Disease
|
|
LY-272015 hydrochloride is an orally active, specific 5-HT2B receptor antagonist. LY-272015 hydrochloride completely inhibits the phosphorylation of ERK2 induced by 5-HT or BW723C86. LY-272015 hydrochloride is antihypertensive in Deoxycorticosterone Acetate (DOCA)-salt-hypertensive rats .
|
-
- HY-P3429A
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA TFA is conjugated to the cell permeable peptide TAT47-57. SAMβA TFA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-150555
-
|
|
Potassium Channel
|
Others
|
|
P-CAB agent 1 (compound B19) is a highly potent potassium-competitive acid blocker agent with an IC50 value of 60.50 nM for H +/K +-ATPase. P-CAB agent 1 has acceptable oral absorption in rats. P-CAB agent 1 can be used for researching acid-related disorders (ARDs) .
|
-
- HY-151360
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
NHE3-IN-3 (Compound 1) is a Na +/H + exchanger isoform 3 (NHE3) inhibitor with pIC50 of 6.2 and 6.6 against human and rat NHE3, respectively. NHE3-IN-3 shows high (98%) oral bioavailability in Sprague–Dawley rats .
|
-
- HY-101679A
-
|
|
mAChR
|
Neurological Disease
|
|
YM-58790 free base is a potent antagonist of mAChR. YM-58790 free base binds M1, M2, M3 with Ki values of 28 nM, 260 nM, and 15 nM. YM-58790 free base exhibits potent inhibitory activity on bladder pressuer in reflexly-evoked rhythmic contraction in rats .
|
-
- HY-100617
-
|
(S)-4-Carboxyphenylglycine
|
mGluR
|
Neurological Disease
|
|
(S)-4CPG ((S)-4-Carboxyphenylglycine) is a potent mGluR2 agonist. (S)-4CPG reduces hyperalgesia and allodynia associated with sciatic nerve contraction injury in rats. (S)-4CPG can be used in research on neurological diseases .
|
-
- HY-P5914
-
|
WaTx
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-P10046
-
|
|
Vasopressin Receptor
|
Metabolic Disease
|
|
[Deamino-Pen1,Val4,D-Arg8]-vasopressin (AVP-A) is an arginine-vasopressin (AVP) antagonist. AVP-A can significantly lower plasma aldosterone concentration in rats. AVP-A can be used for the research of the growth and steroidogenic capacity of rat adrenal zona glomerulosa .
|
-
![[Deamino-Pen1,Val4,D-Arg8]-vasopressin](//file.medchemexpress.eu/product_pic/hy-p10046.gif)
- HY-D1005A22
-
|
PEG-PPG-PEG, 14600 (Averag)
|
Biochemical Assay Reagents
|
Others
|
|
Poloxamer 338 F108 is block polymer of polyoxyethylene and polyoxypropylene with average molecular mass of 14600. Poloxamer 338 F108 reduces the aggregation of red blood cells, inhibits proliferation of human lymphocyte cell IIBR1. Poloxamer 338 F108 exhibits short-term and subchronic toxicity in rats .
|
-
- HY-120398
-
|
|
PTHR
|
Endocrinology
|
|
CH5447240 is an agonist for parathyroid hormone receptor 1 (PTHR1), that inhibits human PTHR1 with an EC50 of 12 μM. CH5447240 exhibits good metabolic stability in human liver microsomes. CH5447240 increases serum calcium levels in rats. CH5447240 can be used in research about hypoparathyroidism .
|
-
- HY-125540
-
|
|
Influenza Virus
|
Infection
Inflammation/Immunology
|
|
Saussureamine C shows gastroprotective effect on acidified ethanol-induced gastric mucosal lesions in rats. Saussureamine C inhibits H274Y and N294S mutants and can be used for research of influenza virus infection. Saussureamine C can be isolated from the dried roots of Saussurea lappa Clarke .
|
-
- HY-125625
-
|
|
Renin
|
Cardiovascular Disease
|
|
ES 6864 is an orally active, competitive inhibitor for human renin, with an IC50 of 6.9 nM and a Ki of 7.3 nM. ES 6864 exhibits high species-specific and enzyme-specific properties. ES 6864 exhibits metabolic stability in rat tissue homogenates. ES 6864 reduces blood pressure in rats and sodium-depleted awake marmosets .
|
-
- HY-114565
-
|
|
Lipoxygenase
|
Inflammation/Immunology
|
|
LY221068 is an anti-oxidant and an orally active, potent inhibitor of iron-dependent lipid peroxidation and 5-lipoxygenase with antiinflammatory properties. LY221068 inhibits bone damage and paw swelling in the Freund's Complete adjuvant (HY-153808) induced arthritis (FCA) model of rats. LY221068 is promising for research of arthritis .
|
-
- HY-19126
-
|
|
Platelet-activating Factor Receptor (PAFR)
|
Infection
|
|
CL-184005 is an antagonist for platelet-activating factor (PAF), that inhibits the PAF-induced platelet aggregation with IC50 of 600 nM and 510 nM, in human and rabbit platelet-rich plasma. CL-184005 protects the rats from endotoxin-induced gastrointestinal damage and hypotension. CL-184005 exhibits potential attenuating Gram-negative bacterial sepsis .
|
-
- HY-161672
-
|
|
Liposome
IRE1
|
Cancer
|
|
G-5758 is an orally available IRE1α inhibitor with an IC50 of 38 nM for XBP1s. G-5758 is well tolerated in multiple myeloma models (KMS-11) at oral doses up to 500 mg/kg in rats. G-5758 exhibits pharmacodynamics comparable to that of induced IRE1 knockdown .
|
-
- HY-102065
-
|
|
Prostaglandin Receptor
|
Others
|
|
SC-19220 is a competitive prostaglandinn E2 receptor antagonist. SC-19220 increases the bladder capacity and reduced the voiding efficiency of micturition (elicited by slow transvesical filling) of urethane-anesthetized rats. SC-19220 can restores the balance in bone marrow granulocyte and monocyte production after burn sepsis .
|
-
- HY-101422
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
GAL-021 is a potent BKCa-channel blocker. GAL-021 inhibits KCa1.1 in GH3 cells. GAL-021 is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 increases minute ventilation in rats and non-human primates .
|
-
- HY-P1520
-
|
|
GnRH Receptor
|
Neurological Disease
|
|
Prolactin Releasing Peptide (1-31), human is a high affinity GPR10 ligand that cause the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
|
-
- HY-N0264
-
|
Chuanxiongzine; Tetramethylpyrazine
|
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Ligustrazine (Chuanxiongzine), an alkylpyrazine isolated from Ligusticum chuanxiong Hort. (Chuan Xiong) , is present in french fries, bread, cooked meats, tea, cocoa, coffee, beer, spirits, peanuts, filberts, dairy products and soy products as fragrance and flavouring ingredienexhibits. Ligustrazine also has potential nootropic and anti-inflammatory activities in rats .
|
-
- HY-P1428A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
RFRP-1(human) TFA is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
|
-
- HY-115877
-
|
|
TRP Channel
|
Others
|
|
GDC-0334 is a selective TRPA1 antagonist. GDC-0334 inhibits TRPA1 function on airway smooth muscle and sensory neurons by decreasing cough and allergic airway inflammation in rats and guinea pigs. GDC-0334 can be used for TRPA1-mediated diseases research, such as pain or asthma .
|
-
- HY-15522
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
WAY-267464 is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .
|
-
- HY-P1520A
-
|
|
GnRH Receptor
|
Neurological Disease
|
|
Prolactin Releasing Peptide (1-31), human (acetate) is a high affinity GPR10 ligand that causes the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
|
-
- HY-W017457
-
|
(±)-Penicillamine
|
Others
|
Others
|
|
DL-Penicillamine [(±)-Penicillamine] is a copper chelating agent. DL-Penicillamine has antidotal effects in thallotoxicosis rats when co-treated with Prussian blue (HY-106594A). DL-Penicillamine can cause pyridoxine deficiency and then induce optic axial neuritis. DL-Penicillamine can also depress primary immune response .
|
-
- HY-15112
-
|
|
Prolyl Endopeptidase (PREP)
|
Infection
|
|
JTP-4819 is a potent and specific inhibitor of prolyl endopeptidase (PREP) with IC50s of 0.83 nM (in rat brain supernatant) and 5.43 nM (in Flavobacterium meningosepticum). JTP-4819 has blood-brain penetration, also improves the retention time of amnesia rats induced by Scopolamine (HY-N2096) .
|
-
- HY-106054
-
|
|
Prostaglandin Receptor
|
Metabolic Disease
Inflammation/Immunology
|
|
Nocloprost, a prostaglandin E2 (PGE2) analog, is an orally active EP1- and EP3-receptor agonist. Nocloprost inhibits evoked [ 3H]ACh release. Nocloprost has gastroprotective and ulcer-healing properties. Nocloprost accelerates the healing of chronic gastric ulcerations and enhances mucosal growth in rats .
|
-
- HY-105022
-
|
R 58735
|
Tau Protein
|
Neurological Disease
|
|
Sabeluzole (R 58735), a benzothiazol derivative, has antiischemic, antiepileptic, and cognitive-enhancing properties. Sabeluzole protects rat hippocampal neurons against NMDA- and glutamate-induced neurotoxicity via preventing tau expression. Sabeluzole enhances memory in rats, and prevents the amnesic effect of Chlordiazepoxide. Sabeluzole can be used fro research of Alzheimer's disease .
|
-
- HY-155823
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
TZ4M is a 2,4-thiazolidinedione (TZD)-based anti-ADV agent with neuroprotective effects. TZ4M exhibits AChE inhibition in human plasma. TZ4M improves memory and cognitive impairment in adult rats in a scopolamine (HY-N0296)-induced Alzheimer-type model .
|
-
- HY-155822
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
TZ3O (compound TZ30) is an anticholinergic agent with neuroprotective effects. TZ3O (2 mg/kg, 4 mg/kg) can improve memory impairment and cognitive decline in rats in the Scopolamine (HY-N0296)-induced Alzheimer-type model. TZ3O could be used in Alzheimer’s research .
|
-
- HY-19101
-
|
|
Kallikrein
|
Cardiovascular Disease
|
|
ONO-3307 is a protease inhibitor that competitively inhibits a variety of proteases including trypsin, thrombin, plasma kallikrein, plasmin, pancreatic kallikrein, and chymotrypsin. ONO-3307 alleviates endotoxin-induced experimental disseminated intravascular coagulation (DIC) in rats. ONO-3307 can be used in the study of thrombosis and protease-mediated diseases .
|
-
- HY-108679
-
|
|
Oxytocin Receptor
|
Neurological Disease
|
|
WAY-267464 hydrochloride is a non-peptide oxytocin receptor (OTR) agonist. WAY-267464 hydrochloride can impair social recognition memory in rats through a vasopressin 1A receptor antagonist action. WAY-267464 hydrochloride can be used for the research of psychiatric disorders, such disorders include autism spectrum disorder, schizophrenia, and social anxiety disorder .
|
-
- HY-158183
-
|
|
Chloride Channel
|
Others
|
|
NMD670 is an orally active partial inhibitor of the skeletal muscle-specific chloride channel ClC-1. NMD670 increases muscle excitability in response to movement commands, enhances neuromuscular transmission, restores muscle function and improves muscle mobility. NMD670 has a favorable safety profile and improves muscle function in rats in a MG rat model .
|
-
- HY-163853
-
|
|
GLUT
Akt
|
Metabolic Disease
|
|
Antidiabetic agent 6 (Compound 19) is an antidiabetic Agent. Antidiabetic agent 6 stimulates GLUT4 translocation by activation of the PI3K/AKT-dependent signaling pathway. Antidiabetic agent 6 reduces blood glucose levels in Streptozotocin (HY-13753)-induced diabetic rats .
|
-
- HY-120454
-
|
|
MEK
Potassium Channel
|
Cancer
|
|
G-479 is the inhibitor for MEK and hERG channel (IC50=14 μM). G-479 inhibits the proliferation of HCT-116 and A375 with IC50 of 0.049 μM and 0.004 μM. G-479 exhibits good metabolic stability in liver microsomes and good pharmacokinetic characteristics in rats .
|
-
- HY-117119
-
|
|
5-HT Receptor
|
Metabolic Disease
|
|
VER-3323 is an oral active 5-HT2C agonist and belongs to the class of indoline analogs. VER-3323 reduces food intake in rats by inducing swallowing dysfunction, with no significant impact on energy expenditure generated through thermogenesis or exercise. VER-3323 can be utilized in obesity research .
|
-
- HY-13738R
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene (Standard) is the analytical standard of Raloxifene. This product is intended for research and analytical applications. Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
|
-
- HY-111136
-
|
|
GABA Receptor
5-HT Receptor
Dopamine Receptor
Histamine Receptor
|
Neurological Disease
|
|
BL-1020 mesylate is the mesylate salt form of BL-1020. BL-1020 mesylate is an antipsychotic agent. BL-1020 mesylate is inhibitor for dopamine receptor and serotonin receptor (5-HT receptor), with Ki of 0.066, 0.062 and 0.21 nM, for D2L, D2S and 5-HT2A receptors, respectively. BL-1020 mesylate is agonist for GABAA receptor with Ki of 3.74 μM, and enhances the GABA release. BL-1020 mesylate exhibits high affinity with histamine receptor (Ki is 0.47 nM). BL-1020 mesylate reduces Amphetamine-induced hyperactivity, with lower catalepsy and sedation. BL-1020 mesylate is blood-brain barrier penetrate .
|
-
- HY-N6952
-
-
- HY-Y1362
-
|
|
Autophagy
Apoptosis
Pyroptosis
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Ethyl pyruvate is a simple derivative of the endogenous metabolite pyruvate. Ethyl pyruvate is an HMGB1 release inhibitor. Ethyl pyruvate can induce apoptosis by autophagy. Ethyl pyruvate has anti-inflammatory, antioxidant and anti-tumor activity. Ethyl pyruvate can be used in the study of neurodegenerative diseases such as Alzheimer's and Parkinson's disease .
|
-
- HY-13738
-
|
Keoxifene; LY156758 free base; LY139481
|
Estrogen Receptor/ERR
|
Cancer
|
|
Raloxifene (Keoxifene) is a benzothiophene-derived selective estrogen receptor modulator (SERM). Raloxifene has estrogen-agonistic effects on bone and lipids and estrogen-antagonistic effects on the breast and uterus. Raloxifene is used for breast cancer and osteoporosis research .
|
-
- HY-19687
-
|
CP73850
|
Aldose Reductase
|
Metabolic Disease
|
|
Zopolrestat (CP73850) is a potent, orally active aldose reductase (AR) inhibitor with an IC50 of 3.1 nM. Zopolrestat is used for the research of diabetic complications .
|
-
- HY-101043
-
|
|
Sigma Receptor
iGluR
|
Neurological Disease
|
|
4-PPBP maleate is a potent σ 1 receptor ligand and agonist. 4-PPBP maleate is a non-competitive, selective NR1a/2B NMDA receptors (expressed in Xenopus oocytes) antagonist. 4-PPBP maleate provides neuroprotection .
|
-
- HY-106093
-
|
|
COX
|
Inflammation/Immunology
|
|
Eltenac, a non-steroidal anti-inflammatory drug (NSAID), is a COX inhibitor. Eltenac shows IC50 of 0.03 μM for both COX-1 and COX-2 in isolated human whole blood .
|
-
- HY-115864
-
|
TAK-653; NBI-1065845
|
iGluR
Lipoxygenase
|
Neurological Disease
|
|
Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca 2+ influx in hGluA1i CHO cells (EC50 = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders .
|
-
- HY-108656
-
|
|
P2Y Receptor
Arrestin
|
Cardiovascular Disease
|
|
MRS2365 is a potent and selective P2Y1 receptor (EC50=0.4 nM) /[ 35S]GTPγS binding/β-arrestin 2 recruitment agonist with an EC50 of 0.4 nM. MRS2365 relieves mechanical allodynia and increases mechanical sensitivity. MRS2365 shows little agonist or antagonist activity at the P2Y12 or P2Y13 receptors .
|
-
- HY-145906
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
D4R antagonist-2 is a potent and selective D4R antagonist with an IC50 of 6.52 µM. D4R antagonist-2 displays very favorable in vitro PK parameters and has good brain penetration. D4R antagonist-2 has the potential for the research of Parkinson’s disease .
|
-
- HY-107751
-
-
- HY-150550
-
|
|
COX
|
Inflammation/Immunology
|
|
COX-2-IN-26 is a potent, selective and orally active COX-2 inhibitor with IC50 values of 10.61, 0.067, 1.96 µM for COX-1, COX-2, 15-LOX, respectively. COX-2-IN-26 shows anti-inflammatory activity. COX-2-IN-26 shows gastrointestinal safety profile .
|
-
- HY-108656A
-
|
|
P2Y Receptor
Arrestin
|
Cardiovascular Disease
|
|
MRS2365 trisodium is a potent and selective P2Y1 receptor (EC50=0.4 nM)/[ 35S]GTPγS binding/β-arrestin 2 recruitment agonist. MRS2365 trisodium relieves mechanical allodynia and increases mechanical sensitivity .
|
-
- HY-W012977
-
-
- HY-12718A
-
|
|
Adrenergic Receptor
|
Endocrinology
|
|
(±)-WB 4101 is a potent antagonist of noradrenaline. (±)-WB 4101 interacts with protein in smooth muscle. (±)-WB 4101 makes drug and receptor bind tightly .
|
-
- HY-110221
-
|
|
PKG
|
Neurological Disease
|
|
Rp-8-pCPT-cGMPS sodium is the sodium salt form of Rp-8-pCPT-cGMPS. Rp-8-pCPT-cGMPS is an inhibitor for cGMP-dependent protein kinase (cGK). Rp-8-pCPT-cGMPS sodium is an agonist for cyclic nucleotide-gated (CNG) channels in a voltage-dependent manner .
|
-
- HY-158160
-
|
|
Sodium Channel
|
Metabolic Disease
|
|
LBA-3 is a selective, orally active inhibitor for sodium-coupled citrate transporter SLC13A5, with an IC50 of 67 nM. LBA-3 decreases levels of triglyceride and total cholesterol in oleic and palmitic acid (OPA)-stimulated AML12 cells, PCN-stimulated primary mouse hepatocytes and in mouse models, without detectable toxicity. LBA-3 is blood-brain barrier permeable .
|
-
- HY-162438
-
|
|
HIF/HIF Prolyl-Hydroxylase
|
Metabolic Disease
|
|
PHD2-IN-2 (Compound 12) is a PHD2 inhibitor, with an IC50 of 34.3 nM. PHD2-IN-2 has high erythropoietin (EPO) inducing activity, with an EC50 of 6.79 μM. PHD2-IN-2 can be used for the research of anemia, ischemia, and hypoxia .
|
-
- HY-129246
-
|
|
DNA/RNA Synthesis
|
Cancer
|
|
Cytembena is inhibitor for replicative DNA synthesis, purine synthesis and tetrahydrofolate formylase activity. Cytembena ameliorates ovarian or breast cancer, relieves the pain from skeletal metastases .
|
-
- HY-P10318
-
|
|
GLP Receptor
|
Endocrinology
|
|
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
|
-
- HY-Y1362R
-
|
|
Autophagy
Apoptosis
Pyroptosis
NF-κB
|
Inflammation/Immunology
Cancer
|
|
Ethyl pyruvate (Standard) is the analytical standard of Ethyl pyruvate. This product is intended for research and analytical applications. Ethyl pyruvate is a simple derivative of the endogenous metabolite pyruvate. Ethyl pyruvate is an HMGB1 release inhibitor. Ethyl pyruvate can induce apoptosis by autophagy. Ethyl pyruvate has anti-inflammatory, antioxidant and anti-tumor activity. Ethyl pyruvate can be used in the study of neurodegenerative diseases such as Alzheimer's and Parkinson's disease .
|
-
- HY-113958
-
|
LM-2219
|
Others
|
Others
|
|
Difethialone (LM-2219) is an anticoagulant rodenticide. Difethialone shows high rodenticide activity in warfarin-sensitive and resistant strains of rats and mice. Difethialone interferes with the circulation of vitamin K in the liver, preventing the synthesis of coagulation factors, resulting in the inability of the blood to coagulate properly, ultimately causing internal bleeding and death. Difethialone can be used in studies of ecological impacts .
|
-
- HY-13340
-
|
VU152100
|
mAChR
|
Neurological Disease
|
|
VU0152100 (VU152100) is a highly selective mAChR positive allosteric modulator (permeable to the blood-brain barrier). VU0152100 reverses Amphetamine-induced hypermotility in rats and increased levels of extracellular dopamine in nucleus accumbens and caudate-putamen. VU0152100 has good research potential in psychosis and cognitive impairment associated with mental disorders such as schizophrenia .
|
-
- HY-116175
-
|
|
Others
|
Metabolic Disease
|
|
BIBB 515 is a potent, selective and orally active 2,3-oxidosqualene cyclase (OSC) inhibitor with ED50 values of 0.2-0.5 mg/kg and 0.36-33.3 mg/kg in rats and mice (1-5 hours), respectively. BIBB 515 exerts lipid-lowering effect mainly by inhibiting the production of low-density lipoprotein (LDL) .
|
-
- HY-19801
-
|
|
Aldehyde Dehydrogenase (ALDH)
|
Neurological Disease
|
|
CVT-10216 is a highly selective, reversible aldehyde dehydrogenase-2 (ALDH-2) inhibitor with an IC50 of 29 nM. CVT-10216 also has inhibitory effect of ALDH-1 with an IC50 of 1.3 μM. CVT-10216 can reduce excessive alcohol drinking in alcohol-preferring rats and exhibit anxiolytic effects .
|
-
- HY-W008574
-
|
|
PROTAC Linkers
|
Inflammation/Immunology
Cancer
|
|
TGN-020 is a selective Aquaporin 4 (AQP4) inhibitor with an IC50 of 3.1 μM . TGN-020 is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs .TGN-020 alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats .
|
-
- HY-P1131
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
M617 is a selective galanin receptor 1 (GAL1) agonist, with Kis of 0.23 and 5.71 nM for GAL1 and GAL2, respectively. M617, acting through its central GAL1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats .
|
-
- HY-105084
-
|
|
Others
|
Neurological Disease
|
|
Lubeluzole is a neuroprotective anti-ischemic compound. Lubeluzole, but not its (-)-R-isomer, protects against sensorimotor deficits provoked by photochemical stroke in rats. Lubeluzole inhibited glutamate-stimulated guanosine 3',5'-cyclic monophosphate production with an IC50 of 37 nM. Lubeluzole also has the potential for developing a novel class of antibacterial adjuvants endowed with spasmolytic activity .
|
-
- HY-101369
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
BW-723C86 is a potent and a selective 5-HT2B receptor agonist. BW-723C86 exhibits anxiolytic-like actions. BW-723C86 also causes hyperphagia and reduced grooming in rats .
|
-
- HY-115914
-
|
|
Others
|
Others
|
|
Lipid-lowering agent-1 is a potent lipid-lowering agent. Lipid-lowering agent-1 has significant pharmacological effects on the inhibition of low-density lipoprotein cholesterol (LDLC) and promotion of high-density lipoprotein cholesterol (HDLC) production. Lipid-lowering agent-1 shows potent hypolipidemic effect in high-fat diet rats .
|
-
- HY-A0039
-
|
UK-116044
|
5-HT Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine .
|
-
- HY-100446
-
|
|
Glutaminase
Apoptosis
|
Metabolic Disease
Inflammation/Immunology
|
|
NTU281 is a potent transglutaminase-2 inhibitor. NTU281 can reduce the increases in serum creatinine and albuminuria in diabetic rats. NTU281 can also reduce glomerular collagen I accumulation, Hic-5 and α-SMA expression, and apoptosis. NTU281 can be used for researching glomerulosclerosis caused by diabetes .
|
-
- HY-147384
-
|
|
Calcium Channel
|
Cardiovascular Disease
|
|
CXL-1020 is a hydroxylamine-based nitroxyl (HNO) donor. CXL-1020 improves cardiac inotropy/lusitropy and Ca 2+ cycling in rats with abnormal relaxation. CXL-1020 induces vasorelaxation and improves cardiac function in canine models. CXL-1020 has been used to research systolic heart failure and stable heart failure .
|
-
- HY-P3676
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide Y (3-36) (porcine) is an agonist of neuropeptide Y (NPY) receptor subtype Y2, and stimulates feeding in rats. Neuropeptide Y (3-36) (porcine) is a highly Y2 selective ligand compared with nselective Y1/Y2 receptor ligand, Neuropeptide Y 1-36 .
|
-
- HY-W008574A
-
|
|
PROTAC Linkers
|
Inflammation/Immunology
Cancer
|
|
TGN-020 sodium is a selective Aquaporin 4 (AQP4) inhibitor with an IC50 of 3.1 μM . TGN-020 sodium is an alkyl chain-based PROTAC linker that can be used in the synthesis of PROTACs . TGN-020 sodium alleviates edema and inhibits glial scar formation after spinal cord compression injury in rats .
|
-
- HY-148530
-
|
|
PROTACs
CDK
|
Cancer
|
|
YX-2-107 is a PROTAC (IC50= 4.4 nM) that selectively degrades CDK6. YX-2-107 effectively inhibits RB phosphorylation and FOXM1 expression in vitro and inhibits the development of Ph + ALL in rats. YX-2-107 can be used in the study of Ph chromosome-positive (Ph +) acute lymphoblastic leukemia (ALL) .
|
-
- HY-N0157C
-
|
6-Carboxyuracil potassium; Vitamin B13 potassium
|
Endogenous Metabolite
DNA/RNA Synthesis
|
Metabolic Disease
|
|
Orotic acid potassium (Vitamin B13 potassium) is a precursor of pyrimidine bases and is involved in the synthesis of DNA and RNA. Orotic acid potassium stimulates the growth of animals, plants and microorganisms, participates in carbohydrate metabolism, and is necessary for the growth and life activities of organisms. Orotic acid potassium is a measurement indicator in routine newborn screening for urea cycle abnormalities. Orotic acid potassium can cause hepatic steatosis and hepatomegaly in rats .
|
-
- HY-107518
-
|
(R,S)-3,4-DCPG
|
iGluR
|
Neurological Disease
|
|
(R,S)-3,4-Dicarboxyphenylglycine ((RS)-3,4-DCPG) is an AMPA receptor antagonist. (R,S)-3,4-Dicarboxyphenylglycine antagonizes AMPA-mediated depolarization of motor neurons in neonatal rats. (R,S)-3,4-Dicarboxyphenylglycine can be used in the study of neurological diseases .
|
-
- HY-W061043
-
|
|
Serotonin Transporter
Dopamine Transporter
|
Neurological Disease
|
|
DOV-216,303 is an antidepressant compound. DOV-216,303 inhibits the reuptake of norepinephrine (NE), serotonin (5‐HT), and dopamine (DA), with IC50 values of 14 nM, 20 nM and 78 nM for hSERT, hNET and hDAT, respectively. DOV-216,303 increases monoamine release in the prefrontal cortex of olfactory bulbectomized (OBX) rats .
|
-
- HY-W013989R
-
|
|
Epoxide Hydrolase
|
Cardiovascular Disease
|
|
1,3-Dicyclohexylurea (Standard) is the analytical standard of 1,3-Dicyclohexylurea. This product is intended for research and analytical applications. 1,3-Dicyclohexylurea (DCU) is an orally active and potent sEH (soluble epoxide hydrolase) inhibitor. Oral Delivery of 1,3-Dicyclohexylurea nanosuspension enhances exposure and lowers blood pressure in hypertensive Rats .
|
-
- HY-160864
-
|
HWA 448
|
Phosphodiesterase (PDE)
|
Cancer
|
|
Torbafylline is a PDE inhibitor. Torbafylline mitigates protein breakdown in rat skeletal muscle following burns by activating the PDE4/cAMP/EPAC/PI3K/Akt signaling pathway. Torbafylline suppresses the increased ubiquitin-proteasome-dependent protein degradation observed in the skeletal muscles of rats susceptible to cancer and sepsis .
|
-
- HY-W012946R
-
|
|
ATP Citrate Lyase
Acyltransferase
Endogenous Metabolite
|
Metabolic Disease
|
|
2-Furoic acid (Standard) is the analytical standard of 2-Furoic acid. This product is intended for research and analytical applications. 2-Furoic acid (Furan-2-carboxylic acid) is an organic compound produced through furfural oxidation . 2-Furoic acid exhibits hypolipidemic effet, lowers both serum cholesterol and serum triglyceride levels in rats .
|
-
- HY-14977
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
CS-0777-P, the phosphorylated form of CS-0777, acts as a potent and selective modulator of the S1P receptor-1 (S1P1). It exhibits approximately 320-fold higher agonist activity for human S1P1 compared to S1P3, with an EC50 of 1.1 nM. In pharmacological studies, CS-0777-P demonstrated significant effects in vitro as an S1P1 and S1P3 agonist, leading to lowered peripheral blood lymphocyte counts and suppressive effects on experimental autoimmune encephalomyelitis (EAE) in rats. Pharmacokinetic studies in rats revealed rapid lymphocyte count reductions following oral administration, making CS-0777 a promising candidate currently undergoing clinical trials for the treatment of multiple sclerosis (MS) .
|
-
- HY-143330
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
MAO-B-IN-4 (Compound 26) is an orally active and reversible MAO-B inhibitor with an IC50 of 9 nM. MAO-B-IN-4 has good metabolic stability, safety profile and brain permeability. MAO-B-IN-4 shows antidepressant activity in rats and mice. MAO-B-IN-4 can be used in studies related to Alzheimer's disease .
|
-
- HY-121624
-
|
|
Glutathione S-transferase
|
Infection
|
|
Anthglutin is a gamma-glutamyltransferase inhibitor isolated from Penicillium oxalicum cultures. The Ki values ??of Anthglutin for different enzymes are: porcine kidney enzyme 5.7 μM, human kidney enzyme 18.3 μM, human liver soluble enzyme 13.6 μM, and conjugated enzyme 10.2 μM. Anthglutin had no significant effect on intestinal absorption of methionine in rats .
|
-
- HY-118374
-
|
|
PI3K
Akt
|
Inflammation/Immunology
|
|
AM-9635 is a selective PI3Kδ inhibitor with oral bioavailability, good in vitro and in vivo activity and pharmacodynamic properties. AM-9635 inhibits PI3Kδ-dependent B cell receptor-mediated AKT phosphorylation and suppresses the production of specific IgG and IgM antibodies in rats immunized with Aplysia leocyanin (KLH).
|
-
- HY-145476
-
|
N-NAT; N'-Nitrosoanatabine
|
Others
|
Cancer
|
|
(R,S)-N-Nitrosoanatabine (N-NAT) is a tobacco-specific nitrosamine (TSNA) that has been found in tobacco, tobacco products, and electronic cigarettes. The (S) enantiomer comprises approximately 80% of the N-NAT found in commercial and research cigarettes and smokeless tobacco.3 Unlike other TSNAs, N-NAT is not carcinogenic in rats when administered at doses of 1, 3, and 9 mmol/kg.
|
-
- HY-76569
-
|
PNU-200577; 5-Hydroxymethyl Tolterodine
|
mAChR
|
Neurological Disease
|
|
Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-12461
-
-
- HY-124754
-
|
BTRX-335140; CYM-53093
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
|
|
Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC50 values of 0.8 nM, 110 nM, and 6500 nM, respectively.
Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy .
|
-
- HY-P1131A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
M617 TFA is a selective galanin receptor 1 (GAL1) agonist, with Kis of 0.23 and 5.71 nM for GAL1 and GAL2, respectively. M617 TFA, acting through its central GAL1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats .
|
-
- HY-P1216
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats .
|
-
- HY-111615A
-
|
|
Somatostatin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
|
-
- HY-W027951
-
|
DMTU
|
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
N,N'-Dimethylthiourea (DMTU), isolated from Allium sativum, is an orally active scavenger of hydroxyl radical (•OH) and blocks •OH production by activated neutrophils in vitro. N,N'-Dimethylthiourea protects against water-immersion restraint stress (WIRS)-induced gastric mucosal lesions in rats by exerting its antioxidant action including •OH scavenging and anti-inflammatory action .
|
-
- HY-110125
-
|
CID 1261822
|
GPR55
|
Neurological Disease
|
|
ML-193 (CID 1261822) is a potent and selective antagonist of GPR55, with an IC50 of 221 nM. ML-193 shows more than 27-fold selectivity for GPR55 over GPR35, CB1 and CB2. ML-193 can improve the motor and the sensorimotor deficits of Parkinson’s disease (PD) rats .
|
-
- HY-101422A
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
GAL-021 sulfate is a potent BKCa-channel blocker. GAL-021 sulfate inhibits KCa1.1 in GH3 cells. GAL-021 sulfate is a novel breathing control modulator that is based on selective modification of the almitrine pharmacophore. GAL-021 sulfate increases minute ventilation in rats and non-human primates .
|
-
- HY-P1368
-
|
Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)
|
CRFR
|
Endocrinology
|
|
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) is a potent CRF1 receptor-selective agonist with a Ki of 1.7 nM. Stressin I induces increases in adrenocorticotropic hormone (ACTH) levels in rats .
|
-
- HY-P990093
-
|
CM310
|
Interleukin Related
|
Inflammation/Immunology
|
|
Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats .
|
-
- HY-105034
-
|
BMY 13859-1 free base
|
5-HT Receptor
|
Neurological Disease
|
|
Tiospirone is a 5-HT2 receptor antagonist with affinity for D2, 5-HT1a, and 5-HT7, and sigma receptors. Tiospirone decreases consumption of ethanol while increasing food intake of rats. Tiospirone can also reduce the reinforcing properties of Cocaine exhibited in the conditioned place preference paradigm .
|
-
- HY-135216
-
|
|
Src
VEGFR
Raf
EGFR
|
Cancer
|
|
Antiproliferative agent-54 (Compound 6z) is the inhibitor for multiple kinases, such as ABL WT, B-RAF, EGFR, HCK, LYN A and SRC with IC50 of 6-50 nM. Antiproliferative agent-54 inhibits proliferation of several cancer cell, inhibits HUVEC and HepG2, with EC50 of 34 and 38 nM. Antiproliferative agent-54 exhibits good pharmacokinetic characteristics in rats .
|
-
- HY-163924
-
|
|
Apoptosis
|
Cancer
|
|
Apoptosis inducer 25 (Compound 4H) inhibits the proliferation of cell BGC-823 with IC50 of 0.37 μM. Apoptosis inducer 25 arrests cell cycle at G2/M phase, induces apoptosis in cell BGC-823, and causes mitochondrial dysfunction. Apoptosis inducer 25 exhibits good pharmacokinetic properties in rats .
|
-
- HY-N13208
-
|
|
MMP
TGF-beta/Smad
|
Others
|
Stevia Powder is a natural sweetener with antioxidant activity. Stevia Powder can downregulate pro fibrotic pathways in cirrhotic rats, including reduced hepatic myofibroblasts and decreased expression of matrix metalloproteinases MMP2 and MMP13, upregulate anti fibrotic molecule Smad7, prevent serum necrosis and elevated bile stasis markers, thereby inhibiting the development of liver fibrosis .
|
-
- HY-163998
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
TLR4-IN-1 (compound 3k) inhibits the cell viability of RAW264.7 with an IC50 of 1.02 μM. TLR4-IN-1 inhibits the release of cytokine TNF-α, IL-1β and IL-6, and exhibits anti-inflammatory efficacy in rats rheumatoid arthritis models .
|
-
- HY-111073
-
|
Y101
|
HBV
|
Infection
Inflammation/Immunology
|
|
Bentysrepinine (Y101) is an orally active HBV inhibitor with anti-hepatitis B virus infection activity. Bentysrepinine exhibits favorable pharmacokinetic characteristics, with absolute bioavailability of 44.9%, 43.1%, and 19.2% in rats, dogs, and monkeys, respectively, and it does not accumulate in monkeys after 90 days of oral administration. Bentysrepinine is under research in the antiviral and hepatitis fields .
|
-
- HY-16290
-
|
ZK 230211; BAY86 5044
|
Progesterone Receptor
|
Endocrinology
|
|
Lonaprisan (ZK 230211; BAY86 5044) is an antagonist for progesterone receptor, with IC50 of 3.6 pM and 2.5 pM for PR-A and PR-B, respectively. Lonaprisan exhibits antiprogestagenic activity in rabbits, interrupts early pregnancy in rats, and exhibits antitumor efficacy against DMBA (HY-W011845)-induced mammary tumor. Lonaprisan reveals antiglucocorticoid and antiandrogenic effect .
|
-
- HY-B0377G
-
|
MK-208 (GMP)
|
Histamine Receptor
|
Inflammation/Immunology
Cancer
|
|
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine GMP is a competitive histamine H2-receptor antagonist, inhibits gastric secretion, activates the gastric mucosal defensive mechanisms. Famotidine GMP ameliorates peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD) in rats model .
|
-
- HY-118350
-
|
|
Others
|
Neurological Disease
|
|
FR 75513 is a 1,1'-biphenyl-2,6-dicarboxylic acid diester series compound that can inhibit the contraction of the detrusor muscle of guinea pig bladder (IC50=3.3 μg/mL). After intravenous injection of FR 75513 into anesthetized rats, it also showed strong inhibitory activity on the detrusor contraction (ID50=0.04 mg/kg).
|
-
- HY-32351B
-
|
3-epi-25-hydroxy Cholecalciferol
|
PTHR
|
Endocrinology
|
|
3-epi-25-hydroxy Vitamin D3 is the C-3 epimer of 25-hydroxy vitamin D3.1 Dietary administration of 3-epi-25-hydroxy vitamin D3 (0.5 and 1 IU/g) decreases levels of serum parathyroid hormone (PTH) in male, but not female, weanling rats.
|
-
- HY-162525
-
|
|
HIV Protease
|
Infection
|
|
GS-9770 is an orally active inhibitor for HIV protease with Ki of 0.16 nM. GS-9770 exhibits antiviral activity aginst HIV-1 strains and HIV-2 strains with EC50 of 1.9-26 nM, and 26 nM. GS-9770 is metabolic stable in human liver microsomes. GS-9770 exhibits good pharmacokinetic characters in Sprague Dawley rats .
|
-
- HY-124191
-
|
PPI-668 hydrochloride
|
HCV
|
Infection
|
|
Ravidasvir hydrochloride (PPI-668 hydrochloride) is a pan-genotypic inhibitor for hepatitis C virus (HCV) NS5A protein. Ravidasvir hydrochloride inhibits the replication of HCV, with EC50 of 0.12, 0.01 and 1.14 nM, for HCV gt-1a, gt-1b, and gt-3a replicons, respectively. Ravidasvir hydrochloride exhibits good pharmacokinetic characters in rats .
|
-
- HY-146421
-
|
|
NO Synthase
NF-κB
Reactive Oxygen Species
|
Inflammation/Immunology
|
|
Anti-inflammatory agent 21 (compound 9o) is an orally active and low cytotoxic anti-inflammatory agent, with an IC50 value of 0.76 μM for NO. Anti-inflammatory agent 21 acts via accumulation ROS and blocks the NF-κB/MAPK signaling pathway. Anti-inflammatory agent 21 can ameliorate cartilage destruction and inflammatory cell infiltration in arthritis rats model .
|
-
- HY-18100A
-
|
|
Sigma Receptor
Akt
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway .
|
-
- HY-137231B
-
|
|
nAChR
|
Neurological Disease
|
|
(S)-UFR2709 (hydrochloride) is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 (hydrochloride) decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 (hydrochloride) acts as an anxiolytic agent and can be used for the study of nicotine addiction .
|
-
- HY-137231A
-
|
|
nAChR
|
Neurological Disease
|
|
(S)-UFR2709 is a competitive nAChR antagonist and displays higher affinity for α4β2 nAChRs than for α7 nAChRs. (S)-UFR2709 decreases anxiety and reduces ethanol consumption and ethanol preference in alcohol-preferring rats. (S)-UFR2709 acts as an anxiolytic agent and can be used for the study of nicotine addiction .
|
-
- HY-116807
-
|
DHLA
|
Reactive Oxygen Species
|
Neurological Disease
Inflammation/Immunology
|
|
Dihydrolipoic Acid (DHLA) is an excellent antioxidant capable of scavenging almost any oxygen-centered radical . Dihydrolipoic acid exhibits anti-inflammatory properties in various diseases. Dihydrolipoic Acid exerts a preventive effect via ERK/Nrf2/HO-1/ROS/NLRP3 pathway in LPS-induced sickness behavior rats. Dihydrolipoic Acid can be used for the reaserch of depression .
|
-
- HY-108493
-
|
|
LPL Receptor
|
Inflammation/Immunology
|
|
CS-2100 (Compound 10b) is a potent, selective, orally active and S1P3-sparing S1P1 agonist with an EC50 of 4.0 nM for human S1P1. CS-2100 shows in vivo immunosuppressive efficacy in rats with an ID50 (infective dose) of 0.407 mg/kg for HvGR .
|
-
- HY-15008
-
|
|
Oxytocin Receptor
|
Endocrinology
|
|
L-368,899 is an orally active and selective OT (oxytocin ) receptor antagonist, with IC50s of 8.9 and 26 nM for uterus of rat and human, respectively. L-368,899 can cross the blood-brain barrier (BBB). L-368,899 inhibits oxytocin-stimulated uterine contractions in rats and can be used in study of preterm labor .
|
-
- HY-P3567
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
(p-Iodo-Phe7)-ACTH (4-10) is a adrenocorticotrophic hormone (ACTH) derivative, which is produced and secreted by the anterior pituitary gland. (p-Iodo-Phe7)-ACTH (4-10) serves as a melanocortin (MC) receptor antagonist and inhibits α-melanocyte-stimulating hormone (α-MSH)-induced excessive grooming behavior in rats .
|
-
- HY-W152604
-
|
Cyclo(leu-gly)
|
Dopamine Receptor
|
Neurological Disease
|
|
Cyclo(glycyl-L-leucyl) (Cyclo(leu-gly)), a neuropeptide, down-regulates dopamine (DA) receptors and attenuates dopaminergic supersensitivity. Cyclo(glycyl-L-leucyl) inhibits the development of Morphine induced pain relief as well as dopamine receptor supersensitivity in rats. Cyclo(glycyl-L-leucyl) has the potential for the prevention of tardive and/or L-DOPA (HY-N0304)-induced dyskinesias .
|
-
- HY-18100
-
|
|
Sigma Receptor
Akt
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
PRE-084 is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway .
|
-
- HY-P1368A
-
|
Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41) TFA
|
CRFR
|
Endocrinology
|
|
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) TFA is a potent CRF1 receptor selective agonist, Ki is 1.7 nM. Stressin I induces an increase in adrenocorticotropic hormone (ACTH) levels in rats .
|
-
- HY-120355
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
AP14145 is an inhibitor for small conductance calcium-activated potassium channel, inhibits KCa2.2 channel and KCa channel with IC50 of 1.1 μM and 1.1 μM. AP14145 prolongs atrial effective refractory period (AERP) in rats, causes the conversion of atrial fibrillation to sinus rhythum in porcine left ventricular dysfunction models, and exhibits antiarrhythmic effect .
|
-
- HY-B1869R
-
|
|
Others
|
Others
|
|
Metsulfuron-methyl (Standard) is the analytical standard of Metsulfuron-methyl. This product is intended for research and analytical applications. Metsulfuron-methyl is a systemic sulfonylurea herbicide that has been widely used to control broadleaf weeds and annual grasses in rice, corn, wheat, and barley. Metsulfuron-methyl exhibits high herbicidal activity and low mammalian toxicity, with an LD50 for rats exceeding 5000 mg/kg .
|
-
- HY-N0495R
-
|
|
Beta-secretase
|
Neurological Disease
|
|
Aloenin (Standard) is the analytical standard of Aloenin. This product is intended for research and analytical applications. Aloenin (Aloenin A) is a kind of natural product, has effective clearing and free radical activity, and has moderate inhibitory activity on β-secretion (BACE) (IC50=14.95 μg/mL). Aloenin suppresses peritoneal hypertrophy in large rats and suppresses its release .
|
-
- HY-117712
-
|
|
Others
|
Cardiovascular Disease
|
|
LG 6-101 is an orally active and new antiarrhythmic agent. LG 6-101 shows strong antiarrhythmic effects in a coronary-artery-ligation model of rats, better than Propafenone (HY-B0432). LG 6-101 also delays the occurence of ventricular premature beat (VPB)'s and has protective effects against cardiac arrest caused by infusion of aconitine .
|
-
- HY-105110
-
|
SM-8668
|
Fungal
|
Infection
|
|
SM-8668 is an effective orally active antifungal agent, with median effective doses (ED50) of 0.18, 3.7, and 5.9 mg/kg for systemic candidiasis, aspergillosis, and cryptococcosis in mice, respectively. Pharmacokinetic studies in mice and rats indicate that SM-8668 has a long half-life and a high total exposure. SM-8668 can be used in anti-infective research .
|
-
- HY-154979
-
|
|
Others
|
Inflammation/Immunology
|
|
Anti-hepatic fibrosis agent 2 (Compound 6k) is an orally active COL1A1 inhibitor. Anti-hepatic fibrosis agent 2 is an anti-fibrogenic agent targeting ewing sarcoma breakpoint region 1 (EWSR1) .
|
-
- HY-162513
-
|
|
Dipeptidyl Peptidase
|
Cardiovascular Disease
|
|
DPP-4-IN-10 (compound 1) is a DPP-4 inhibitor. DPP-4-IN-10 is orally active. DPP-4-IN-10 blocks the degradation of GLP-1 and GIP, which may improve glycemic control in type 2 diabetes (T2MD) .
|
-
- HY-116881
-
|
|
mAChR
|
Neurological Disease
|
|
SCH 57790 is a selective antegonist for muscarinic M2 receptor, which increases acetylcholine release, and thus improves cognitive performance. SCH 57790 reverses Scopolamine (HY-N0296)-induced memory deficits in mice, without significant toxicity (100 mg/kg).
|
-
- HY-15591
-
|
|
HCV
|
Infection
|
|
TMC647055 is a potent nonnucleoside NS5B polymerase inhibitor of HCV replication. TMC647055 has potent HCV combine activity with an IC50 value of 82 nM. TMC647055 can be used for the research of Hepatitis C virus (HCV) .
|
-
- HY-B0226
-
|
Nitrofural
|
Bacterial
Antibiotic
|
Infection
|
|
Nitrofurazone (Nitrofural) is a broad spectrum antibiotic that has oral activity. Nitrofurazone is a nitro-aromatic drug. Nitrofurazone is active against both Gram-positive and Gram-negative bacteria .
|
-
- HY-15707
-
NS6180
1 Publications Verification
|
Potassium Channel
|
Inflammation/Immunology
|
|
NS6180 is a new orally active KCa3.1 channel inhibitor. NS6180 inhibits cloned human KCa3.1 channels with an IC50value of 9 nM. NS6180 can be used for the research of inflammatory bowel disease (IBD) .
|
-
- HY-15591A
-
|
|
HCV
|
Infection
|
|
TMC647055 (Choline salt) is a potent nonnucleoside NS5B polymerase inhibitor of HCV replication. TMC647055 Choline salt has potent HCV combine activity with an IC50 value of 82 nM. TMC647055 Choline salt can be used for the research of Hepatitis C virus (HCV) .
|
-
- HY-100454
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
CGP 25454A is a selective presynaptic dopamine autoreceptor antagonist which induces the increase of dopamine and acetyl choline. CGP 25454A can be used for major depression research .
|
-
- HY-125588
-
|
Chromium (III) picolinate; Cr(Pic)3
|
Apoptosis
p38 MAPK
|
Metabolic Disease
|
|
Chromium picolinate (Chromium (III) picolinate) is a compound that has oral activity. Chromium picolinate induces apoptosis. Chromium picolinate is the activator of p38 MAPK. Chromium picolinate has antioxidant activity. Chromium picolinate can be used in research on type 2 diabetes .
|
-
- HY-106968
-
|
|
iGluR
|
Neurological Disease
|
|
ZD-9379 is a potent, orally active, and brain penetrant full antagonist at the glycine site of the NMDA receptor. ZD-9379 has neuroprotective effect .
|
-
- HY-116228
-
|
Caderofloxacin; CS-940
|
Bacterial
|
Infection
|
|
Cadrofloxacin (Caderofloxacin; CS-940), a orally active fluoroquinolone, is effective against aerobic/anaerobic Gram-positive and Gram-negative bacteria. Cadrofloxacin can be used for the research of infectious diseases .
|
-
- HY-115913
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE4-IN-6 is a potent, safe and moderately selective PDE4 inhibitor with IC50s of 0.125 and 0.43 µM for PDE4B and PDE4D, respectively. PDE4-IN-6 can downregulate the expression level of TNF-α and IL-6. PDE4-IN-6 has potent immunomodulatory activity thereby its potential against rheumatoid arthritis. Anti-inflammatory and anti-arthritic effects .
|
-
- HY-100554
-
|
|
Adrenergic Receptor
5-HT Receptor
|
Cardiovascular Disease
|
|
BMY 7378 is a selective antagonist of α1D-adrenoceptor (α1D-AR). BMY 7378 binds to membranes expressing the cloned rat α1D-AR with a >100-fold higher affinity (Ki=2 nM) than binding to either the cloned rat α1A-AR (Ki=800 nM) or the hamster α1B-AR (Ki=600 nM). BMY 7378 is a 5-HT1A receptor partial agonist .
|
-
- HY-17610
-
|
TS-091
|
Histamine Receptor
|
Neurological Disease
|
|
Enerisant is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
|
-
- HY-17610A
-
|
TS-091 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
|
-
- HY-105266
-
-
- HY-128142
-
|
|
PKD
PKC
|
Cardiovascular Disease
|
|
PKC/PKD-IN-1 (Compound 13C) is an orally active dual protein kinase C/D (PKC/PKD) inhibitor with an IC50 value of 0.6 nM for PKD1. PKC/PKD-IN-1 can attenuate high-salt diet-induced cardiac hypertrophy and can be used in the study of heart failure .
|
-
- HY-163505
-
|
|
Bacterial
|
Others
|
|
Anti-MRSA agent 11 suppresses fluoroquinolone-sensitive strain USA500 and -resistant MRSA isolate Mu50 (MIC =0.39 μg/mL). Anti-MRSA agent 11 displayes favorable in vivo half-life and safety profiles .
|
-
- HY-B0226R
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Nitrofurazone (Standard) is the analytical standard of Nitrofurazone. This product is intended for research and analytical applications. Nitrofurazone (Nitrofural) is a broad spectrum antibiotic that has oral activity. Nitrofurazone is a nitro-aromatic drug. Nitrofurazone is active against both Gram-positive and Gram-negative bacteria .
|
-
- HY-16773
-
|
GS-9451
|
HCV Protease
BCRP
P-glycoprotein
|
Infection
|
|
Vedroprevir (GS-9451) is an inhibitor for HCV NS3/4A protease with an IC50 of 3.2 nM. Vedroprevir is also an inhibitor for breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM. Vedroprevir inhibits P-gp, MRP1 and MRP2 with IC50 of 34, 14.9 and 12 μM, respectively. Vedroprevir exhibits good pharmacokinetic characteristics in rats and dogs .
|
-
- HY-124304
-
|
LOE-908
|
TRP Channel
SARS-CoV
|
Neurological Disease
|
|
Pinokalant is a broad-spectrum and non-selectivecation channel inhibitor. Pinokalant significantly reduces cortical infarct volume. Pinokalant o improves the metabolic and electrophysiologic status of the ischemic penumbra. Pinokalant reduces lesion size on magnetic resonance images in the acute phase following middle cerebral artery occlusion in rats. Pinokalant has the potential for the research of stroke. Pinokalant also shows anti-SARS-CoV-2 activity .
|
-
- HY-122229
-
|
|
HIV
|
Infection
|
|
GS-9822 is a potent antivira agent with nanomolar activity against wild-type HIV-1 viruses. GS-9822 potently inhibits the LEDGF/p75-integrase interaction with an IC50 of 0.07 μM. GS-9822 has high in vitro metabolic stability and favorable oral pharmacokinetic profiles with low systemic clearance in rats, dogs, and monkeys .
|
-
- HY-107384
-
|
EMD-61753
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Asimadoline (EMD-61753) is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
|
-
- HY-76006
-
|
M-Hydroxybenzaldehyde
|
Aldehyde Dehydrogenase (ALDH)
NF-κB
p38 MAPK
|
Cardiovascular Disease
Inflammation/Immunology
|
|
3-Hydroxybenzaldehyde (3-HBA) is a precursor compound for phenolic compounds like Protocatechuic aldehyde (PCA) (HY-N0295). 3-Hydroxybenzaldehyde, produced by 3-hydroxybenzyl-alcohol dehydrogenase, is a substrate of aldehyde dehydrogenase (ALDH) in rats and humans. 3-Hydroxybenzaldehyde has vasculoprotective effects in vitro and in vivo. 3-Hydroxybenzaldehyde is proming for research of atherosclerosis .
|
-
- HY-P1322
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[D-Trp34]-Neuropeptide Y is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y markedly increases food intake in rats .
|
-
![[D-Trp34]-Neuropeptide Y](//file.medchemexpress.eu/product_pic/hy-p1322.gif)
- HY-107384A
-
|
EMD-61753 hydrochloride
|
Opioid Receptor
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
Asimadoline (EMD-61753) hydrochloride is an orally active, selective and peripherally active κ-opioid agonist with IC50s of 5.6 nM (guinea pig) and 1.2 nM (human recombinant). Asimadoline hydrochloride has low permeability across the blood brain barrier and has peripheral anti-inflammatory actions. Asimadoline hydrochloride ameliorates allodynia in diabetic rats and has the potential for irritable bowel syndrome (IBS) .
|
-
- HY-150732
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK4-IN-18 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 value of 15 nM. IRAK4-IN-18 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-18 can be used for researching arthritis disease .
|
-
- HY-150733
-
|
|
IRAK
|
Inflammation/Immunology
|
|
IRAK4-IN-19 is a potent interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitor with an IC50 value of 4.3 nM. IRAK4-IN-19 can inhibit LPS-induced IL23 production in THP and DC cells, and stop arthritis development in arthritis rats. IRAK4-IN-19 can be used for researching arthritis disease .
|
-
- HY-N0157R
-
|
6-Carboxyuracil (Standard); Vitamin B13 (Standard)
|
Nucleoside Antimetabolite/Analog
Endogenous Metabolite
|
Metabolic Disease
|
|
Orotic acid (Standard) is the analytical standard of Orotic acid. This product is intended for research and analytical applications. Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats .
|
-
- HY-N2026R
-
|
|
Endogenous Metabolite
Bacterial
Apoptosis
|
Infection
|
|
Propylparaben (Standard) is the analytical standard of Propylparaben. This product is intended for research and analytical applications. Propylparaben (Propyl parahydroxybenzoate) is an antibacterial preservative that can be produced by plants and bacteria. Propylparaben is commonly used in cosmetics, pharmaceuticals and foods. Propylparaben disrupts follicular growth and steroidogenic function by altering cell cycle, apoptosis and steroidogenic pathways. Propylparaben also reduced sperm count and motility in rats .
|
-
- HY-B0816R
-
|
|
Others
|
Others
|
|
Etofenprox (Standard) is the analytical standard of Etofenprox. This product is intended for research and analytical applications. Etofenprox is an orally active non-ester pyrethroid insecticide. Etofenprox induces toxicity against many pest insects, including Diptera rather than mammalian and fish. Etofenprox has a liver tumor-promoting activity in rats accompanied with microsomal ROS production increase. Etofenprox can be used in agricultural pest control and malaria research .
|
-
- HY-111291
-
|
|
5-HT Receptor
|
Neurological Disease
Endocrinology
|
|
ICI 169369 (free base) is an orally active, selective and non-competitive antagonist against 5HT receptor. ICI 169369 (free base) blunts the vasopressin (AVP), but not the ACTH, prolactin or growth hormone reponses to insulin-induced hypoglycaemia. ICI 169369 (free base) blocks centrally mediated 5-HT responses and lowers portal pressure in portal hypertensive rats .
|
-
- HY-101586A
-
|
Lu 25-109 maleate
|
mAChR
|
Neurological Disease
|
|
Alvameline (Lu 25-109) maleate is a partial agonist of M1 and an antagonist of M2/M3. Alvameline maleate competitively antagonizes contractions induced by ammonium chloride (HY-Y1269) and electrical field stimulation in human detrusor muscle, indicating its potential application in regulating bladder function. Additionally, alvameline maleate can improve cognitive function following traumatic brain injury in rats .
|
-
- HY-129431
-
|
|
Others
|
Others
|
|
U-89843A is a precursor of U-97924 and forms U-97924 as the major metabolite. Although U-97924 showed mutagenic potential in rat hepatocytes in a serum-free in vitro assay, no genotoxicity of U-97924 was observed in rats at high oral doses. Rat serum also inhibited the in vitro metabolism of U-89843 and the formation of the corresponding hydroxylated metabolite, U-97924 .
|
-
- HY-146112
-
|
|
IRAK
|
Cancer
|
|
IRAK4-IN-14 (compound 28) is a potent, selective and orally active IRAK4 inhibitor with an IC50 of 0.003 µM. IRAK4-IN-14 shows good PK parameters in rats and mouse. IRAK4-IN-14 shows synergistic in vitro activity against MyD88/CD79 double mutant ABC-DLBCL in combination with Acalabrutinib .
|
-
- HY-18596
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
SB-215505 is a potent and subtype-selective 5-HT2B receptor antagonist with pKi values of 8.3, 6.77, 7.66 for 5-HT2B, 5-HT2A, 5-HT2C, respectively . SB-215505 increases wakefulness and motor activity in rats .
|
-
- HY-139467
-
|
|
SHP2
PKC
|
Metabolic Disease
|
|
PF-04577806 is a potent, selective and ATP competitive PKC inhibitor. PF-04577806 shows potent inhibitory activity towards PKCα, PKCβI, PKCβII, PKCγ, and PKCθ with IC50s of 2.4 nM, 8.1 nM, 6.9 nM, 45.9 nM, and 29.5 nM, respectively. PF-04577806 can reverse retinal vascular leakage in diabetic rats .
|
-
- HY-145196
-
|
|
Cannabinoid Receptor
|
Neurological Disease
|
|
RTICBM-189 is a potent, brain-penetrant allosteric modulator of the cannabinoid type-1 (CB1) receptor with a pIC50 of 7.54 in Ca 2+ mobilization assay. RTICBM-189 has pIC50s of 5.29 and 6.25 for hCB1 and mCB1, respectively. RTICBM-189 significantly and selectively attenuates the reinstatement of the addictive agent-seeking behavior in rats .
|
-
- HY-100813
-
|
|
GABA Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats .
|
-
- HY-129143
-
|
Dp3‐Sam chloride
|
Others
|
Metabolic Disease
Inflammation/Immunology
|
|
Delphinidin-3-sambubioside (Dp3‐Sam) chloride is an anthocyanin that has orally active anti-inflammatory activity. Delphinidin-3-sambubioside chloride inhibits LPS-induced inflammatory factors release. Delphinidin-3-sambubioside chloride also alleviates hepatic lipid accumulation in HFD rats. Delphinidin-3-sambubioside chloride can be isolated from Hibiscus sabdariffa L. .
|
-
- HY-158014
-
|
|
Dopamine Transporter
|
Neurological Disease
|
|
JJC8-089 is a dopamine transporter (DAT) inhibitor that may improve motivational dysfunction and increase effortful behavior in goal-directed activities. JJC8-089 significantly reversed the low-effort effects induced by the VMAT-2 inhibitor Tetrabenazine (HY-B0590) in rats and increased the choice of high-effort fixed-ratio 5-bar presses versus food intake. .
|
-
- HY-N0264R
-
|
|
Apoptosis
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Inflammation/Immunology
Cancer
|
|
Ligustrazine (Standard) is the analytical standard of Ligustrazine. This product is intended for research and analytical applications. Ligustrazine (Chuanxiongzine), an alkylpyrazine isolated from Ligusticum chuanxiong Hort. (Chuan Xiong) , is present in french fries, bread, cooked meats, tea, cocoa, coffee, beer, spirits, peanuts, filberts, dairy products and soy products as fragrance and flavouring ingredienexhibits. Ligustrazine also has potential nootropic and anti-inflammatory activities in rats .
|
-
- HY-121328
-
|
S-2852F
|
Parasite
|
Infection
Neurological Disease
|
|
Empenthrin (S-2852F) is a synthetic pyrethroid. Empenthrin can be used in insecticides. Empenthrin shows a clear species-specificity in the inhibitory effect on the Pentobarbital (PTB)-metabolizing enzyme(s). Empenthrin prolongs PTB induced-sleeping time in mice through an inhibition of the PTB-metabolizing enzyme(s) in the liver, an effect that does not occur in rats. Empenthrin shows a clear species-specificity in the inhibitory effect on the PTB-metabolizing enzyme(s) .
|
-
- HY-18211
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
CGS 35601 is the inhibitor for endothelin-converting enzyme-1 (ECE-1), neutral endopeptidase 24.11 (NEP), and angiotensin-converting enzyme (ACE), with IC50s of 55, 2, and 22 nM, respectively. CGS 35601 suppresses the big endothelin-1 (big ET-1)- and angiotensin I-induced pressor response, and enhances circulation of atrial natriuretic peptide (ANP), regulates the cardiovascular function in SD rats .
|
-
- HY-W017457R
-
|
|
Others
|
Others
|
|
DL-Penicillamine (Standard) is the analytical standard of DL-Penicillamine. This product is intended for research and analytical applications. DL-Penicillamine [(±)-Penicillamine] is a copper chelating agent. DL-Penicillamine has antidotal effects in thallotoxicosis rats when co-treated with Prussian blue (HY-106594A). DL-Penicillamine can cause pyridoxine deficiency and then induce optic axial neuritis. DL-Penicillamine can also depress primary immune response .
|
-
- HY-155992
-
|
|
Sigma Receptor
|
Neurological Disease
|
|
WLB-89462 (Compound 20c) is a selective σ2 receptor ligand (Ki: 13 nM). WLB-89462 has neuroprotective activity. WLB-89462 improves short-term memory impairment induced by Aβ peptide in rats. WLB-89462 has good ADMET profile (good solubility, no CYP inhibition, good metabolic stability, high permeability, brain penetration, and high oral exposure in rodents) .
|
-
- HY-B0124
-
|
AD 810; CI 912
|
Carbonic Anhydrase
Apoptosis
|
Neurological Disease
|
|
Zonisamide (AD 810) is an orally active carbonic anhydrase inhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy .
|
-
- HY-B0124A
-
|
AD 810 sodium; CI 912 sodium
|
Carbonic Anhydrase
Apoptosis
|
Cardiovascular Disease
Neurological Disease
|
|
Zonisamide (AD 810) sodium is an orally active carbonic anhydrase inhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide sodium exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide sodium also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide sodium can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy .
|
-
- HY-17444
-
|
|
PPAR
|
Metabolic Disease
Cancer
|
|
Tesaglitazar is a dual peroxisome proliferator-activated receptor (PPAR) alpha/gamma agonist that is more potent on PPARγ than on PPARα, with EC50s of 13.4 μM and 3.6 μM for rat PPARα and human PPARα, respectively, and approximately 0.2 μM for both rat and human PPARγ. Tesaglitazar induces interstitial mesenchymal cell DNA synthesis and fibrosarcomas in subcutaneous tissues in rats .
|
-
- HY-112671
-
|
RTA dh404
|
Keap1-Nrf2
NF-κB
|
Inflammation/Immunology
|
|
CDDO-dhTFEA (RTA dh404) is a synthetic oleanane triterpenoid compound which potently activates Nrf2 and inhibits the pro-inflammatory transcription factor NF-κB . CDDO-dhTFEA restores hypertension (MAP), increases Nrf2 and expression of its target genes, attenuates activation of NF-κB and transforming growth factor-β pathways, and reduces glomerulosclerosis, interstitial fibrosis and inflammation in the chronic kidney disease (CKD) rats .
|
-
- HY-15671
-
|
|
Glucokinase
|
Metabolic Disease
|
|
GKA50 is a potent glucokinase activator (EC50=33 nM at 5 mM glucose). GKA50 stimulates insulin release from mouse islets of Langerhans. GKA50 is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 shows significant glucose lowering in high fat fed female rats .
|
-
- HY-110143
-
|
|
Potassium Channel
|
Neurological Disease
|
|
CLP257 is a selective K +-Cl ? cotransporter KCC2 activator with an EC50 of 616 nM. CLP257 is inactive against NKCC1, GABAA receptors, KCC1, KCC3 or KCC4. CLP257 restores impaired Cl ? transport in neurons with diminished KCC2 activity. CLP257 alleviates hypersensitivity in rats with neuropathic pain. CLP257 modulates plasmalemmal KCC2 protein turnover post-translationally .
|
-
- HY-P1322A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[D-Trp34]-Neuropeptide Y TFA is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y TFA is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y TFA markedly increases food intake in rats .
|
-
![[D-Trp34]-Neuropeptide Y TFA](//file.medchemexpress.eu/product_pic/hy-p1322a.gif)
- HY-135483A
-
|
|
nAChR
|
Neurological Disease
|
|
AR-R17779 hydrochloride is a potent and selective full agonist of nAChR, with Kis of 92 and 16000 nM for α7 and α4β2 subtype, respectively. AR-R17779 hydrochloride can improve learning and memory in rats. AR-R17779 hydrochloride also has anxiolytic activity. AR-R17779 hydrochloride can reduce inflammation by activating antiinflammatory cholinergic (vagal) pathways .
|
-
- HY-15671A
-
|
|
Glucokinase
|
Metabolic Disease
|
|
GKA50 quarterhydrate is a potent glucokinase activator (EC50=33 nM at 5 mM glucose) and stimulates insulin release from mouse islets of Langerhans. GKA50 quarterhydrate is a glucose-like activator of beta-cell metabolism in rodent and human islets and a Ca 2+-dependent modulator of insulin secretion. GKA50 quarterhydrate shows significant glucose lowering in high fat fed female rats .
|
-
- HY-A0039S1
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
Eletriptan-d5 is the deuterium labeled Eletriptan[1]. Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine[2].
|
-
- HY-163005
-
|
|
Glucosidase
|
Metabolic Disease
|
|
α-Glucosidase-IN-43 (compound AS14) is an α-glucosidase inhibitor (IC50: 4.32 μM) with acute hypoglycemic activity. α-Glucosidase-IN-43 exhibits safety and in vivo efficacy, is nontoxic to normal mouse fibroblasts, and is able to rescue streptozotocin (HY-13753)-induced diabetic rats. α-Glucosidase-IN-43 can be used to study postprandial hyperglycemia in diabetic patients .
|
-
- HY-125626
-
|
8-iso-15-keto PGF2α
|
Prostaglandin Receptor
|
Cardiovascular Disease
|
|
8-iso-15-keto Prostaglandin F2α (8-iso-15-keto PGF2α) is a partial agonist for Thromboxane receptor (TP), which exhibits a vasoconstrictor efficacy with a pD2 of 5.8. 8-iso-15-keto Prostaglandin F2α mediates a weak relaxation of rats aorta rings at high concentration .
|
-
- HY-125091
-
|
|
Estrogen Receptor/ERR
|
Cancer
|
|
LY2066948 is a selective and orally active estrogen receptor modulator (SERM). LY2066948 has high affinity for estrogen receptors ERα and ERβ (Ki: 0.51 and 1.36 nM respectively) and shows potent antiestrogenic activity. LY2066948 blocks uterine weight gain induced by Ethynyl estradiol (HY-B0216) in immature rats. LY2066948 can be used for research of uterine fibroids and myomas .
|
-
- HY-129210
-
|
|
Phosphodiesterase (PDE)
Potassium Channel
|
Cardiovascular Disease
|
|
KMUP-4, as a xanthine derivative with cGMP-enhancing activity, induces aortic relaxation through endothelium-dependent and independent mechanisms. KMUP-4 increases cytoplasmic cyclic guanosine monophosphate (cGMP) and cyclic adenosine monophosphate (cAMP) levels by inhibiting phosphodiesterases (PDEs) and activating K + channels. KMUP-4 can be used in the study of cardiovascular diseases .
|
-
- HY-124064
-
|
|
Acyltransferase
|
Metabolic Disease
|
|
TMP-153 is an orally active inhibitor of ACAT with an IC50 value of approximately 5-10 nM against hepatic and intestinal ACAT in varicose animals. TMP-153 exhibits cholesterol-lowering effects and can be utilized in the research of atherosclerosis .
|
-
- HY-106892
-
|
348U87
|
DNA/RNA Synthesis
|
Infection
|
|
BW 348U87 is an inhibitor for ribonucleotide reductase, which exhibits synergistic effect with Acyclovir (HY-17422), potentiate the antiviral activity of Acyclovir against herpes simplex virus (HSV) in athymic nude mouse model .
|
-
- HY-B1038
-
|
|
Others
|
Inflammation/Immunology
|
|
L-Cysteine methyl ester hydrochloride is an antitussive, phlegmolytic agent used to relieve breathing difficulties caused by large amounts of phlegm. L-Cysteine methyl ester hydrochloride is a copper corrosion inhibitor used in various industrial studies .
|
-
- HY-N7697F
-
|
|
Others
|
Others
|
|
Chitobiose, a chitosan oligosaccharide, is a dimer of β-1,4-linked glucosamine units . Chitobiose has orally activity and high antioxidant activity .
|
-
- HY-113608
-
|
|
Adenosine Receptor
|
Neurological Disease
|
|
VCP171 is a potent adenosine A1 receptor (A1R) positive allosteric modulator (PAM). VCP171 is effective at decreasing excitatory synaptic currents in Lamina II of neuropathic pain model. VCP171 can be used for researching neuropathic pain .
|
-
- HY-150080
-
|
BMS-986180
|
HIV
HIV Integrase
|
Infection
|
|
GSK3739936 (BMS-986180) is a potent HIV-1 allosteric integrase inhibitor with an IC50 value of 11.1 nM and an EC50 value of 1.7 nM. GSK3739936 is also a weak CYP inhibitor (IC50>24.3 μM). GSK3739936 shows favorable pharmacokinetic property in preclinical species with rapid absorption, low to moderate clearance and excellent oral bioavailability .
|
-
- HY-148456
-
-
- HY-P99615
-
|
SB 209763; RSHZ19
|
RSV
|
Infection
|
|
Felvizumab (SB 209763) is a humanized IgG1κ monoclonal antibody directed to distinct neutralizing epitopes on the F glycoprotein of RSV .
|
-
- HY-N8903
-
-
- HY-152535
-
|
|
Others
|
Infection
Inflammation/Immunology
|
|
ATV041 is an orally active Ibuprofen (HY-78131) and nucleotide analogue. ATV041 improves oral pharmacokinetic (PK) profile and tissue distribution with anti-mouse hepatitis virus (MHV) activity. ATV041 reduces viral load, tissue damage and virus-induced inflammation in a dose-dependent manner .
|
-
- HY-161349
-
|
|
Aminopeptidase
|
Inflammation/Immunology
|
|
LTA4H-IN-4 (compound 3) is an orally active LTA4H inhibitor. The IC50 value of LTA4H-IN-4 for hERG is 156 μM. LTA4H-IN-4 can be used in inflammation related studies .
|
-
- HY-P1409
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases .
|
-
- HY-107655
-
|
ABET
|
mAChR
|
Cardiovascular Disease
|
|
Arecaidine but-2-ynyl ester tosylate (ABET) is a selective mAChR M2 agonist that dose-dependently decreases mean arterial pressure and heart rate in rats. Arecaidine but-2-ynyl ester tosylate can be used for cardiovascular disease research . Arecaidine but-2-ynyl ester (tosylate) is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
|
-
- HY-N2026S
-
|
Propyl parahydroxybenzoate-d7; Propyl 4-hydroxybenzoate-d7
|
Isotope-Labeled Compounds
|
Others
|
|
Propylparaben-d7 (Propyl parahydroxybenzoate-d7)is the deuterium labeledPropylparaben(HY-N2026) . Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats .
|
-
- HY-162583
-
|
|
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
PDE4-IN-17 (compound 4e) is a potent PDE4 inhibitor. PDE4-IN-17 inhibits PDE4B and PDE4D with IC50s of 10.0 and 15.2 nM, respectively. PDE4-IN-17 has good oral bioavailability (F=66%) and longer half-life (t1/2=2.0 h) in SD rats .
|
-
- HY-162647
-
|
|
PI3K
|
Inflammation/Immunology
|
|
PI3Kδ-IN-22 (Compound 26) is a selective inhibitor for PI3Kδ with pKi of 9.3. PI3Kδ-IN-22 inhibits PI3Kδ-AKT signaling pathway in THP-1 cells, with pIC50 of 9.4. PI3Kδ-IN-22 exhibits good pharmacokinetic characters in rats .
|
-
- HY-19202
-
|
rac-EMA401; rac-PD-126055; EMA400
|
Angiotensin Receptor
|
Neurological Disease
|
|
rac-Olodanrigan (rac-EMA401; EMA400) is a racemic mixture of the S-enantiomer (EMA401; HY-13106) and R-enantiomer (EMA402). rac-Olodanrigan is a potent and selective AT2 receptor antagonist with IC50s of 75.2 nM and 2918 nM for AT2R and AT1R, respectively. rac-Olodanrigan evokes dose-dependent relief of mechanical allodynia in the ipsilateral hind paws of rats with a chronic constriction injury (CCI) of the sciatic nerve .
|
-
- HY-76569R
-
|
|
mAChR
|
Neurological Disease
|
|
Desfesoterodine (Standard) is the analytical standard of Desfesoterodine. This product is intended for research and analytical applications. Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-N7860
-
|
|
Others
|
Infection
|
|
Δ2-cis Eicosenoic acid is an α,β-unsaturated fatty acid that has been extracted from fresh water clams and purified. A related compound, 2-octadecenoic acid, has been shown to improve liver function and decrease blood sugar in streptozocin-induced diabetic rats. Δ2-cis Eicosenoic acid and its salts have potential medicinal use for treating diabetes and improving lipid metabolism.
|
-
- HY-10932
-
|
Ro 13-5057
|
nAChR
iGluR
|
Neurological Disease
|
|
Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders .
|
-
- HY-12119
-
|
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
GW274150 is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 also displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-W015309
-
|
|
iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
Endogenous Metabolite
|
Neurological Disease
Metabolic Disease
Cancer
|
|
Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
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-
- HY-N1964
-
|
Gibberellin A3
|
Others
|
Others
|
|
Gibberellic Acid is named after the fungus Gibberella fujikuroi. Gibberellic Acid regulates processes in plant development and growth, including seed development and germination, stem and root growth, cell division, and flowering time. Gibberellic Acid also improves plant response to growth stress caused by various environmental stresses, such as cold stress, drought stress, heavy metal stress, etc. Gibberellic Acid also causes increased lipid peroxidation and fluctuations in the antioxidant defense system in rats .
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-
- HY-12119A
-
|
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
GW274150 phosphate is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 phosphate displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 phosphate exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-106720
-
|
YM 09538
|
Adrenergic Receptor
|
Cardiovascular Disease
|
|
Amosulalol (YM 09538) is an orally active and dual inhibitor of α1/β1-Adrenergic Receptor. Amosulalol exhibits antihypertensive activity via α1-Adrenergic Receptor inhibition. Amosulalol decreases reflexogenic increases in heart rate and plasma renin activity (PRA) via β1-Adrenergic Receptor inhibition in spontaneously hypertensive rats (SHR) .
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-
- HY-A0039S2
-
|
|
5-HT Receptor
|
Inflammation/Immunology
|
|
Eletriptan-d5 (hydrochloride) is the deuterium labeled Eletriptan hydrochloride[1]. Eletriptan (UK-116044) hydrochloride is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan hydrochloride has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan hydrochloride can be used for researching migraine[2].
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-
- HY-12119B
-
|
|
NO Synthase
|
Neurological Disease
Inflammation/Immunology
|
|
GW274150 (dihydrochloride) is a potent, selective, orally active and NADPH-dependent inhibitor of human inducible nitric oxide synthase (iNOS) (IC50=2.19 μM; Kd=40 nM) and rat iNOS (ED50=1.15 μM). GW274150 (dihydrochloride) displays less potency for both humans or rats endothelial NOS (eNOS) and neuronal NOS (nNOS). GW274150 (dihydrochloride) exerts a protective role in an acute model of lung injury inflammation .
|
-
- HY-157928
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Keap1-Nrf2-IN-18 (Compound 22) is an orally active Keap1-Nrf2 protein-protein interaction (PPI) inhibitor with good pharmacokinetics (PK) profiles and more potent in vivo activities in rats. Keap1-Nrf2-IN-18 has the strongest inhibitory activity in structure−activity relationship (SAR) study (KD = 0.0029 μM) .
|
-
- HY-130358
-
|
|
Calcium Channel
|
Neurological Disease
|
|
PDDHV is a calcium absorption inducer and may achieve 45Ca 2+ influx by stimulating vanillic acid receptor VR1. PDDHV induces 45Ca 2+ uptake (EC50: 70 nM) in rat dorsal root ganglion neurons (expressing native vanilloid receptors) and calcium mobilization (EC50: 125 nM) in VR1-transfected CHO cells. PDDHV also inhibits [3H]-resiniferatoxin (RTX) binding to the dorsal root ganglion membrane in rats .
|
-
- HY-76569S1
-
|
PNU-200577-d14; 5-Hydroxymethyl Tolterodine-d14
|
mAChR
Isotope-Labeled Compounds
|
Neurological Disease
|
|
(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
|
-
- HY-P5914A
-
|
WaTx TFA
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin TFA (WaTx TFA) is the TFA salt form of Wasabi Receptor Toxin (HY-P5914). Wasabi Receptor Toxin TFA is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin TFA is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin TFA causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-N13218
-
|
|
Others
|
Cardiovascular Disease
|
|
Pueraria Extract is a kudzu extract, and its components include: Isoflavones. Pueraria Extract (ethanol extract) can significantly improve cardiac damage in rats with acute myocardial infarction. Pueraria Extract improves bile acid levels by increasing the expression of CYP7A1 and restoring the diversity of intestinal microbiota. Pueraria Extract can also inhibit the FXR-FGF15 signaling pathway and increase the expression of OST-α to increase bile acid reabsorption and fecal excretion. .
|
-
- HY-116807R
-
|
|
Reactive Oxygen Species
|
Neurological Disease
Inflammation/Immunology
|
|
Dihydrolipoic Acid (Standard) is the analytical standard of Dihydrolipoic Acid. This product is intended for research and analytical applications. Dihydrolipoic Acid (DHLA) is an excellent antioxidant capable of scavenging almost any oxygen-centered radical . Dihydrolipoic acid exhibits anti-inflammatory properties in various diseases. Dihydrolipoic Acid exerts a preventive effect via ERK/Nrf2/HO-1/ROS/NLRP3 pathway in LPS-induced sickness behavior rats. Dihydrolipoic Acid can be used for the reaserch of depression .
|
-
- HY-123411
-
|
BCI 632
|
mGluR
|
Neurological Disease
|
MGS0039 is a type II group mGluR antagonist. MGS0039 has a high affinity for mGluR2 and mGluR3, with Ki values of 2.2 nM and 4.5 nM, respectively. MGS0039 can attenuate the inhibitory effect of glutamate-induced cyclic AMP formation triggered by Forskolin (HY-15371) in CHO cells expressing mGluR2/mGluR3. MGS0039 shows antidepressant-like activity in rats .
|
-
- HY-119379
-
|
HOE-720 free acid
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
Fonsartan (HOE-720) free acid is an orally active angiotensin II receptor (AT1R) antagonist with an IC50 value of 0.48 nM, exhibiting potent antihypertensive activity. Fonsartan free acid dose-dependently inhibits angiotensin II-induced pressor response in rats (ID50 = 0.11 mg/kg) and shows significant long-lasting blood pressure-lowering effects in high-renin animal models. Fonsartan free acid is primarily used in research on hypertension and cardiovascular diseases .
|
-
- HY-D1056A2
-
|
LPS, from Escherichia coli (O127:B8)
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Lipopolysaccharides, from E. coli O127:B8 is a lipopolysaccharide endotoxin from E. coli O127:B8 and TLR-4 activator, Activates disease-associated molecular patterns (PAMPs) of the immune system and induces cell secretion of migratory bodies. Lipopolysaccharides, from E. coli O127:B8 consists of an antigen-specific O-chain, A core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O127:B8 can induce changes in body temperature in rats and is dose and serotype specific. High dose of Lipopolysaccharides, from E. coli O127:B8 can cause a double change of body temperature in rats, that is, hypothermia followed by fever. In addition, Lipopolysaccharides, from E. coli O127:B8 can induce inflammation and inhibit reproduction, and can significantly increase the mitotic activity of mollusks .
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-
- HY-162573
-
|
|
Monoamine Oxidase
|
Neurological Disease
|
|
Monoamine Oxidase B inhibitor 5 (Compound 16d) is a selective and reversible inhibitor for monoamine oxidase B (hMAO-B) with an IC50 of 67.3 nM and a Ki of 82.5 nM. Monoamine Oxidase B inhibitor 5 exhibits good pharmacokinetic characters and weak toxicity in rats model. Monoamine Oxidase B inhibitor 5 alleviates MPTP-induced (HY-15608) motor impairment in Parkinson’s mouse model. Monoamine Oxidase B inhibitor 5 is blood-brain barrier (BBB) penetrate .
|
-
- HY-121670
-
|
|
Others
|
Neurological Disease
|
|
Ambenoxan is a central nervous system-acting skeletal muscle relaxant that is effective in mice, rats, rabbits, dogs, and monkeys without loss of the righting reflex. It has no peripheral neuromuscular blocking effects and significantly reduces or eliminates decerebrate rigidity in rabbits, but does not antagonize the effects of strychnine, leptazol, or tremorine. Like other central nervous system depressants, ambenoxan prolongs sleep duration with hexobarbitone, but it has no local anesthetic effects. In anesthetized cats, the agent lowers blood pressure and reduces the pressor response to epinephrine, but has no effect on norepinephrine.
|
-
- HY-120984
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
AcylCoA:cholesterol acyltransferase (ACAT) is an intracellular cholesteryl ester synthase tied closely to the absorption of dietary cholesterol.1 Oleic acid-2,6-diisopropylanilide is an inhibitor of acylCoA:cholesterol acyltransferase with an IC50 of 7 nM.2 When co-administered to rabbits or rats fed a high fat, high cholesterol diet, oleic acid-2,6-diisopropylanilide decreased low density lipoproteins and elevated high density lipoprotein levels when administered at 0.05%.
|
-
- HY-121888
-
|
|
Others
|
Metabolic Disease
|
|
20-HEPE is a metabolite of eicosapentaenoic acid formed by ω-oxidation of EPA by cytochrome P450 (CYP) ω-oxidases, including human CYP4F3B. At 10 μM, it activates peroxisome proliferator-activated receptor α (PPARα) in COS-7 cells expressing a luciferase reporter gene. 20-HEPE also activates mouse transient receptor potential vanilloid receptor 1 (mTRPV1) in vitro but lacks analgesic activity in rats.
|
-
- HY-121166
-
|
(S)-Betaxolol
|
Adrenergic Receptor
|
Others
|
|
Levobetaxolol is a potent and high affinity β-adrenergic antagonist with IC50 values of 33.2, 2970, 709 nM for guinea pig atrial β1, tracheal β2 and rat colonic β3 receptors, respectively. Levobetaxolol reduces IOP (intraocular pressure). Levobetaxolol exhibits a micromolar affinity for L-type Ca21-channels. Levobetaxolol decreases the effects of ischaemia/reperfusion injury in rats. Levobetaxolol has the potential for the research of glaucoma .
|
-
- HY-155993
-
|
|
PARP
|
Cancer
|
|
YCH1899 is an orally active PARP inhibitor, with an IC50< 0.001 nM for PARP1/2. YCH1899 exhibits distinct antiproliferation activity against Olaparib (HY-10162)-resistant and Talazoparib (HY-16106)-resistant Capan-1 cells (Capan-1/OP and Capan-1/TP cells) , with IC50 values of 0.89 and 1.13 nM, respectively. YCH1899 has acceptable pharmacokinetic properties in rats .
|
-
- HY-B1350A
-
|
Sodium fusidate; SQ-16360
|
Bacterial
Antibiotic
Interleukin Related
|
Infection
Inflammation/Immunology
|
|
Fusidic acid sodium salt is an orally available antibacterial agent that inhibits bacterial protein synthesis by preventing the release of translation elongation factor G (EF-G) from ribosomes. Fusidic acid sodium salt inhibits the inhibitory and activating effects of interleukins IL-1 and IL-6 on glucose-induced insulin production and exhibits antidiabetic effects in a rat model. Fusidic acid sodium salt improves the symptoms of colitis in rats and inhibits the growth of Toxoplasma gondii and Listeria monocytogenes EGD in vitro, but not in mice .
|
-
- HY-W009732
-
|
Sinapic acid
|
HDAC
Angiotensin-converting Enzyme (ACE)
Reactive Oxygen Species
Apoptosis
|
Metabolic Disease
Cancer
|
|
Sinapinic acid (Sinapic acid) is a phenolic compound isolated from Hydnophytum formicarum Jack. Rhizome, acts as an inhibitor of HDAC, with an IC50 of 2.27 mM , and also inhibits ACE-I activity . Sinapinic acid posssess potent anti-tumor activity, induces apoptosis of tumor cells . Sinapinic acid shows antioxidant and antidiabetic activities . Sinapinic acid reduces total cholesterol, triglyceride, and HOMA-IR index, and also normalizes some serum parameters of antioxidative abilities and oxidative damage in ovariectomized rats .
|
-
- HY-117482
-
|
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
|
-
- HY-120355A
-
|
|
Potassium Channel
|
Cardiovascular Disease
|
|
AP14145 hydrochloride is a potent KCa2 (SK) channel negative allosteric modulator with an IC50 of 1.1 μM for KCa2.2 (SK2) and KCa2.3 (SK3) channels. AP14145 hydrochloride inhibition strongly depends on two amino acids, S508 and A533 in the channel. AP14145 hydrochloride prolonged atrial effective refractory period (AERP) in rats and demonstrates antiarrhythmic effects in a Vernakalant-resistant porcine model of atrial fibrillation (AF) .
|
-
- HY-P1323
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
[Leu31,Pro34]-Neuropeptide Y(human,rat) is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) can increase blood pressure in anesthetized rats and increases food intake .
|
-
![[Leu31,Pro34]-Neuropeptide Y (human,rat)](//file.medchemexpress.eu/product_pic/hy-p1323.gif)
- HY-P1323A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA can increase blood pressure in anesthetized rats and increases food intake .
|
-
![[Leu31,Pro34]-Neuropeptide Y(human,rat,mouse) TFA](//file.medchemexpress.eu/product_pic/hy-p1323a.gif)
- HY-117482A
-
|
|
γ-secretase
|
Neurological Disease
|
|
BPN-15606 besylate is a highly potent, orally active γ-secretase modulator (GSM), attenuates the production of Aβ42 and Aβ40 by SHSY5Y neuroblastoma cells with IC50 values of 7 nM and 17nM, respectively. BPN-15606 besylate lowers Aβ42 and Aβ40 levels in the central nervous system of rats and mice. BPN-15606 besylate has acceptable PK/PD properties, including bioavailability, half-life, and clearance .
|
-
- HY-146005
-
|
|
Microtubule/Tubulin
|
Neurological Disease
Inflammation/Immunology
|
|
Tau-aggregation and neuroinflammation-IN-1 is a potent tau-aggregation and neuroinflammation inhibitor. Tau-aggregation and neuroinflammation-IN-1 exhibits remarkable inhibitory activities against AcPHF6 and full-length tau aggregation. Tau-aggregation and neuroinflammation-IN-1 has a low cytotoxicity and reduced NO release in LPS-stimulated BV2 cells. Tau-aggregation and neuroinflammation-IN-1 can reverse okadaic acid-induced memory impairment in rats .
|
-
- HY-P3641
-
|
|
GnRH Receptor
|
Neurological Disease
Metabolic Disease
|
|
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
|
-
- HY-100978
-
|
DL-Hexanoylcarnitine chloride
|
Endogenous Metabolite
|
Metabolic Disease
|
|
(±)-Hexanoylcarnitine chloride is a fatty acid metabolite that breaks down fatty acids into energy that can be used by the body. (±)-Hexanoylcarnitine chloride also serves as a specific and easily detectable biomarker for rat skeletal muscle toxicity. Cerivastatin (HY-129458) and TMPD (HY-W012145) induce an increase in Hexanoylcarnitine in rats in a metabolomic analysis of the rectus femoris muscle. In type 2 diabetes, Hexanoylcarnitine is also significantly associated with and improves prediction of all-cause mortality. Hexanoylcarnitine is a biomarker for the identification of novel pathogenic pathways .
|
-
- HY-N12445
-
|
|
Others
|
Metabolic Disease
|
|
Quercetin-3'-O-glucoside is a flavonol, which can be isolated from the flowers of Quercetin. Quercetin-3'-O-glucoside modulates Alloxan (HY-W017227)-induced hyperglycemia and lipid peroxidation (LPO) in rats, exerting anti-diabetic and anti-peroxidation effects. Quercetin-3'-O-glucoside improves diabetes and tissue lipid peroxidation by virtue of its insulin-stimulating and/or free radical-scavenging properties .
|
-
- HY-18100AR
-
|
|
Sigma Receptor
Akt
NO Synthase
|
Cardiovascular Disease
Neurological Disease
|
|
PRE-084 (hydrochloride) (Standard) is the analytical standard of PRE-084 (hydrochloride). This product is intended for research and analytical applications. PRE-084 hydrochloride is a highly selective σ1 receptor (S1R) agonist, with an IC50 of 44 nM. PRE-084 hydrochloride exhibits good neuroprotective effects, can improve motor function and motor neuron survival in mice. PRE-084 hydrochloride also can ameliorate myocardial ischemia-reperfusion injury in rats by activating the Akt-eNOS pathway .
|
-
- HY-111164
-
|
|
p38 MAPK
Phosphodiesterase (PDE)
|
Inflammation/Immunology
|
|
CBS-3595 is a dual inhibitor of p38 MAP kinase and phosphodiesterase 4 with anti-inflammatory and anti-allodynic activities. CBS-3595 reduces the production of the proinflammatory cytokine IL-6 and increases the levels of the anti-inflammatory cytokine IL-10 in rats. CBS-3595 reduces paw oedema formation in the Complete Freund’s adjuvant (CFA) (HY-153808)-induced arthritis rat model. CBS-3595 is promising for research of autoimmune diseases .
|
-
- HY-129213
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
Others
|
|
CL-242817 is an orally available angiotensin converting enzyme (ACE) inhibitor. CL-242817 inhibits the conversion of angiotensin I to angiotensin II and has blood pressure lowering activity. CL-242817 can also improve Monocrotaline (HY-N0750) induced lung injury. CL-242817 can be used in the study of pulmonary fibrosis and hypertension-related diseases .
|
-
- HY-N0378
-
|
Mannitol; Mannite
|
Endogenous Metabolite
Apoptosis
Adrenergic Receptor
PGC-1α
PKA
|
Metabolic Disease
Cancer
|
|
D-Mannitol (Mannitol) is an oral, resistant sugar widely used in the food and pharmaceutical industries to promote the absorption and retention of calcium and magnesium through cecal fermentation, while acting as a osmotic diuretic to reduce tissue edema. D-Mannitol can enhance brown fat formation, improve insulin effect, reduce blood sugar levels, And through the start the β3-adrenergic receptor (β3-AR), PGC1α and PKA induced by means of white fat cells into brown fat cells .
|
-
- HY-111827
-
-
- HY-Y0946
-
|
|
Biochemical Assay Reagents
|
Inflammation/Immunology
Cancer
|
|
Acetamide is used as an intermediate in the synthesis of methylamine, thioacetamide, and insecticides, and as a plasticizer in leather, cloth and coatings. Acetamide has carcinogenicity. Acetamide derivatives may has antioxidant activity and potential anti-inflammatory activity. Acetamide holds promise for research in the fields of anti-inflammatory and cancer studies .
|
-
- HY-B1727
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Phenanthrene is an orally active polycyclic aromatic hydrocarbon (PAH) that induces inflammation, oxidative stress, and apoptosis. Additionally, phenanthrene is commonly used to detect or assess PAH pollution in the environment .
|
-
- HY-N0171B
-
|
β-Sitosterol (purity>75%); 22,23-Dihydrostigmasterol (purity>75%)
|
Apoptosis
|
Cardiovascular Disease
Inflammation/Immunology
Cancer
|
|
Beta-Sitosterol (purity>75%) is a phytosterol with oral activity. Beta-Sitosterol (purity>75%) interferes with a variety of cell signaling pathways, including the cell cycle, apoptosis and cell proliferation. Beta-Sitosterol (purity>75%) has anti-inflammatory, antioxidant, and antitumor activities .
|
-
- HY-143406
-
|
|
Fungal
|
Infection
|
|
Antifungal agent 25 is a potent broad-spectrum antifungal agent. Antifungal agent 25 shows antifungal effect against Candida albicans and fluconazole-resistant strain of Candida albicans. Antifungal agent 25 stable metabolic property in vivo .
|
-
- HY-146704
-
|
|
Epoxide Hydrolase
COX
|
Cardiovascular Disease
|
|
COX-2/sEH-IN-1 (Compound 9c) is an orally active, dual COX-2 and sEH (soluble epoxide hydrolase) inhibitor with IC50 values of 1.24 µM and 0.40 nM against COX-2 and sEH, respectively. COX-2/sEH-IN-1 shows improved anti-inflammatory activity and highly reduced cardiovascular risks .
|
-
- HY-149179
-
|
|
Bacterial
Antibiotic
|
Infection
|
|
Polymyxin B is an antibiotic. Polymyxin B inhibits Gram-negative infections by binding to the LPS of the bacterial wall with high affinity. Polymyxin B neutralizes the effect of endotoxin. Polymyxin B induces bacterial death by increasing its permeability. Polymyxin B is used in endotoxemia research .
|
-
- HY-163207
-
|
|
Epoxide Hydrolase
HDAC
|
Neurological Disease
|
|
sEH/HDAC6-IN-1 (compound M9) is a selective, orally active dual inhibitor for sEH and HDAC6, with IC50s of 2 nM, 0.72 nM and 5 nM, for human sEH, murine sEH and HDAC6, respectively. sEH/HDAC6-IN-1 reveals analgesic and anti-inflammatory effects .
|
-
- HY-P10269
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GZR18 is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes .
|
-
- HY-B1727R
-
|
|
Apoptosis
|
Inflammation/Immunology
Cancer
|
|
Phenanthrene (Standard) is the analytical standard of Phenanthrene. This product is intended for research and analytical applications. Phenanthrene is an orally active polycyclic aromatic hydrocarbon (PAH) that induces inflammation, oxidative stress, and apoptosis. Additionally, phenanthrene is commonly used to detect or assess PAH pollution in the environment .
|
-
- HY-149340
-
|
|
Cholinesterase (ChE)
|
Neurological Disease
|
|
PD07 is an orally active AChE inhibitor (IC50: 0.29 μM for hAChE). PD07 also inhibits ChEs, BACE1 (IC50: 13.42 μM), and Aβ1–42 aggregation in in vitro. PD07 is an antioxidant, and shows DPPH inhibitory activity (IC50: 26.46 μM). PD07 improves memory and cognition in Scopolamine (HY-N0296)-induced amnesia rats. PD07 can be used for research of Alzheimer’s disease .
|
-
- HY-159091
-
|
|
HIV Integrase
|
Infection
|
|
HIV-1 integrase inhibitor 12 (Compound 17) is an inhibitor for HIV-1 integrase with an IC50 of 1.4 nM. HIV-1 integrase inhibitor 12 inhibits the HIV-1 WT and HIV-1 T125A, with IC50 of 7.4 and 120 nM, respectively. HIV-1 integrase inhibitor 12 exhibits metabolic stability and Caco-2 permeability, and good pharmacokinetic characteristics with good bioavailability (64%) and low clearance (0.16 L/hr/kg) in rats .
|
-
- HY-B2195
-
|
|
Others
|
Metabolic Disease
|
|
Aidioxa has the ability to improve delayed gastric emptying in rats. It can partially improve delayed gastric emptying caused by clonidine or restraint stress. The allyltoin part of Aidioxa restores gastric emptying activity by antagonizing α-2 adrenergic receptors. Its aluminum hydroxide part is involved in restoring gastric compliance. Aidioxa can improve both delayed gastric emptying and impaired gastric compliance, both of which play an important role in functional dyspepsia (FD). Aidioxa is a candidate agent for inhibiting FD.
|
-
- HY-B0124R
-
|
|
Carbonic Anhydrase
Apoptosis
|
Neurological Disease
|
|
Zonisamide (Standard) is the analytical standard of Zonisamide. This product is intended for research and analytical applications. Zonisamide (AD 810) is an orally active carbonic anhydrase inhibitor, with Kis of 35.2 and 20.6 nM for hCA II and hCA V, respectively. Zonisamide exerts neuroprotective effects through anti-apoptosis and upregulating MnSOD levels. Zonisamide also increases the expression of Hrd1, thereby improving cardiac function in AAC rats. Zonisamide can be used in studies of seizure, parkinson’s disease and cardiac hypertrophy .
|
-
- HY-153808B
-
|
|
Toll-like Receptor (TLR)
|
Inflammation/Immunology
|
|
Complete Freund's adjuvant (CFA, 1 mg/ml) is an immunoadjuvant emulsified with antigen that can enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA, 1 mg/ml) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA, 1 mg/ml) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA, 1 mg/ml) stimulates a strong and durable immune response and can be used to induce rheumatoid arthritis in rats, and more .
|
-
- HY-145549
-
|
N-eicosanoyl-D-erythro-Sphingosylphosphorylcholine; SM(d18:1/20:0)
|
Others
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Infection
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C20 Sphingomyelin is a naturally occurring sphingolipid. Levels of C20 sphingomyelin are upregulated in the hippocampus of rats with diabetes induced by streptozotocin (HY-13753) and in human plasma where it is positively correlated with insulin resistance in obese humans. C20 sphingomyelin is also upregulated in the liver of a mouse model of Niemann-Pick type C1 disease, a neurodegenerative cholesterol-sphingolipid lysosomal storage disorder. The plasma concentration of C20 sphingomyelin is decreased in men with prostate cancer. As this product is derived from a natural source, there may be variations in the sphingoid backbone.
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- HY-130272
-
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Others
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Cardiovascular Disease
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Anti-MI/R injury agent 1 (compound 18), a Panaxatriol derivative, is an orally active, potent anti-myocardial ischemia/reperfusion (anti-MI/R) injury agent. Anti-MI/R injury agent 1 enhances oxygen-glucose deprivation and reperfusion (OGD/R)-induced cardiomyocyte injury cell viability. Anti-MI/R injury agent 1 can markedly reduce myocardial infarction size, decrease circulating cardiac troponin I (cTnI) leakage, and alleviate cardiac tissue damage in the rats .
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- HY-W103463
-
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1-Phenylpyrrolidin-2-one
|
GABA Receptor
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Neurological Disease
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|
1-Phenyl-2-pyrrolidinone (1-Phenylpyrrolidin-2-one) is a phenyl analogue of GABA with sedative effect, decreasing the exploratory behavior of rats at 50-100 mg/kg (i.v.). 1-Phenyl-2-pyrrolidinone also has been proved to inhibit emotional reactions in dogs and cats. 1-Phenyl-2-pyrrolidinone induces decreases in the pressor reaction to emotional stress without accompanied by normalization of the function of baroreceptor reflexes .
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-
- HY-155733
-
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iGluR
Cholinesterase (ChE)
Amyloid-β
|
Neurological Disease
|
|
AChE/Aβ-IN-1 (compound 32) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with an IC50 of 86 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 3.876 μM. AChE/Aβ-IN-1 also inhibits Aβ aggregation and shows good blood-brain barrier permeability and neuroprotection. AChE/Aβ-IN-1 improves cognitive and spatial memory impairment in rats model .
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-
- HY-155735
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iGluR
Cholinesterase (ChE)
Amyloid-β
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Neurological Disease
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AChE/Aβ-IN-2 (compound 33) is a potent and orally active inhibitor of acetylcholinesterase (AChE) with IC50 of 135 nM, as well as an antagonist of NMDA receptor (GluN1-1b/GluN2B subunit combination) with IC50 of 5.054 μM. AChE/Aβ-IN-2 also inhibits Aβ aggregation and shows good blood-brain barrier permeability. AChE/Aβ-IN-2 improves cognitive and spatial memory impairment in rats model .
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-
- HY-106353
-
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mAChR
Endogenous Metabolite
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Neurological Disease
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Smilagenin (SMI) is a small-molecule steroidal sapogenin from Anemarrhena asphodeloides and Pelargonium hortorum widely used in traditional Chinese medicine for treating chronic neurodegeneration diseases .
Smilagenin (SMI) improves memory of aged rats by increasing the muscarinic receptor subtype 1 (M1)-receptor density .
Smilagenin (SMI) attenuates Aβ(25-35)-induced neurodegenerationvia stimulating the gene expression of brain-derived neurotrophic factor, may represents a novel therapeutic strategy for AD .
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- HY-P1723A
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Neuropeptide Q TFA
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Neuropeptide Y Receptor
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Metabolic Disease
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Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
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- HY-P4683
-
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Vasopressin Receptor
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Cardiovascular Disease
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(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats .
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- HY-P4683A
-
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Vasopressin Receptor
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Cardiovascular Disease
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(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats .
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- HY-W015309R
-
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iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
|
Neurological Disease
Metabolic Disease
Cancer
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Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
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- HY-101823A
-
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Abbott 81282
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Angiotensin Receptor
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Cardiovascular Disease
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A-81282 (Abbott 81282) is an antagonist of angiotensin II's AT1 receptor, with a pA2 value of 9.64 at the AT1 receptor in rabbit aorta. A-81282 also demonstrates significant inhibitory action on the binding of [125i]_Sar1_lle8_Angiotensin_ll to rat liver membranes, with a pKI value of 8.505. A-81282 has antihypertensive activity and can effectively lower blood pressure in renal artery-ligated rats .
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- HY-B1232R
-
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Endogenous Metabolite
Cytochrome P450
Autophagy
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Neurological Disease
Metabolic Disease
Endocrinology
Cancer
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Metyrapone (Standard) is the analytical standard of Metyrapone. This product is intended for research and analytical applications. Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression .
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- HY-B1232
-
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Su-4885
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Endogenous Metabolite
Cytochrome P450
Autophagy
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Neurological Disease
Metabolic Disease
Endocrinology
Cancer
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Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression .
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- HY-19720A
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ACU-4429 hydrochloride
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Others
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Metabolic Disease
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Emixustat (ACU-4429) hydrochloride is an orally active RPE65 inhibitor with an IC50 value of 4.4 nM. Emixustat hydrochloride is also a visual cycle modulator, capable of regulating visual cycle activity by inhibiting retinol isomerization, and holds potential for studying vision disorders such as age-related macular degeneration (AMD) .
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- HY-19720
-
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ACU-4429
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Others
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Metabolic Disease
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Emixustat is an orally active RPE65 inhibitor with an IC50 value of 4.4 nM. Emixustat is also a visual cycle modulator, capable of regulating visual cycle activity by inhibiting retinol isomerization, and holds potential for studying vision disorders such as age-related macular degeneration (AMD) .
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- HY-117661
-
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SRPK
VEGFR
|
Cardiovascular Disease
Cancer
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SPHINX31 is a potent and selective SRPK1 inhibitor, with an IC50 of 5.9 nM. SPHINX31 inhibits phosphorylation of serine/arginine-rich splicing factor 1 (SRSF1). SPHINX31 also decreases the mRNA expression of pro-angiogenic VEGF-A165a isoform. SPHINX31 can be used to research neovascular eye disease .
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- HY-115989
-
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HCV
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Infection
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HCV-IN-38 is a potent, selective and orally active HCV inhibitor (EC50=15 nM, SI=431). HCV-IN-38 has high anti-HCV activity and low cytotoxicity. HCV-IN-38 has a good safety and oral pharmacokinetic profile .
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- HY-144627
-
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PROTACs
TAM Receptor
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Cancer
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PROTAC Axl Degrader 2 is a potent and selective PROTAC Axl degrader with an IC50 of 1.61 μM. PROTAC Axl Degrader 2 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 2 induces mehuosis .
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- HY-144624
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PROTACs
TAM Receptor
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Cancer
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PROTAC Axl Degrader 1 is a potent and selective PROTAC Axl degrader with an IC50 of 0.92 μM. PROTAC Axl Degrader 1 shows anti-proliferation activity, anti-migration activity in vitro. PROTAC Axl Degrader 1 induces mehuosis .
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- HY-B1232A
-
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Su-4885 Tartrate
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Endogenous Metabolite
Cytochrome P450
Autophagy
mTOR
|
Neurological Disease
Endocrinology
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Metyrapone (Su-4885) Tartrate is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone Tartrate inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone Tartrate increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone Tartrate can be used for researching Cushing's syndrome and depression .
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- HY-158055
-
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Keap1-Nrf2
|
Inflammation/Immunology
|
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Keap1-Nrf2-IN-20 (Compound ZC9) is an inhibitor for Keap-Nrf2 pathway with KD2 of 51 nM. Keap1-Nrf2-IN-20 exhibits good cell permeability, cell activity, and metabolic stability (serum t1/2 > 24 h) .
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- HY-163533
-
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VEGFR
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Inflammation/Immunology
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CPD-002 is an inhibitor for vascular endothelial growth factor receptor 2 (VEGFR 2), that inhibits angiogenesis through inhibition of VEGFR2/PI3K/AKT signaling pathway. CPD-002 exhibits anti-inflammatory activity and attenuates rheumatoid arthritis .
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- HY-P5155
-
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Potassium Channel
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Neurological Disease
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Stromatoxin 1 is an inhibitor of Potassium Channel, a peptide which can be isolated from tarantulas. Stromatoxin 1 selectively inhibits K(V)2.1, K(V)2.2, K(V)4.2, and K(V)2.1/9.3 channels. K(V)2.1 and K(V)2.2, but not K(V)4.2, channel subunits play a key role in opposing both myogenic and neurogenic urinary bladder smooth muscle (UBSM) contractions in rats .
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- HY-135783
-
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nAChR
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Neurological Disease
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AT 1001 is a high-affinity and selective antagonist of the α3β4 nicotinic acetylcholine receptor (α3β4 nAChR) (Ki=2.64 nM). AT 1001 reversibly blocks inward currents induced by Epibatidine (HY-101078) in HEK cells transfected with α3β4 nAChR. AT-1001 dose-dependently inhibits nicotine self-administration behavior in rats without affecting food-reinforced responding. AT 1001 can be utilized in the research of nicotine addiction and smoking cessation therapies .
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- HY-120623
-
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Na+/H+ Exchanger (NHE)
|
Neurological Disease
|
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BMS-284640 is a synthetic sodium hydrogen exchange isomer-1 (NHE-1) inhibitor. BMS-284640 has a more than 380-fold higher NHE-1 inhibitory activity (IC50: 9 nM) compared to cariporide (HY-19693) and is more selective for NHE-1 over NHE-2 (IC50: 1.8 μM) and NHE-5 (IC50: 3.36 μM). BMS-284640 and its analogs also exhibit enhanced oral bioavailability and prolonged plasma half-life in rats. .
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- HY-123567
-
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Others
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Neurological Disease
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LY86057 is an ergoline derivative without N1 substituents. It has higher affinity for porcine, squirrel monkey and human 5-HT2 receptors than rats and is an antagonist of 5-HT2 receptors. When studying the differences in recognition of a series of ergolines between species, LY86057 was found to be more selective for 5-HT2 receptors. Compared with LY53857, LY108742 resulted in a higher affinity for rat 5-HT2 receptors even when the N1 substituent was only methyl.
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-
- HY-118285
-
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mGluR
|
Neurological Disease
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Ro4491533 is a selective, negative allosteric mGluR2/3 receptor modulator that is equally effective on both subtypes. Ro4491533 can completely block glutamate-induced calcium mobilization and glutamate-induced [35S]GTPγS binding accumulation. Ro4491533 has good pharmacokinetic properties in mice and rats, high oral bioavailability, and can pass through the blood-brain barrier. Ro4491533 can also reverse the motor inhibition effect of LY379268 in mice and show antidepressant activity in the forced swim test and tail suspension test.
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- HY-10932R
-
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nAChR
iGluR
|
Neurological Disease
|
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Aniracetam (Standard) is the analytical standard of Aniracetam. This product is intended for research and analytical applications. Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO2-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders .
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- HY-W750595
-
|
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Others
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Cancer
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6-(L-1,2,3-Trihydroxybutyl)-pterin is a derivative of L-biopterin (HY-102015) and is the oxidized form of tetrahydro-L-biopterin (BH4) as well as D-biopterin. Co-ingestion of 6-(L-1,2,3-Trihydroxybutyl)-pterin (0.5%) with the carcinogen 4-dimethylaminoazobenzene reduces the incidence of 4-dimethylaminoazobenzene-induced liver tumors in rats. 6-(L-1,2,3-Trihydroxybutyl)-pterin has been used as an internal standard for the LC-MS quantification of biopterin and neopterin in rat plasma.
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- HY-125088
-
|
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Others
|
Others
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Oleoyl-estrone (OE) is a signaling molecule derived from adipose tissue that reduces energy intake and body fat while maintaining energy expenditure and blood glucose balance. In studies in adrenalodepleted female rats, administration of OE resulted in significant fat mobilization, reduced food intake, and sustained energy expenditure. However, concomitant administration of corticosterone inhibits OE-induced fat mobilization and aggravates insulin resistance and glycemic imbalance by promoting fat deposition. This suggests that corticosterone has an antagonistic effect on the beneficial metabolic effects of OE, particularly on lipid metabolism and insulin sensitivity .
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-
- HY-14151
-
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5-HT Receptor
Apoptosis
Autophagy
|
Neurological Disease
Cancer
|
|
Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
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-
- HY-106224
-
|
Hypocretin-1 (human, rat, mouse)
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Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
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-
- HY-59291
-
|
|
Endogenous Metabolite
Amino Acid Derivatives
|
Neurological Disease
Metabolic Disease
Inflammation/Immunology
|
|
N-Acetyl-L-leucine, an orally bioavailable endogenous metabolite, is an acetylated derivative of amino acid leucine. N-Acetyl-L-leucine is the active form of N-acetyl-leucine (NAL). N-Acetyl-L-leucine attenuates neuronal death and neuroinflammation in the cortical tissue of mice. N-Acetyl-L-leucine also potentially improves ameliorates lysosomal and metabolic dysfunction. N-Acetyl-L-leucine improves compensation of postural symptoms after unilateral chemical labyrinthectomy (UL) in rats. N-Acetyl-L-leucine is promising for research of Niemann-Pick disease type C, traumatic brain injury and neurodegeneration prevention .
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-
- HY-128679
-
|
|
IKK
|
Cancer
|
|
TBK1/IKKε-IN-5 (compound 1) is an orally active TBK1 and IKKε dual inhibitor, with IC50 values of 1 and 5.6 nM, respectively. TBK1/IKKε-IN-5 enhances the blockade response to PD-1 and induces immune memory in rats when combines with anti-PD-L1. TBK1/IKKε-IN-5 can be used in cancer research, especially in tumour immunity .
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-
- HY-N0194
-
|
|
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
|
|
Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
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-
- HY-N1940
-
|
Cycloicaritin
|
Interleukin Related
TNF Receptor
MMP
|
Inflammation/Immunology
|
|
β-Anhydroicaritin is isolated from Boswellia carterii Birdware, has important biological and pharmacological effects, such as antiosteoporosis, estrogen regulation and antitumor properties . β-Anhydroicaritin ameliorates the degradation of periodontal tissue and inhibits the synthesis and secretion of TNF-α and MMP-3 in diabetic rats . β-Anhydroicaritin decreases the overproduction of NO, IL-10, TNF-α, MCP-1 and IL-6 in inperitonitis mice. β-Anhydroicaritin inhibits the elevation of intracellular Ca 2+, and markedly decreases iNOS protein expression .
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-
- HY-101365
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS-102221 is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 can promote the differentiation of new nerve cells. RS-102221 increases food-intake and weight-gain in rats .
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-
- HY-101365A
-
|
|
5-HT Receptor
|
Neurological Disease
|
|
RS-102221 hydrochloride is a selective 5-HT2C receptor antagonist (Ki=10 nM). RS-102221 hydrochloride shows nearly 100-fold selectivity for the 5-HT2C receptor as compared to the 5-HT2A and 5-HT2B receptors. RS-102221 hydrochloride can promote the differentiation of new nerve cells. RS-102221 hydrochloride increases food-intake and weight-gain in rats .
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-
- HY-156124
-
|
|
Sigma Receptor
|
Cancer
|
|
Sigma-2 Radioligand 1 (compound 1) is a Sigma-2 selective ligand. Sigma-2 Radioligand 1 has good biodistribution in mice and good in vivo activity in rats. [18F] Modified Sigma-2 Radioligand 1 for visualization of tumors in micro-PET/CT imaging, exhibiting high tumor uptake and tumor-to-background ratio. Experiments show that Sigma-2 Radioligand 1 binds highly specifically in U87MG glioma xenografts .
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-
- HY-P3206
-
|
Thymulin; Thymic factor
|
ERK
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Serum thymic factor (Thymulin) is a zinc-dependent immunomodulatory peptide hormone, which can be produced by the thymic epithelial cells. Serum thymic factor stimulates the release of hormones from the pituitary gland, exhibits hypophysiotropic activity. Serum thymic factor protects rats from Cephaloridine (HY-B2072)-induced nephrotoxicity by inhibiting ERK activation. Serum thymic factor exhibits anti-diabetic, anti-inflammatory and analgesic effects. Serum thymic factor can be used in research about endocrine, reproductive, neurodegenerative and inflammatory diseases .
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-
- HY-P3247
-
|
|
Insulin Receptor
|
Neurological Disease
Metabolic Disease
|
|
[D-Ala2]-GIP (human) is a GIP receptor agonist. [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc
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-
![[D-Ala2]-GIP (human)](//file.medchemexpress.eu/product_pic/hy-p3247.gif)
- HY-19210
-
|
|
Endothelin Receptor
|
Cardiovascular Disease
|
|
SB-209670 is an extremely potent and highly specific non-peptide, subnanomolar endothelin (ET) receptor antagonist. SB 209670 selectively inhibits binding of 125I-labeled ET-1 to cloned human ET receptor subtypes ETA and ETB (Ki=0.2 and 18 nM, respectively). SB 209670 produces a dose-dependent reduction in blood pressure in hypertensive rats, protects from ischemia-induced neuronal degeneration in a gerbil stroke model, and attenuates neointima formation following rat carotid artery balloon angioplasty .
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-
- HY-14152
-
|
|
5-HT Receptor
|
Cancer
|
|
Prucalopride hydrochloride is an orally active, selective and specific 5-HT4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride hydrochloride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride hydrochloride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride hydrochloride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- HY-12694
-
|
R-108512
|
5-HT Receptor
Apoptosis
Autophagy
|
Metabolic Disease
Cancer
|
|
Prucalopride succinate is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride succinate improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride succinate also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride succinate can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
|
-
- HY-112499
-
|
Vitamin K2-7; Vitamin K2(35); Vitamin MK-7
|
Others
|
Cardiovascular Disease
|
|
Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs (orally active), is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 inhibits osteoclast bone resorption in vitro and stimulates bone formation in femoral tissue of aged female rats. Menaquinone-7 has a well-researched potential in the prevention of aging-induced bone degeneration. Menaquinone-7 is also a pharmacological option for activating Gla matrix protein and intervening in the progression of calcific aortic stenosis (CAVS) .
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-
- HY-106224A
-
|
Hypocretin-1 (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
-
- HY-162729
-
|
|
Histone Demethylase
Monoamine Oxidase
TGF-beta/Smad
|
Cardiovascular Disease
|
|
LSD1-IN-34 (Compound 7d) is the orally active inhibitor for Lysine-specific demethylase (LSD) and monoamine oxidase (MAO), with IC50 of 4.51 and 18.46 nM, for LSD1 and MAO A. LSD1-IN-34 inhibits the Ang II-induced neonatal rat myocardial fibroblasts (NRCFs) activation, without significant toxicity (20 μM). LSD1-IN-34 inhibits TGFβ/Smad signaling pathway, and ameliorates heart failure in mice. LSD1-IN-34 exhibits good pharmacokinetic characteristics in rats .
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-
- HY-101390A
-
|
(R)-Niguldipine hydrochloride
|
Calcium Channel
|
Cardiovascular Disease
|
|
(-)-Niguldipine ((R)-Niguldipine) hydrochloride is a calcium channel antagonist. (-)-Niguldipine hydrochloride exerts a vasodilatory effect by blocking calcium channels and reducing the transmembrane influx of calcium ions. (-)-Niguldipine can inhibit U-46619 (HY-108566)-induced coronary artery contraction in guinea pig Langendorff hearts (pID50 of 9.93), has high affinity for calcium channel binding sites on guinea pig skeletal muscle membranes (Ki of 8.10), and lowers blood pressure in spontaneously hypertensive rats (pED30 of 5.55). (-)-Niguldipine hydrochloride can improve cardiovascular diseases such as hypertension, angina pectoris, and arrhythmias .
|
-
- HY-P1556
-
|
|
PKG
|
Cardiovascular Disease
|
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Vasonatrin Peptide (VNP) is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway .
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- HY-P1556A
-
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PKG
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Metabolic Disease
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Vasonatrin Peptide (VNP) TFA is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide TFA possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide TFA protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway .
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- HY-115986
-
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Monoamine Oxidase
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Neurological Disease
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|
MAO-B-IN-5 is a potent, selective and orally active MAO-B inhibitor with an IC50 of 0.204 µM. MAO-B-IN-5 has the potential for the research of Parkinson's disease (PD) .
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- HY-155406
-
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Estrogen Receptor/ERR
Caspase
Bcl-2 Family
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Cancer
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|
Estrogen receptor modulator 10 (compound G-5b) is an Estrogen receptor (ER) antagonist (IC50=6.7 nM) and degrader (DC50=0.4 nM). Estrogen receptor modulator 10 can induce apoptosis. Estrogen receptor modulator 10 can block cells at the G1/G0 phase. Estrogen receptor modulator 10 can be used in cancer studies .
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-
- HY-163537
-
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Cholinesterase (ChE)
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Neurological Disease
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|
AChE/BuChE-IN-5 (compound 5a) is a dual target inhibitor. AChE/BuChE-IN-5 has excellent nanomolar inhibitory activity on acetylcholinesterase (AChE) (IC50=46.9 nM) and butyryl cholinesterase (BuChE) (IC50=3.5 nM). AChE/BuChE-IN-5 can be used for Alzheimer's Disease research .
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-
- HY-120714
-
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16091 RP
|
Others
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Inflammation/Immunology
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|
Metiazinic acid (16091 RP) is an anti-inflammatory agent. Metiazinic acid can be used for study of inflammation .
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- HY-15048
-
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PARP
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Inflammation/Immunology
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GPI 15427 is a potent inhibitor of the enzyme poly (ADP-ribose) polymerase-1 (PARP-1), which plays a harmful role during inflammation. In a rat model of gut injury and inflammation, including splanchnic artery occlusion (SAO) shock and dinitrobenzene sulfonic acid (DNBS)-induced colitis, GPI 15427 demonstrated strong anti-inflammatory effects. It reduced inflammatory cell infiltration, histological injury, and delayed clinical signs of inflammation. GPI 15427 also diminished the accumulation of poly (ADP-ribose) in the ileum and colon of treated rats. These results suggest GPI 15427 could be useful for treating intestinal ischemia and inflammation .
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- HY-118264
-
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Angiotensin-converting Enzyme (ACE)
Neprilysin
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Cardiovascular Disease
|
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MDL-100240 is a dual-acting angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP) inhibitor. MDL-100240 can significantly lower blood pressure, reverse left ventricular hypertrophy, and effectively prevent hypertrophy and dilatation of the aorta and resistance arteries, with an effect comparable to that of ramipril (HY-B0279). In addition, MDL-100240 can also reduce aldosterone levels, but has no significant effect on atrial natriuretic peptide and cGMP. In 3-month-old transgenic rats, MDL-100240 can reduce adrenomedullin concentrations, prevent and reverse severe hypertension and cardiovascular damage, and enhance bradykinin effects.
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- HY-P3641A
-
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GnRH Receptor
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Neurological Disease
Metabolic Disease
|
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Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
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- HY-W052508
-
|
N-Desalkylquetiapine
|
5-HT Receptor
|
Neurological Disease
|
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Norquetiapine is an antidepressant and neuroprotective agent and is the active metabolic component of Quetiapine (HY-14544). Norquetiapine is also a partial 5-HT1A receptor agonist, and a presynaptic α2, 5-HT2C and 5-HT7 b> Receptor antagonist. Norquetiapine can also selectively inhibit norepinephrine transporter (NET), inhibit norepinephrine reuptake, and has potential inhibitory effects on bipolar depression, major depressive disorder, and generalized anxiety disorder. Norquetiapine demonstrated in vivo activity in forced swimming in mice and learned helplessness tests in rats .
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- HY-N0807
-
|
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MMP
NF-κB
JAK
Keap1-Nrf2
|
Metabolic Disease
Inflammation/Immunology
Cancer
|
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Swertiamarin is an orally active natural product with hypoglycemic, lipid-lowering, anti-rheumatic, and antioxidant activities. Swertiamarin can regulate the levels of pro-inflammatory cytokines, MMP, and NF-κB, and promote osteoblast proliferation. Swertiamarin has antioxidant and hepatoprotective effects against carbon tetrachloride induced rat liver toxicity through the Nrf2/HO-1 pathway. Swertiamarin can attenuate inflammatory mediators by regulating JAK2/STAT3 transcription factors in adjuvant induced arthritis rats. Swertiamarin can be used in the research of diabetes and arthritis .
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-
- HY-N0507
-
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TNF Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
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- HY-P5875A
-
|
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Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
P4pal10 TFA is the TFA salt form of P4pal10 (HY-P5875). P4pal10 TFA is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 TFA inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 TFA reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 TFA ameliorates the injury in rats myocardial ischemia/reperfusion (I/R) models .
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- HY-N0194R
-
|
|
Apoptosis
Parasite
|
Inflammation/Immunology
Cancer
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Asiatic acid (Standard) is the analytical standard of Asiatic acid. This product is intended for research and analytical applications. Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
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- HY-103117
-
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5-HT Receptor
|
Neurological Disease
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|
S 32212 is an inverse agonist of the serotonin (5-HT) receptor subtypes 5-HT2CINI and 5-HT2CVSV (Kis=6.6 and 8.9 nM, respectively). It is also an antagonist of the 5-HT2A receptor and the α2B-adrenergic receptor (Ki=5.8 nM for both). S 32212 is greater than 70-fold selective for these receptors in a panel of 80 receptors, enzymes, and ion channels. S 32212 reduces binding of GTPγS to Gαq and decreases the activity of phospholipase C (PLC) in HEK293 cells expressing 5-HT2CINI receptors (EC50s=38 and 18.6 nM, respectively) and in CHO cells expressing 5-HT2CVSV receptors (EC50s=38 and 18.6 nM, respectively). S 32212 (2.5 mg/kg) decreases head twitching, penile erections, and drug discrimination induced by 5-HT receptor agonists in mice and rats. It reduces immobility time in the forced swim test and decreases marble burying in mice and rats when administered at doses of 10 and 40 mg/kg, indicating anti-depressant-like and anxiolytic activities.
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- HY-P3206A
-
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Thymulin acetate; Thymic factor acetate
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ERK
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
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Serum thymic factor acetate (Thymulin acetate) is the acetate salt form of Serum thymic factor (HY-P3206). Serum thymic factor acetate is a zinc-dependent immunomodulatory peptide hormone, which can be produced by the thymic epithelial cells. Serum thymic factor acetate stimulates the release of hormones from the pituitary gland, exhibits hypophysiotropic activity. Serum thymic factor acetate protects rats from Cephaloridine (HY-B2072)-induced nephrotoxicity by inhibiting ERK activation. Serum thymic factor acetate exhibits anti-diabetic, anti-inflammatory and analgesic effects. Serum thymic factor acetate can be used in research about endocrine, reproductive, neurodegenerative and inflammatory diseases .
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- HY-14151R
-
|
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5-HT Receptor
Apoptosis
Autophagy
|
Neurological Disease
Cancer
|
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Prucalopride (Standard) is the analytical standard of Prucalopride. This product is intended for research and analytical applications. Prucalopride is an orally active, selective and specific 5-HT 4 receptor agonist (high affinity), with pKis of 8.6 and 8.1 for human 5-HT4a/4b receptors, respectively. Prucalopride improves intestinal motility by promoting regeneration of the intestinal nervous system in rats. Prucalopride also shows anticancer activity by blocking of the PI3K/AKT/mTor signaling pathway. Prucalopride can be used in studies of chronic constipation, pseudo-intestinal obstruction and cancer .
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- HY-103151A
-
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5-HT Receptor
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Others
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|
CP94253 is a selective, orally active agonist for serotonin receptor 1B (5-HT1B), through competitive binding with iodocyanopindolol (ICP) to the 5-HT1 receptor. CP94253 binds to the 5-HT1B, 5-HT1A, 5-HT1D, 5-HT1C and 5-HT2 receptors, with Kis of 2, 89, 49, 860 and 1600 nM. CP94253 causes satiety, anorexia, weight loss and hyperlocomotion in rats model .
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-
- HY-W679754
-
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PFTrDA
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Others
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Infection
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|
Perfluorotridecanoic acid (PFTrDA) is a perfluoroalkyl substance (PFAS). Embryo larval exposure of PFTrDA induces yolk sac edema and increases mRNA expression of thyroid hormone synthesis genes, including tshβ, in zebrafish when used at concentrations of 0.1 and 0.3 mg/L, respectively. PFTrDA (10 mg/kg) decreases serum testosterone and luteinizing hormone levels, testis palmitic acid, linoleic acid, and oleic acid levels, and the number of Leydig cells in rats in late puberty. Maternal plasma levels of PFTrDA during gestation are positively associated with the development of eczema in female, but not male, infants, and liver levels of PFTrDA are higher in cancerous human livers compared with non-cancerous human livers. It has been found in marine mammals.
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- HY-N7690
-
|
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Calcium Channel
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Cardiovascular Disease
Metabolic Disease
|
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3,5,7,3’,4’-Pentamethoxyflavone is a Ca 2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases .
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-
- HY-156017
-
|
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5-HT Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
5-HT6R antagonist 1 (Comopund 8) is a 5-HT6R antagonist (Ki: 5 nM). 5-HT6R antagonist 1 inhibits platelet aggregation. 5-HT6R antagonist 1 has excellent metabolic stability. 5-HT6R antagonist 1 reverses MK-801 (HY-15084B)-induced memory impairments in rats. 5-HT6R antagonist 1 can be used for Alzheimer's disease (AD) research .
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- HY-132225
-
|
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5-HT Receptor
|
Inflammation/Immunology
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|
SB 206553 is a 5-HT2C inverse agonist. SB 206553 can attenuate methamphetamine-seeking in rats. SB 206553 has activity for 5-HT2 receptor ligands in HEK-293 or CHO-K1 cells expressing human recombinant 5-HT2 receptors with pKi values of 5.6 nM (5-HT2A), 7.7 nM (5-HT2B) and 7.8 nM (5-HT2C), respectively. SB 206553 can be used for the research of psychostimulant abuse disorders .
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- HY-162641
-
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IRAK
NF-κB
p38 MAPK
TNF Receptor
|
Inflammation/Immunology
|
|
AF-45 inhibits IRAK4 and IRAK1, with IC50s of 128 nM and 1765 nM. AF-45 inhibits the release of IL-6 and TNF-α in macrophages, with IC50s of 0.53-1.54 μM and 0.6-2.75 μM. AF-45 is also an inhibitor for NF-κB/MAPK signaling pathway. AF-45 exhibits anti-inflammatory activities against DSS-induced ulcerative colitis and Lipopolysaccharide (HY-D1056)-induced acute lung injury in mouse model. AF-45 exhibits good pharmacokinetic characteristics in rat models .
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-
- HY-W747868
-
|
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HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
Molidustat sodium is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat sodium can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat sodium can be utilized in the research of renal anemia .
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-
- HY-12654
-
|
BAY 85-3934
|
HIF/HIF Prolyl-Hydroxylase
|
Cardiovascular Disease
|
|
Molidustat (BAY 85-3934) is an orally active inhibitor of hypoxia-inducible factor prolyl hydroxylase (HIF-PH) with IC50 values of 480 nM, 280 nM, and 450 nM for PHD1, PHD2, and PHD3, respectively. Molidustat can elevate the levels of circulating erythropoietin (EPO) to near-normal physiological ranges. Molidustat can be utilized in the research of renal anemia .
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- HY-N0108
-
|
Parietin; Rheochrysidin
|
Bacterial
Toll-like Receptor (TLR)
NF-κB
Apoptosis
Autophagy
Antibiotic
|
Infection
Inflammation/Immunology
Cancer
|
|
Physcion (Parietin), an anthraquinone derivative derived from the traditional Chinese medicine rhubarb, is an effective oral active 6-phosphogluconate dehydrogenase inhibitor with blood-brain barrier permeability, with IC50 and Kd values of 38.5 μM and 26.0 μM, respectively. Additionally, Physcion is an inhibitor of the <>bTLR4/NF-κB signaling pathway, exhibiting anti-inflammatory, antibacterial, and anticancer effects, and can induce Apoptosis and Autophagy in cancer cells .
|
-
- HY-163514
-
|
|
Cholinesterase (ChE)
DYRK
|
Neurological Disease
|
|
hAChE-IN-8 (Compound S-12) is a orally effective and selective inhibitor of hAChE (IC50=0.486 μM). hAChE-IN-8 also inhibits BACE-1 (IC50=0.542 μM), and does not inhibit Dyrk1A (IC50>10 μM). hAChE-IN-8 can reduce Aβ aggregation, has good blood-brain barrier penetration. hAChE-IN-8 is mainly used in Alzheimer's disease research .
|
-
- HY-160959
-
|
|
nAChR
|
Neurological Disease
|
|
AN317 is a selective agonist for α6β2-containing nicotinic acetylcholine receptor (nAChR) with Ki of 6.2 nM and 4.1 nM, for α6/α3β2β3 receptor and α4β2 receptor, respectively. AN317 induces dopamine release in the synaptosomes of the rat striatum, enhances dopaminergic neuronal activity in substantia nigra, and exhibits protective efficacy to rat neurons against dopamine neurotoxin MPP +. AN317 exhibits good pharmacokinetic characteristics in rats. AN317 penetrates the blood-brain barrier (BB) .
|
-
- HY-121129
-
|
FLB-131
|
Dopamine Receptor
|
Neurological Disease
|
|
Eticlopride, a potent and selective D2 receptor antagonist, was investigated in rats with extensive dopamine denervation induced by 6-hydroxydopamine. Daily injections of eticlopride over 21 days increased D2 receptor density in intact brain regions but did not further augment already increased densities in denervated areas. Despite receptor density changes, functional sensitivity remained evident, as shown by contralateral rotations induced by D2 agonist quinpirole during wash-out periods. The study suggests that chronic D2 receptor blockade and dopamine denervation may share a common mechanism in upregulating D2 receptor density, contrary to previous reports suggesting additive effects of denervation and antagonist treatment .
|
-
- HY-W017540
-
|
|
ATP Synthase
|
Cardiovascular Disease
Neurological Disease
Metabolic Disease
Cancer
|
|
Cyclocreatine, a creatine analogue, acts as a brain-penetrant and potent bioenergetic protective agent by providing high levels of ATP. Cyclocreatine can be phosphorylated and dephosphorylated by creatine kinases. Cyclocreatine suppresses creatine metabolism ameliorating the cognitive, autistic and epileptic phenotype in a mouse model of creatine transporter defciency. Cyclocreatine protects against ischemic injury and enhances cardiac recovery during early reperfusion in dogs and rats. Cyclocreatine decreases plaque-adjacent neuronal dystrophy in TREM2-deficient mice with amyloid-β pathology. Cyclocreatine is proming for research of ischemic heart disease, cardiovascular diseases, Alzheimer’s disease and other neurodegenerative diseases associated with microglial dysfunction, prostate cancer .
|
-
- HY-155330
-
|
|
5-HT Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
PZ-1922 (Compound 16) is a BBB-penetrable 5-HT6R/5-HT3R antagonist (Ki: 17 nM, 0.45 nM for 5-HT6R/5-HT3R respectively). PZ-1922 reversibly inhibits MAO-B (pIC50: 8.93). PZ-1922 reverses Scopolamine (SCOP) (HY-N0296) induced memory deficits in the novel object recognition (NOR) test in rats. PZ-1922 prevents Aβ-induced memory decline in the T-maze test .
|
-
- HY-112499R
-
|
Vitamin K2-7(Standard); Vitamin K2(35)(Standard); Vitamin MK-7 (Standard)
|
Others
|
Cardiovascular Disease
|
|
Menaquinone-7 (Standard) is the analytical standard of Menaquinone-7. This product is intended for research and analytical applications. Menaquinone-7 (Vitamin K2-7), belongs to a class of K2-vitamin homologs (orally active), is originally discovered as the anti-hemorrhagic factors. Menaquinone-7 inhibits osteoclast bone resorption in vitro and stimulates bone formation in femoral tissue of aged female rats. Menaquinone-7 has a well-researched potential in the prevention of aging-induced bone degeneration. Menaquinone-7 is also a pharmacological option for activating Gla matrix protein and intervening in the progression of calcific aortic stenosis (CAVS) .
|
-
- HY-103216A
-
|
|
Adrenergic Receptor
|
Neurological Disease
|
|
RWJ-52353 hydrochloride is an orally potent, highly selective α2D adrenergic receptor agonist (Ki: 1.5 nM) with potential analgesic effects. RWJ-52353 hydrochloride demonstrated analgesic activity in abdominal tests in rats and mice, and improved agitation in mice in the hot plate test and tail flick test. RWJ-52353 hydrochloride also regulates the organic cation transporter (OCT) subtype, inhibiting rOCT1 and rOCT2 with IC50s of 100 μM and 20 μM respectively; it also activates rOCT3, affecting [3H]-1- in cells. Methyl-4-phenylpyridinium ([3H]MPP) transport .
|
-
- HY-N0507R
-
|
|
TNF Receptor
Interleukin Related
|
Neurological Disease
Inflammation/Immunology
|
|
Rosavin (Standard) is the analytical standard of Rosavin. This product is intended for research and analytical applications. Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
|
-
- HY-124110
-
|
|
nAChR
|
Neurological Disease
|
|
TC299423 is an orally active, brain-penetrant, selective and potent agonist for α6β2 ∗ and α4β2 ∗ nicotinic acetylcholine receptors (nAChRs) with anxiolytic and antinociceptive properties. TC299423 acts primarily through α6β2 ∗ nAChRs that are implicated in the anxiolytic effects of nicotine. TC299423 elicits reward-related behavior mediated through α6β2 ∗ nAChRs in hypersensitive α6L90’S mice. TC299423 elicits dopamine release and dose not suppress nicotine self-administration in rats. TC299423 is proming for rasearch of addiction and Parkinson’s disease .
|
-
- HY-N2983
-
|
|
Tyrosinase
|
Others
|
|
Cajanin is a potent and orally active anti-melanogenic agent. Cajanin shows antiproliferative activity in MNT1 Cells. Cajanin efficiently decreases the melanin content. Cajanin down-regulates the mRNA and protein expression levels of MITF, tyrosinase, TRP-1 and Dct (TRP-2). Cajanin induces cell cycle arrest at G2/M and S phase. Cajanin stimulates osteoblast proliferation. Cajanin has the potential for the research of human hyperpigmented disorders and menopausal osteoporosis .
|
-
- HY-144074
-
|
|
LRRK2
|
Neurological Disease
|
|
LRRK2-IN-4 is a potent, selective, CNS-penetran and orally active leucine-rich repeat kinase 2 (LRRK2) inhobitor with an IC50 of 2.6 nM. LRRK2-IN-4 has the potential for the research of Parkinson’s disease .
|
-
- HY-144658
-
|
|
Factor Xa
|
Cardiovascular Disease
|
|
FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>[1].
|
-
- HY-147376
-
-
- HY-164049
-
|
|
Prostaglandin Receptor
|
Inflammation/Immunology
|
|
TG8-260 is a second-generation EP2 antagonist developed to alleviate the pathology of central nervous system and peripheral diseases driven by inflammation. TG8-260 can reduce neuroinflammation and gliosis in the hippocampus of rats after pilocarpine-induced persistent epileptic status. Pharmacokinetic data of TG8-260 showed that its plasma half-life was 2.14 hours and its oral bioavailability was 77.3%. TG8-260 is also a potent inhibitor of CYP450 and shows antagonistic activity in inhibiting EP2 receptor-mediated inflammatory gene expression in BV2-hEP2 microglia, which is suitable for studying anti-inflammatory pathways in animal models of peripheral inflammatory diseases .
|
-
- HY-12193
-
|
|
Histamine Receptor
|
Others
|
|
A-349821 is a histamine H3 receptor antagonist characterized as a radioligand ([3H]-A-349821) for in vivo receptor occupancy assessment. In rats, [3H]-A-349821 penetrated the brain, showing higher levels in the cortex compared to the cerebellum, indicating selective H3 receptor binding. Its cortical occupancy was saturable, correlating with in vitro binding data. Inhibition studies with ABT-239 and other H3 antagonists showed dose-dependent reductions in receptor occupancy, matching blood levels associated with cognitive efficacy in preclinical models. [3H]-A-349821 thus serves as a valid tracer for H3 receptor occupancy, aiding in the development and clinical interpretation of H3 receptor antagonists .
|
-
- HY-118030
-
|
|
Calcium Channel
|
Neurological Disease
|
|
RQ-00311651 is a T-type calcium channel blocker that specifically targets the Cav3.2 isoform with a role in neuropathic and visceral pain. RQ-00311651 significantly inhibits T currents in HEK293 cells expressing human Cav3.1 or Cav3.2. RQ-00311651 also inhibited high potassium-induced calcium signaling. RQ-00311651 also inhibits antiallergic properties in rats and mice with neuropathic pain induced by spinal nerve injury or Paclitaxel (HY-B0015). Oral and intraperitoneal injection (10-20 mg/kg) inhibits Cerulein (HY-A0190)-induced acute pancreatitis and cyclophosphamide-induced cystitis in mice .
|
-
- HY-W010201
-
|
(±)-Citronellol; (±)-β-Citronellol
|
Reactive Oxygen Species
ERK
PI3K
TNF Receptor
Atg8/LC3
p62
Apoptosis
Necroptosis
Autophagy
Fungal
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Citronellol ((±)-Citronellol) is an orally active inducer of apoptosis. Citronellol can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis .
|
-
- HY-W027553
-
|
NIK-247 free base
|
Cholinesterase (ChE)
Potassium Channel
Sodium Channel
|
Neurological Disease
Metabolic Disease
|
|
Ipidacrine is orally active and brain-penetrant AChE and BuChE inhibitors with IC50 values of 1 μM and 1.9 μM, respectively, which is also a partial agonist of M2-cholinergic receptors and a reversible cholinesterase inhibitor. Ipidacrine has a stimulating effect on neuromuscular transmission and excitation along the nerve fibres with a moderately anti-pain effect. Ipidacrine is an aminopyridines and is structurally similar to Tacrine (HY-111338). Ipidacrine is effective in various amnesia models, improves erectile function and inhibits K + and Na +-channels in the neuronal membrane in diabetic rats. Ipidacrine is promising for research of Alzheimer’s disease, ischaemic stroke, idiopathic neuropathy of the facial nerve, diabetes mellitus-induced erectile dysfunction and other deficits in central or peripheral cholinergic deseases .
|
-
- HY-155330A
-
|
|
5-HT Receptor
Monoamine Oxidase
|
Neurological Disease
|
|
PZ-1922 free base is a BBB-penetrable 5-HT6R/5-HT3R antagonist (Ki: 17 nM, 0.45 nM for 5-HT6R/5-HT3R respectively). PZ-1922 free base reversibly inhibits MAO-B (pIC50: 8.93). PZ-1922 free base reverses Scopolamine (SCOP) (HY-N0296) induced memory deficits in the novel object recognition (NOR) test in rats. PZ-1922 free base prevents Aβ-induced memory decline in the T-maze test .
|
-
- HY-126049
-
|
(S)-(-)-Oxiracetam; (S)-ISF2522
|
Apoptosis
|
Neurological Disease
|
|
(S)-oxiracetam (S-ORC) is an inhibitor targeting apoptosis. S-ORC reduces brain infarct size and lessens neurological dysfunction in middle cerebral artery occlusion/reperfusion (MCAO/R) models. S-ORC prevents neuronal apoptosis via activating PI3K/Akt/GSK3β signaling pathway via α7 nAChR after ischemic stroke. S-ORC can prevent neuronal death after ischemic stroke .
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- HY-109968A
-
|
CEP-26401 hydrochloride
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment .
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-
- HY-109968
-
|
CEP-26401
|
Histamine Receptor
|
Neurological Disease
|
|
Irdabisant (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment .
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- HY-B1311
-
|
SKF-525A; U-5446; RP-5171
|
Cytochrome P450
Monoamine Oxidase
Bcl-2 Family
Survivin
PARP
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Proadifen (SKF-525A) hydrochloride is a non-competitive Cytochrome P450 inhibitor with an IC50 value of 19 μM. Proadifen hydrochloride reduces monoamine oxidase A (MAO-A) activity and reverses the antidepressantlike behavioral effect of Imipramine (HY-B1490A) and Desipramine (HY-B1272A) in rats. Proadifen hydrochloride also reduces N, N-dimethyltryptamine (DMT) metabolism in liver microsomes and inhibits N-demethylationand Acridone (HY-W007771) formation. Proadifen hydrochloride augments Lipopolysaccharide (LPS) (HY-D1056)-induced fever and exacerbates Prostaglandin E2 (PGE2) (HY-101952) levels in the rat. Proadifen hydrochloride is promising for research of metabolism-related deseases, ovarian carcinoma, inflammation and dopamine neurons-related deseases .
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-
- HY-101392
-
Harmane
1 Publications Verification
|
Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
Harmane is an inhibitor that binds to benzodiazepine receptors (with an IC50 value of 7 μM), has an IC50 of 24 μM for muscarinic acetylcholine receptors (QNB), an IC50 of 2.8 μM for opioid receptors, and IC50 values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC50 values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) .
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-
- HY-W010201R
-
|
(±)-Citronellol (Standard); (±)-β-Citronellol (Standard)
|
Reactive Oxygen Species
ERK
PI3K
TNF Receptor
Atg8/LC3
p62
Apoptosis
Necroptosis
Autophagy
Fungal
|
Cardiovascular Disease
Neurological Disease
Cancer
|
|
Citronellol (Standard) is the analytical standard of Citronellol. Citronellol (Standard) is an orally active inducer of apoptosis. Citronellol (Standard) can prevent oxidative stress, mitochondrial dysfunction, and apoptosis in the SH-SY5Y cell Parkinson's disease model induced by 6-OHDA by regulating the ROS-NO, MAPK/ERK, and PI3K/Akt signaling pathways. Citronellol (Standard) can induce necroptosis in human lung cancer cells through the TNF-α pathway and accumulation of ROS. Citronellol (Standard) can reduce the levels of LC-3 and p62 to regulate the autophagy pathway, inhibit oxidative stress and neuroinflammation, and thus have neuroprotective effects on Parkinson's rats. Citronellol (Standard) exhibits anti-fungal activity against Trichophyton rubrum by inhibiting ergosterol synthesis .
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- HY-A0093
-
|
KOE-1173 hydrochloride
|
Sodium Channel
|
Cardiovascular Disease
Neurological Disease
|
|
Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research .
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-
- HY-N7140
-
|
γ-Linolenic acid
|
Endogenous Metabolite
Apoptosis
NF-κB
ERK
JNK
|
Neurological Disease
Inflammation/Immunology
Cancer
|
|
Gamma-linolenic acid (γ-Linolenic acid) is an orally active unsaturated fatty acid. Gamma-linolenic acid exerts anti-inflammatory effects by inhibiting the NF-κB pathway and the phosphorylation of ERK1/2 and JNK. At the same time, it exerts anticancer effects by inducing apoptosis (Apoptosis) in cancer cells. Additionally, Gamma-linolenic acid also has antioxidant and memory-improving effects. It holds promise for research in the fields of inflammation, neurology, and cancer diseases .
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-
- HY-N6996
-
|
|
Autophagy
PI3K
mTOR
Akt
|
Inflammation/Immunology
Cancer
|
|
Methyl Eugenol is a bait that has oral activity against oriental fruit fly (Hendel).Methyl Eugenol has anti-cancer and anti-inflammatory activities. Methyl Eugenol can induce Autophagy in cells. Methyl Eugenol can be used in the study of intestinal ischemia/reperfusion injury .
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-
- HY-A0093R
-
|
KOE-1173 hydrochloride (Standard)
|
Sodium Channel
|
Cardiovascular Disease
Neurological Disease
|
|
Mexiletine (hydrochloride) (Standard) is the analytical standard of Mexiletine (hydrochloride). This product is intended for research and analytical applications. Mexiletine is an orally effective antiarrhythmic agent which has also been found to be effective for myotonia and neuropathic pain. Mexiletine exerts its efficacy through blocking sodium channels (IC50 : 75±8 μM for tonic block, 23.6±2.8 μM for use-dependent block), therefore can be used for cardiovascular and neurological research .
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-
- HY-N6996R
-
|
|
Autophagy
PI3K
mTOR
Akt
|
Inflammation/Immunology
Cancer
|
|
Methyl Eugenol (Standard) is the analytical standard of Methyl Eugenol. This product is intended for research and analytical applications. Methyl Eugenol is a bait that has oral activity against oriental fruit fly (Hendel).Methyl Eugenol has anti-cancer and anti-inflammatory activities. Methyl Eugenol can induce Autophagy in cells. Methyl Eugenol can be used in the study of intestinal ischemia/reperfusion injury .
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-
- HY-136410
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
4-hydroxy Nonenal Mercapturic Acid (4-HNE) is generated by the peroxidation of common ω-6 polyunsaturated fatty acids (PUFAs) such as linoleic acid, DGLA, and arachidonic acid. 4-hydroxy Nonenal Mercapturic Acid is rapidly cleared from plasma and enters the enterohepatic circulation in rats as a glutathione conjugate. Approximately two-thirds of 4-hydroxy Nonenal Mercapturic Acid is excreted in the urine within 48 hours, primarily as mercapturic acid conjugates. Approximately half of the metabolites are C-1 aldehydes of 4-hydroxy Nonenal Mercapturic Acid that are reduced to alcohols. The remainder are C-1 aldehydes or have been oxidized to C-1 carboxylic acids. These aldehydes and carboxylic acids can also form gamma-lactols and gamma-lactones, respectively, resulting in at least four or five final urinary metabolites of 4-HNE in vivo.
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-
- HY-P3801
-
|
DiMe-C7
|
Neurokinin Receptor
|
Others
Neurological Disease
Metabolic Disease
|
|
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of addictive agent-seeking behavior in rats .
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-
![[Glp5,(Me)Phe8,Sar9] Substance P (5-11)](//file.medchemexpress.eu/product_pic/hy-p3801.gif)
- HY-W127391
-
|
(Rac)-1,2-Didodecanoylglycerol
|
Biochemical Assay Reagents
|
Others
|
|
1,2-Dilaurin is a diacylglycerol containing lauric acid at the sn-1 and sn-2 positions. It has been used as an internal standard for the quantification of diglycerides in rat desheathed sciatic nerves. [1] Monomolecular films containing 1,2-dilauroyl-rac-glycerol have been used as substrates to measure surface pressure and the effect of pancreatic procolipase and colipase on porcine pancreatic lipase activity. [2] References: [1]. Zhu, X. and Eichberg, J. 1,2-Diacylglycerol content and its arachidonyl-containing molecular species are reduced in the sciatic nerve of streptozotocin-induced diabetic rats. J. Neurochemistry. 55(3), 1087-1090 (1990).[2]. Wieloch, T., Borgstr m, B., Piéroni, G. et al. Porcine trypsinogen and its trypsin-activated form: lipid binding and lipase activation on monomolecular membranes. FEBS Express. 128(2), 217-220 (1981).
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-
- HY-B0328
-
-
- HY-15026
-
|
|
Endogenous Metabolite
|
Inflammation/Immunology
|
|
ATB-429, a novel H2S-releasing derivative of mesalamine, demonstrates significant anti-nociceptive and anti-inflammatory effects in models of irritable bowel syndrome (IBS). By releasing hydrogen sulfide (H2S), ATB-429 modulates colorectal distension-induced hypersensitivity in both healthy and postcolitic rats. It attenuates abdominal withdrawal responses and suppresses spinal c-Fos mRNA expression, indicating its potential to alleviate pain associated with gastrointestinal inflammation. Moreover, ATB-429 down-regulates colonic cyclooxygenase-2 and interleukin-1β mRNA expression, effects not observed with mesalamine alone. The mechanism involves ATP-sensitive K+ (KATP) channels, as evidenced by reversal of ATB-429's effects with glibenclamide. These findings suggest ATB-429 could offer therapeutic benefits for managing painful intestinal disorders linked to inflammation .
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-
- HY-W017113
-
|
|
Endogenous Metabolite
Aryl Hydrocarbon Receptor
|
Metabolic Disease
|
|
2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
|
-
- HY-14608R
-
|
|
Endogenous Metabolite
iGluR
Ferroptosis
Apoptosis
|
Neurological Disease
|
L-Glutamic acid (Standard) is the analytical standard of L-Glutamic acid. This product is intended for research and analytical applications. L-Glutamic acid is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid can be used in the study of neurological diseases .
IC50 & Target:DA .
In Vitro: L-Glutamic acid (120, 500, 750, 1000 mg/dL) can reduce the harmful effect of lithium on the embryonic development of Xenopus Xenopus .
L-Glutamic acid (2, 5, 10, 20 mM, 24-48 h) can induce neuroexcitotoxicity in neuroblastoma .
In Vivo: L-Glutamic acid (3 g/kg, subcutaneous injection) can promote excitotoxic degeneration of retinal ganglion cells in mice .
L-Glutamic acid (750 mg/kg, intraperitoneal injection) can reduce and inhibit oxidative stress induced by chlorpyrifos (CPF) in rats .
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-
- HY-N0124
-
|
Collettiside III; CCRIS 4123
|
Autophagy
Apoptosis
|
Cancer
|
|
Dioscin (CCRIS 4123; Collettiside III) is a natural plant-derived steroidal saponin that has good anti-cancer activity against a variety of cancer cells. Dioscin causes DNA damage and induces apoptosis in HeLa and SiHa cells. Dioscin regulates ROS-mediated DNA damage and mitochondrial signaling pathways, exerting anticancer activity .
|
-
- HY-155489
-
|
|
Anaplastic lymphoma kinase (ALK)
Apoptosis
|
Cancer
|
|
DDO-2728 (compound 19) is a selective AlkB homologue 5 (ALKBH5) inhibitor with an IC50 of 2.97 μM. DDO-2728 increases the abundance of N 6 methyladenosine (m 6A) modifications, inducing cell apoptosis and cycle arrest. DDO-2728 suppresses tumor growth in the MV4−11 xenograft model with favorable safety profile, shows the potential of targeting ALKBH5 in cancer research .
|
-
- HY-30004
-
|
|
Endogenous Metabolite
|
Metabolic Disease
|
|
1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
|
-
- HY-N6792
-
|
T-2 Mycotoxin
|
Apoptosis
DNA/RNA Synthesis
|
Metabolic Disease
|
|
T-2 Toxin (T-2 Mycotoxin) is a toxic trichothecene mycotoxin produced by various Fusarium species in feedstuffs and cereal grains, LD50 values of T-2 Toxin in mice and rats are 5.2 and 1.5 mg/kg BW a,respectively . T-2 Toxin (T-2 Mycotoxin) can be transformed into a variety of metabolite, the typical metabolites of T-2 toxin in animals are HT-2 toxin and T-2-triol, which are hydrolysates . T-2 Toxin (T-2 Mycotoxin) is an inhibitor of protein synthesis resulting from binding peptidyltransferase, which is an integral part of the 60s ribosomal subunit. T-2 Toxin (T-2 Mycotoxin) inhibits the synthesis of DNA and RNA, interferes with the metabolism of membrane phospholipids, and increases the level of liver lipid peroxides . T-2 Toxin (T-2 Mycotoxin) induces apoptosis in the immune system, gastrointestinal tissues, and fetal tissues .
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-
- HY-B0442C
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil dihydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil dihydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM respectively, while IC50s are >1000 nM for PDE3 and PDE4. Vardenafil dihydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels. Vardenafil dihydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes - .
|
-
- HY-B0442R
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0442
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0442A
-
|
|
Phosphodiesterase (PDE)
Endogenous Metabolite
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B1019
-
|
|
Dopamine Receptor
|
Neurological Disease
|
|
Sulpiride is an orally active dopamine D2/D3 receptor antagonist. Sulpiride is an atypical antipsychotic agent of the benzamide family. Sulpiride can be used in research into anxiety, depression and breast cancer .
|
-
- HY-103247
-
|
|
Angiotensin Receptor
|
Cardiovascular Disease
|
|
EMD 66684 is an antagonist of Angiotensin II Type 1 (AT1) receptor. EMD 66684 shows potent binding affinities for the AT1 subtype Ang II receptor with an IC50 value of 0.7 nM. EMD 66684 also serves as an antiischemic cytoprotectant - .
|
-
- HY-B0442B
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil hydrochloride trihydrate is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride trihydrate shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride trihydrate competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride trihydrate can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
|
-
- HY-B0442AS
-
|
|
Endogenous Metabolite
Phosphodiesterase (PDE)
Isotope-Labeled Compounds
|
Metabolic Disease
Inflammation/Immunology
Endocrinology
|
|
Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
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-
- HY-Y0966
-
Glycine
5 Publications Verification
|
Endogenous Metabolite
iGluR
VEGFR
|
Neurological Disease
|
|
Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
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-
- HY-Y0966R
-
|
|
Endogenous Metabolite
iGluR
VEGFR
|
Neurological Disease
|
|
Glycine (Standard) is the analytical standard of Glycine. This product is intended for research and analytical applications. Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
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-
- HY-106024A
-
|
ALT711 bromide
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Others
|
Infection
|
|
Alagebrium bromide is a cross-link breaker. This study investigated the role of advanced glycation end products (AGEs) in mediating protein kinase C (PKC) isoform expression in diabetic nephropathy. In vitro, vascular smooth muscle cells cultured in high glucose (25-mmol/l) showed increased translocation and expression of PKC-α compared with cells cultured in low glucose (5-mmol/l). Coculture with ALT-711 more effectively attenuated the increased expression and translocation of PKC-α compared with aminoguanidine, an inhibitor of AGE formation. Streptozotocin-induced diabetic rats were randomized to no treatment, ALT-711 treatment, or aminoguanidine treatment. Diabetes induced an increase in PKC-α as well as -βI, -βII, and -ε isoforms. ALT-711 and aminoguanidine treatment, both of which attenuated renal AGE accumulation, abolished these increases in PKC expression. However, only ALT-711 reduced the translocation of phosphorylated PKC-α from the cytoplasm to the membrane. ALT-711 treatment attenuated the expression of vascular endothelial growth factor (VEGF) and extracellular matrix proteins (fibronectin and laminin) and was associated with a reduction in albuminuria. Aminoguanidine had no effect on VEGF expression, although a reduction in fibronectin and laminin was observed. These findings suggest that AGEs are important stimulators of PKC activation, particularly PKC-α, in patients with diabetic nephropathy, which can be directly inhibited by ALT-711.
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-
- HY-N0469R
-
|
|
Endogenous Metabolite
Virus Protease
HSV
|
Infection
Metabolic Disease
Inflammation/Immunology
|
L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
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-
- HY-B0592R
-
|
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Trandolapril (Standard) is the analytical standard of Trandolapril. This product is intended for research and analytical applications. Trandolapril (RU44570) is a nonsulfhydryl proagent that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI) .
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-
- HY-B0592
-
|
RU44570
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Trandolapril (RU44570) is a nonsulfhydryl proagent that is hydrolysed to the active diacid Trandolaprilat. Trandolapril is an orally administered angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI) .
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-
- HY-B0592A
-
|
RU44570 hydrochloride
|
Angiotensin-converting Enzyme (ACE)
|
Cardiovascular Disease
|
|
Trandolapril (RU44570) hydrochloride is a nonsulfhydryl proagent that is hydrolysed to the active diacid Trandolapril hydrochlorideat. Trandolapril hydrochloride is an orally active angiotensin converting enzyme (ACE) inhibitor that has been used in the treatment of hypertension and congestive heart failure (CHF), and after myocardial infarction (MI) .
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- HY-136625
-
|
|
Others
|
Neurological Disease
|
|
LY134046 is an inhibitor of norepinephrine N-methyltransferase (NMT). Its cardiovascular activity was studied in anesthetized spontaneously hypertensive rats (SHR). Acute intraperitoneal injection of 10 and 20 mg/kg of LY134046 caused minimal cardiovascular changes, while 40 mg/kg resulted in a sustained decrease in mean arterial blood pressure and heart rate. This hypotension and bradycardia occurred rapidly and occurred when brain NMT activity was significantly inhibited. However, norepinephrine concentrations in rat brains were not significantly reduced at the time when LY134046-induced blood pressure and heart rate effects were maximal. The acute cardiovascular activity of LY134046 was not significantly affected by pretreatment of SHR with phentolamine, propranolol, or atropine, and LY134046 reduced heart rate in suspended SHR. In addition, acute or chronic administration of LY134046 did not antagonize the vasoconstrictor responses induced by sympathetic nerve stimulation or exogenous norepinephrine. These observations suggest that LY134046 does not interact with adrenergic or cholinergic receptors and that its hypotensive and bradycardic effects do not require neurogenic tension. Chronic intraperitoneal administration of LY134046 (40 mg/kg/day) resulted in a sustained and significant inhibition of hypothalamic and brainstem NMT activity, leading to central norepinephrine depletion. During chronic treatment, norepinephrine and dopamine concentrations increased in the brainstem and hypothalamus of SHR. Despite chronic inhibition of central NMT and norepinephrine depletion, cardiovascular parameters in SHR treated groups were not significantly different from those in saline-injected controls. Chronic treatment with LY134046 did not result in tolerance to its central biochemical effects or acute cardiovascular activity. The present study does not support the idea that norepinephrine-producing neurons are involved in the central regulation of cardiovascular function, because the hypotension and bradycardia induced by acute administration of LY134046 occurred before a significant decrease in hypothalamic norepinephrine concentrations, whereas chronic inhibition of central NMT and depletion of norepinephrine resulted in minimal changes in baseline cardiovascular parameters.
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| Cat. No. |
Product Name |
Type |
-
- HY-D0256
-
|
Chlorazol Black E; Ferristatin II disodium; C.I. 30235
|
Dyes
|
|
Direct Black 38 (Chlorazol Black E) is an azo dye. Direct Black 38 induces unscheduled DNA synthesis in liver and micronucleus in bone marrow of rats in vivo .
|
-
- HY-D0256A
-
|
Chlorazol Black E free acid; Ferristatin II; C.I. 30235 free acid
|
Dyes
|
|
Direct Black 38 free acid is an azo dye. Direct Black 38 induces unscheduled DNA synthesis in liver and micronucleus in bone marrow of rats in vivo .
|
-
- HY-B0377G
-
|
MK-208 (GMP)
|
Fluorescent Dye
|
|
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine GMP is a competitive histamine H2-receptor antagonist, inhibits gastric secretion, activates the gastric mucosal defensive mechanisms. Famotidine GMP ameliorates peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD) in rats model .
|
| Cat. No. |
Product Name |
Type |
-
- HY-D1005A6
-
|
PEG-PPG-PEG, 2200 (Averag)
|
Co-solvents
|
|
Poloxamer 124 L44 is block polymer of polyoxyethylene and polyoxypropylene with average molecular mass of 2200. Poloxamer 124 L44 reveals toxicity with an oral LD50 of 5 g/kg in albino rats. Poloxamer 124 L44 causes ocular irritation. Poloxamer 124 L44 forms thermoreversible hydrogel, that is utilized in food additives, drug delivery carriers in cosmetics, pharmaceutical ingredients and tissue engineering .
|
-
- HY-D1056
-
|
LPS
|
Carbohydrates
|
|
Lipopolysaccharides, from E. coli O55:B5 is an endotoxin extracted from E. coli O55:B5, consisting of an antigen-specific chain, A core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O55:B5 activates TLR-4 of immune cells. Lipopolysaccharides, from E. coli O55:B5 can induce the change of body temperature in rats with dose and serotype specificity. Lipopolysaccharides, from E. coli O55:B5 caused a heterogeneous and dose-independent increase in body temperature in rats .
|
-
- HY-D1005A22
-
|
PEG-PPG-PEG, 14600 (Averag)
|
Co-solvents
|
|
Poloxamer 338 F108 is block polymer of polyoxyethylene and polyoxypropylene with average molecular mass of 14600. Poloxamer 338 F108 reduces the aggregation of red blood cells, inhibits proliferation of human lymphocyte cell IIBR1. Poloxamer 338 F108 exhibits short-term and subchronic toxicity in rats .
|
-
- HY-N0157C
-
|
6-Carboxyuracil potassium; Vitamin B13 potassium
|
Cell Assay Reagents
|
|
Orotic acid potassium (Vitamin B13 potassium) is a precursor of pyrimidine bases and is involved in the synthesis of DNA and RNA. Orotic acid potassium stimulates the growth of animals, plants and microorganisms, participates in carbohydrate metabolism, and is necessary for the growth and life activities of organisms. Orotic acid potassium is a measurement indicator in routine newborn screening for urea cycle abnormalities. Orotic acid potassium can cause hepatic steatosis and hepatomegaly in rats .
|
-
- HY-W127391
-
|
(Rac)-1,2-Didodecanoylglycerol
|
Drug Delivery
|
|
1,2-Dilaurin is a diacylglycerol containing lauric acid at the sn-1 and sn-2 positions. It has been used as an internal standard for the quantification of diglycerides in rat desheathed sciatic nerves. [1] Monomolecular films containing 1,2-dilauroyl-rac-glycerol have been used as substrates to measure surface pressure and the effect of pancreatic procolipase and colipase on porcine pancreatic lipase activity. [2] References: [1]. Zhu, X. and Eichberg, J. 1,2-Diacylglycerol content and its arachidonyl-containing molecular species are reduced in the sciatic nerve of streptozotocin-induced diabetic rats. J. Neurochemistry. 55(3), 1087-1090 (1990).[2]. Wieloch, T., Borgstr m, B., Piéroni, G. et al. Porcine trypsinogen and its trypsin-activated form: lipid binding and lipase activation on monomolecular membranes. FEBS Express. 128(2), 217-220 (1981).
|
-
- HY-D1005A16
-
|
PEG-PPG-PEG, 4600 (Averag)
|
Co-solvents
|
|
Poloxamer 235 P85 is block polymer of polyoxyethylene and polyoxypropylene with average molecular mass of 4600. Poloxamer 235 P85 exhibits acute and subchronic toxicity in albino rats with an oral LD50 of >34.6 g/kg. Poloxamer 235 P85 induces ocular irritation in rabbits .
|
-
- HY-B0377G
-
|
MK-208 (GMP)
|
Biochemical Assay Reagents
|
|
Famotidine GMP (MK-208 GMP) is Famotidine (HY-B0377) produced in GMP guideline. Famotidine GMP is a competitive histamine H2-receptor antagonist, inhibits gastric secretion, activates the gastric mucosal defensive mechanisms. Famotidine GMP ameliorates peptic ulcer disease (PUD) and gastroesophageal reflux disease (GERD/GORD) in rats model .
|
-
- HY-D1056A2
-
|
LPS, from Escherichia coli (O127:B8)
|
Carbohydrates
|
|
Lipopolysaccharides, from E. coli O127:B8 is a lipopolysaccharide endotoxin from E. coli O127:B8 and TLR-4 activator, Activates disease-associated molecular patterns (PAMPs) of the immune system and induces cell secretion of migratory bodies. Lipopolysaccharides, from E. coli O127:B8 consists of an antigen-specific O-chain, A core oligosaccharide, and lipid A. Lipopolysaccharides, from E. coli O127:B8 can induce changes in body temperature in rats and is dose and serotype specific. High dose of Lipopolysaccharides, from E. coli O127:B8 can cause a double change of body temperature in rats, that is, hypothermia followed by fever. In addition, Lipopolysaccharides, from E. coli O127:B8 can induce inflammation and inhibit reproduction, and can significantly increase the mitotic activity of mollusks .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P3662
-
|
|
Tyrosinase
|
Cancer
|
|
Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2 is a melanotropin, a melanocyte-stimulating hormone. Ac-[Nle4,D-Phe7]-α-MSH (4-10)-NH2 stimulates tyrosinase and exhibits thermoregulatory effect in rats model .
|
-
- HY-P1555
-
|
Adrenocorticotropic Hormone (1-13)
|
Peptides
|
Inflammation/Immunology
|
|
ACTH (1-13) is a 13-aa peptide, with cytoprotective effects in the model of ethanol induced gastric lesions in rats.
|
-
- HY-P5130
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Big endothelin-1 (rat 1-39) is a 39-residues peptide. Big endothelin-1 (rat 1-39) induces diuretic and natriuretic response in conscious Sprague-Dawley rats. Big endothelin-1 (rat 1-39) raises blood pressure in mice .
|
-
- HY-P4296
-
|
|
Amino Acid Derivatives
|
Others
|
|
H-Gly-Sar-Sar-OH is an orally active tripeptide. H-Gly-Sar-Sar-OH is transported through PepT1 within Caco-2 cells. H-Gly Sar Sar OH has potential applications in material transportation .
|
-
- HY-P0037
-
|
Org 30850ANT
|
Peptides
GnRH Receptor
|
Endocrinology
|
|
Org-30850 is a potent LHRH antagonist designed for treating hormone-dependent disorders. In animal studies, a single subcutaneous dose effectively inhibited ovulation in rats and significantly reduced testosterone levels in male rats for up to 48 hours post-administration. Daily doses of Org-30850 in female rats suppressed estrous cycles, decreased uterine and ovarian weights, and lowered estradiol and FSH serum levels. In male rats, prolonged treatment resulted in reversible reductions in gonadal function and testosterone levels, with almost complete recovery observed after cessation of treatment. Unlike comparable LHRH antagonists, Org-30850 exhibited minimal injection site irritation and no edematous reactions, suggesting a more favorable therapeutic profile .
|
-
- HY-N13127
-
|
|
Peptides
|
Endocrinology
|
|
Segetalin C is a cyclic peptide that increases uterine weight in ovariectomized rats (2.5 mg/kg).
|
-
- HY-P4708
-
|
|
Peptides
|
Neurological Disease
|
|
Excitin 1 is an orally active and CNS-penetrated peptide, alters behavior and brain monoamine and amino acid concentrations in rats .
|
-
- HY-106043
-
|
Wy 40972
|
GnRH Receptor
|
Endocrinology
|
|
Lutrelin (Wy 40972) is a luteinizing hormone releasing hormone (LHRH) agonist. Lutrelin inhibits the growth of the endometrial expiant in rats .
|
-
- HY-P3060
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Atriopeptin II rat, mouse is an atrial natriuretic peptide, which acts as diuretic and natriuretic agent, and a potent relaxant of vascular smooth muscle .
|
-
- HY-P1421A
-
|
|
Peptides
|
Metabolic Disease
|
|
Obestatin(human) TFA is an endogenous peptide derived from the same prepropeptide as ghrelin. Obestatin(human) suppresses food intake and reduce body weight-gain in rats.
|
-
- HY-W141774
-
|
S-Carboxyethylcysteine
|
Peptides
|
Metabolic Disease
|
|
S-(2-Carboxyethyl)-L-cysteine (S-Carboxyethylcysteine) is a non-protein (modified) sulfur amino acid. S-(2-Carboxyethyl)-L-cysteine is present in Acacia seed. S-(2-Carboxyethyl)-L-cysteine can affect the seed’s protein use in rats. S-(2-Carboxyethyl)-L-cysteine suppresses the methionine-induced growth rate, and has a negative effect on the plasma amino acid levels in rats .
|
-
- HY-P1742
-
|
|
Opioid Receptor
|
Metabolic Disease
|
|
Gluten Exorphin B5 is an exogenous opioid peptides derived from wheat gluten, acts on opioid receptor, increases postprandial plasma insulin level in rats .
|
-
- HY-110183
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Angiotensin A is a renin–angiotensin system (RAS) peptide that causes a vasoconstrictive effect dependent on AT1 receptors. Angiotensin A elicits pressor and renal vasoconstrictor responses in normotensive and hypertensive rats .
|
-
- HY-P0048
-
|
Surfagon
|
GnRH Receptor
|
Others
|
|
(Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH (Surfagon, Mwt 1167.34 Da) is an agonist of gonadotropin-releasing hormone (GnRH). (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH can be used as an internal standard for the LC-MS analysis of leuprorelide acetate. (Des-Gly10,D-Ala6,Pro-NHEt9)-LHRH has potential applications in biochemical analysis and fertility .
|
-
- HY-P4201
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
JKC 301 is a selective Endothelin A receptor antagonist. JKC 301 attenuates the pressor effects of nicotine in rats. JKC 301 can be used to study cardiovascular disease caused by smoking .
|
-
- HY-P2497
-
|
|
GCGR
|
Neurological Disease
|
|
Exendin (5-39) is a potent glucagon-like peptide 1 (GLP-1) receptor antagonist. Exendin (5-39) improves memory impairment in β-amyloid protein-treated rats .
|
-
- HY-P3819
-
|
DSIP-P
|
Peptides
|
Neurological Disease
|
|
Delta (Phospho) Sleep Inducing Peptide (DSIP-P) is a long-lasting sleep-promoting peptide. Delta (Phospho) Sleep Inducing Peptide induces changes in the circadian locomotor behavior in rats .
|
-
- HY-P1236
-
|
Atrial natriuretic factor (1-28) (rat, mouse)
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
|
-
- HY-P1193
-
|
|
Peptides
|
Neurological Disease
|
|
GR 82334 is a potent and specific reversible tachykinin NK1 receptor antagonist . GR 82334 inhibits substance P-induced sensitization by blocking SP NK1 receptors in naked mole-rats .
|
-
- HY-P1236A
-
|
Atrial natriuretic factor (1-28) (rat, mouse) TFA
|
Endothelin Receptor
|
Cardiovascular Disease
Endocrinology
|
|
Atrial Natriuretic Peptide (ANP) (1-28), rat, mouse (TFA) is a major circulating form of ANP in rats, potently inhibits Angiotensin II (Ang II)-stimulated endothelin-1 secretion in a concentration-dependent manner.
|
-
- HY-P4405
-
|
|
Peptides
|
Endocrinology
|
|
(D-Ala2)-GRF (1-29) amide (human) is a superagonist of GRF, exhibiting extremely high GH-releasing activity about 50 times that of GRF (1-29) in both pigs and rats .
|
-
- HY-W019878
-
|
β-Lipotropin 61-91
|
Peptides
|
Cardiovascular Disease
Neurological Disease
|
|
β-Endorphin, rat (β-Lipotropin 61-91), a neuropeptide, is involved in cardiovascular regulation. β-Endorphin, rat induces marked, prolonged muscular rigidity and immobility similar to a catatonic state in rats .
|
-
- HY-P10237
-
|
|
Peptides
|
Others
|
|
Calcitonin chicken is a hormone, that regulates calcium metabolism. Calcitonin chicken suppresses the cell motility and bone resorption in neonatal rat osteoclasts .
|
-
- HY-P10320
-
|
Tumstatin (69-88), human
|
PI3K
Akt
|
Cardiovascular Disease
|
|
T3 Peptide is an active fragment of tumstatin. T3 Peptide binds integrin αvβ3/αvβ5, activates the PI3K/Akt/p70S6K signaling pathway, and thus stimulates the proliferation and migration of rat cardiac fibroblasts .
|
-
- HY-12523
-
|
|
Peptides
|
Others
|
|
Peptide M is a synthetic amino acid (18 amino acids in length which correspond to the amino acid positions 303-322 of bovine S-antigen: DTNLASSTIIKEGIDKTV), is capable of inducing experimental autoimmune uveitis in monkeys and Hartley guinea pigs as well as Lewis rats .
|
-
- HY-P1338
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats .
|
-
- HY-P1338A
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
PL-017 TFA is a potent and selective μ opioid receptor agonist with an IC50 of 5.5 nM for 125I-FK 33,824 binding to μ site. PL-017 TFA produces long-lasting, reversible analgesia in rats .
|
-
- HY-P10498
-
|
|
Peptides
|
Neurological Disease
|
|
[Des-Tyr1]-gamma-Endorphin is a neuropeptide, which can be found in human cerebrospinal fluid. [Des-Tyr1]-gamma-Endorphin exhibits antidepressant efficacy, facilitates the extinction of active avoidance and attenuates the passive avoidance behavior in rats .
|
-
- HY-P1694
-
|
|
Bradykinin Receptor
|
Cardiovascular Disease
|
|
B4148 is a selective competitive bradykinin (BK) antagonist that significantly inhibits BK-induced hypotension in rats. In a rat model of endotoxin shock induced by Escherichia coli lipopolysaccharide, B4148 significantly attenuated the decrease in mean arterial blood pressure compared with the control group .
|
-
- HY-P10148
-
|
Ac-[Leu28,31]-NPY (24-36)
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) is a selective agonist of neuropeptide Y Y2 receptor. N-Acetyl [Leu28, Leu31] neuropeptide Y (24–36) attenuates cardiac vagal action in anaesthetised rats .
|
-
- HY-P4689
-
|
|
Peptides
|
Metabolic Disease
|
|
Prolactin-Releasing Peptide (1-31) (rat) is a UHR-1/GRP10 receptor ligand. Prolactin-Releasing Peptide (1-31) (rat) reduces fasting-induced food intake, increases plasma levels of LH, FSH, and testosterone in rats .
|
-
- HY-P2046
-
|
|
Opioid Receptor
|
Neurological Disease
|
|
β-Endorphin (rat) is an endogenous opioid neuropeptide and peptide hormone. β-Endorphin (rat) has analgesic activity and also contributes to food intake in satiated rats. β-Endorphin (rat) can be used in the research of neurological diseases such as analgesia and drug addiction .
|
-
- HY-P1025
-
-
- HY-118534
-
|
BRN-2209058
|
Peptides
|
Endocrinology
|
|
Cyclobutyrol is a potent choleretic agent. Cyclobutyrol also inhibits biliary lipid secretion. Cyclobutyrol induces choleretic is unrelated to bile acids. Cyclobutyrol and bile acids do not compete for the hepatobiliar transport mechanisms[1]
|
-
- HY-P3064
-
|
Leiurotoxin I
|
Potassium Channel
|
Neurological Disease
|
|
Scyllatoxin (Leiurotoxin I) is a peptide toxin, it can be isolated from the venom of the scorpion (Leiurus quinquestriatus hebraeus). Scyllatoxin is a blocker of small-conductance KCa (SK) channel. Scyllatoxin enhances both norepinephrine (NE) and epinephrine (Epi) release in vivo .
|
-
- HY-P1025A
-
-
- HY-P2263A
-
|
|
Peptides
|
Inflammation/Immunology
|
|
KLD-12 TFA is the TFA salt form of KLD-12 (HY-P2263). KLD-12 TFA is a self a 12-residue self-assembling peptide that is used in tissue-engineering. KLD-12 TFA combined with SDF-1 self-assembled polypeptide enhances chondrogenic differentiation of bone marrow stromal cells (BMSCs). KLD-12 TFA hydrogel can fill full-thickness osteochondral defects in situ and improve cartilage repair .
|
-
- HY-P3429
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA is conjugated to the cell permeable peptide TAT47-57. SAMβA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-P10039
-
|
|
Amyloid-β
|
Neurological Disease
|
|
β-Amyloid (1-16) rat is a β-amyloid peptide (Abeta), a metal-binding domain fragment of amyloid. Three amino acid substitutions in β-Amyloid (1-16) rat that differ from humans render rats and mice less susceptible to AD-like neurodegeneration .
|
-
- HY-P2298
-
|
|
Peptides
|
Neurological Disease
|
|
TAT-P4-(DATC5)2 is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a Ki of 1.7 nM. TAT-P4-(DATC5)2 can inhibit addiction in rats .
|
-
- HY-P2479
-
|
|
Peptides
|
Inflammation/Immunology
|
|
Peripheral Myelin Protein P2 (53-78), bovine is derived from bovine peripheral myelin P2 protein amino acid residues 53-78. Peripheral Myelin Protein P2 (53-78), bovine is a T cell epitope for the induction of experimental autoimmune neuritis (EAN) in Lewis rats .
|
-
- HY-P5495
-
|
|
Peptides
|
Others
|
|
Uroguanylin-15 (Rat) is a biological active peptide. (Uroguanylin is a natriuretic peptide, a hormone that regulates sodium excretion by the kidney when excess NaCl is consumed. Uroguanylin and guanylin are related peptides that activate common guanylate cyclase signaling molecules in the intestine and kidney. Uroguanylin was isolated from urine and duodenum but was not detected in extracts from the colon of rats.)
|
-
- HY-P2298A
-
|
|
Peptides
|
Neurological Disease
|
|
TAT-P4-(DATC5)2 TFA is a high-affinity peptide inhibitor of the PICK1 (protein interacting with C kinase-1) PDZ domain, with a Ki of 1.7 nM. TAT-P4-(DATC5)2 TFA can inhibit addiction in rats .
|
-
- HY-P1216A
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 TFA is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors respectively. HS014 TFA increases food intake in free-feeding rats .
|
-
- HY-P3429A
-
|
|
PKC
|
Cardiovascular Disease
|
|
SAMβA TFA is conjugated to the cell permeable peptide TAT47-57. SAMβA TFA, a rationally designed selective antagonist of Mfn1-βIIPKC association. SAMβA TFA is a selective inhibitor of mitofusin 1-βIIPKC association improves heart failure outcome in rats .
|
-
- HY-P5914
-
|
WaTx
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
-
- HY-P10046
-
|
|
Vasopressin Receptor
|
Metabolic Disease
|
|
[Deamino-Pen1,Val4,D-Arg8]-vasopressin (AVP-A) is an arginine-vasopressin (AVP) antagonist. AVP-A can significantly lower plasma aldosterone concentration in rats. AVP-A can be used for the research of the growth and steroidogenic capacity of rat adrenal zona glomerulosa .
|
-
- HY-P1520
-
|
|
GnRH Receptor
|
Neurological Disease
|
|
Prolactin Releasing Peptide (1-31), human is a high affinity GPR10 ligand that cause the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
|
-
- HY-P1428A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
RFRP-1(human) TFA is a potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats.
|
-
- HY-P1520A
-
|
|
GnRH Receptor
|
Neurological Disease
|
|
Prolactin Releasing Peptide (1-31), human (acetate) is a high affinity GPR10 ligand that causes the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
|
- HY-19648
-
|
HOE-427 free base
|
Peptides
|
Neurological Disease
|
|
Ebiratide (HOE-427 free base) is a synthesized ACTH derivative, which acts directly on the central nervous system and exhibits memory-enhancing efficacy .
|
- HY-P10318
-
|
|
GLP Receptor
|
Endocrinology
|
|
SHR-2042 is a selective agonist of the GLP-1 receptor.SHR-2042 improves glycemic control by activating the GLP-1 receptor, enhancing insulin secretion and inhibiting glucagon secretion. SHR-2042 combined with sodium N-(8-[2-hydroxybenzoyl] amino) caprylate (SNAC) promotes monomerization through the formation of micelles and improves oral absorption efficiency .
|
- HY-P10503
-
|
|
Peptides
|
Cardiovascular Disease
Others
Inflammation/Immunology
|
|
S2-16 is a synthetic peptide from the S2 region of cardiac myosin. S2-16 is a cryptic epitope that induces myocarditis in Lewis rats. A cryptic epitope is an epitope that is not recognized by antibodies or T cells after the animal is immunized with the intact antigen. S2-16 can be used to study the mechanism of autoimmune myocarditis .
|
- HY-P3676
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
Neuropeptide Y (3-36) (porcine) is an agonist of neuropeptide Y (NPY) receptor subtype Y2, and stimulates feeding in rats. Neuropeptide Y (3-36) (porcine) is a highly Y2 selective ligand compared with nselective Y1/Y2 receptor ligand, Neuropeptide Y 1-36 .
|
- HY-P1131A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
|
|
M617 TFA is a selective galanin receptor 1 (GAL1) agonist, with Kis of 0.23 and 5.71 nM for GAL1 and GAL2, respectively. M617 TFA, acting through its central GAL1, can promote GLUT4 expression and enhance GLUT4 content in the cardiac muscle of type 2 diabetic rats .
|
- HY-P1216
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
HS014 is a potent and selective melanocortin-4 (MC4) receptor antagonist, with Kis of 3.16, 108, 54.4 and 694 nM for human MC4, MC1, MC3 and MC5 receptors, respectively. HS014 modulates the behavioral effects of morphine in mice. HS014 increases food intake in free-feeding rats .
|
- HY-111615A
-
|
|
Somatostatin Receptor
|
Neurological Disease
Inflammation/Immunology
|
|
J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA has anti-inflammatory activity and it is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats .
|
- HY-P1368
-
|
Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)
|
CRFR
|
Endocrinology
|
|
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) is a potent CRF1 receptor-selective agonist with a Ki of 1.7 nM. Stressin I induces increases in adrenocorticotropic hormone (ACTH) levels in rats .
|
- HY-P3567
-
|
|
Melanocortin Receptor
|
Neurological Disease
|
|
(p-Iodo-Phe7)-ACTH (4-10) is a adrenocorticotrophic hormone (ACTH) derivative, which is produced and secreted by the anterior pituitary gland. (p-Iodo-Phe7)-ACTH (4-10) serves as a melanocortin (MC) receptor antagonist and inhibits α-melanocyte-stimulating hormone (α-MSH)-induced excessive grooming behavior in rats .
|
- HY-W152604
-
|
Cyclo(leu-gly)
|
Dopamine Receptor
|
Neurological Disease
|
|
Cyclo(glycyl-L-leucyl) (Cyclo(leu-gly)), a neuropeptide, down-regulates dopamine (DA) receptors and attenuates dopaminergic supersensitivity. Cyclo(glycyl-L-leucyl) inhibits the development of Morphine induced pain relief as well as dopamine receptor supersensitivity in rats. Cyclo(glycyl-L-leucyl) has the potential for the prevention of tardive and/or L-DOPA (HY-N0304)-induced dyskinesias .
|
- HY-P1368A
-
|
Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41) TFA
|
CRFR
|
Endocrinology
|
|
Stressin I (Cyclo(31-34)[DPhe12,Nle21,38,Glu31,Lys34]Ac-hCRF(4-41)) TFA is a potent CRF1 receptor selective agonist, Ki is 1.7 nM. Stressin I induces an increase in adrenocorticotropic hormone (ACTH) levels in rats .
|
- HY-P5490
-
|
NPQ 53-70
|
Peptides
|
Others
|
|
Spexin-2 (53-70), human,mouse,rat (NPQ 53-70) is a biological active peptide. (This is Spexin-2 (53-70), non-amidated version of the novel peptide hormone that is derived from prohormone proNPQ and is conserved amongst mammalian species. It is a central modulator of cardiovascular and renal function. Spexin-2, when administered to rats, decreases heart rate and increases urine flow rate)
|
- HY-P1322
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[D-Trp34]-Neuropeptide Y is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y markedly increases food intake in rats .
|
- HY-P10617
-
|
|
Peptides
|
Cardiovascular Disease
|
|
Salusin-β is an endogenous bioactive peptide with significant hemodynamic and mitogenic activity. Salusin-β can stimulate the proliferation of quiescent vascular smooth muscle cells (VSMCs) and fibroblasts, leading to a rapid and significant decrease in blood pressure and heart rate. In addition, Salusin-β can stimulate the release of arginine vasopressin from the pituitary gland in rats. This makes Salusin-β have important application potential in cardiovascular disease research .
|
- HY-P1322A
-
|
|
Neuropeptide Y Receptor
|
Neurological Disease
|
|
[D-Trp34]-Neuropeptide Y TFA is a potent and selective neuropeptide Y (NPY) Y5 receptor agonist. [D-Trp34]-Neuropeptide Y TFA is a significantly less potent agonist at the NPY Y1, Y2, Y4, and y6 receptors. [D-Trp34]-Neuropeptide Y TFA markedly increases food intake in rats .
|
- HY-P3803
-
|
|
Peptides
|
Neurological Disease
|
|
[D-Pro4,D-Trp7,9] Substance P (4-11) is a potent antagonist of Substance P (HY-P0201). [D-Pro4,D-Trp7,9] Substance P (4-11) decreases plasma aldosterone (ALDO) concentration .
|
- HY-P1409
-
|
|
Potassium Channel
|
Inflammation/Immunology
|
|
ADWX 1 is a new peptide inhibitor that is potent and selective for Kv1.3 with an IC50 value of 1.89 pM. ADWX 1 inhibits Kv1.3 channel activity specifically to inhibit both the initial calcium signaling and NF-κB activation. ADWX 1 ameliorates the disease in rats of experimental autoimmune encephalomyelitis (EAE) models. ADWX 1 can be used to study T cell-mediated autoimmune diseases .
|
- HY-P5947
-
|
|
Peptides
|
Neurological Disease
|
|
Tat-HA-NR2B9 contains a fragment of the cellmembrane transduction domain of HIV-1 Tat, a influenza virus hemagglutinin (HA) epitope-tag, and the C-terminal 9 amino acids of NR2B (NR2B9c). Tat-HA-NR2B9 reduces infarct size and improves neurological functions in ischemia-induced cerebral injury in the rats
|
- HY-P5914A
-
|
WaTx TFA
|
TRP Channel
|
Neurological Disease
|
|
Wasabi Receptor Toxin TFA (WaTx TFA) is the TFA salt form of Wasabi Receptor Toxin (HY-P5914). Wasabi Receptor Toxin TFA is a cell-penetrating scorpion toxin. Wasabi Receptor Toxin TFA is the activator for TRPA1 ion channel with EC50 in nanomolar level, and prolongs the channel open time, but reduces Ca 2+ permeability. Wasabi Receptor Toxin TFA causes thermal hypersensitivity and mechanical allodynia in rats, without triggering neurogenic inflammation .
|
- HY-P5448
-
|
|
Peptides
|
Others
|
|
MOG (92–106), mouse, rat is a biological active peptide. (This is amino acids 92 to 106 fragment of the myelin oligodendrocyte glycoprotein (MOG) from mouse/rat. Mice with MOG (92–106)-induced experimental autoimmune encephalomyelitis develop extensive B cell reactivity against secondary myelin antigens. Despite the fact that this MOG peptide induces only weak T cell responses, MOG-induced autoimmunity is very severe. This peptide is encephalitogenic in SJL mice, DA rats, and rhesus monkeys.)
|
- HY-P1323
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
[Leu31,Pro34]-Neuropeptide Y(human,rat) is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) can increase blood pressure in anesthetized rats and increases food intake .
|
- HY-P1323A
-
|
|
Neuropeptide Y Receptor
|
Cardiovascular Disease
Neurological Disease
|
|
[Leu31,Pro34]-Neuropeptide Y(human,rat) TFA is a specific neuropeptide Y Y1 receptor agonist. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA slao activates Y4, Y5. [Leu31,Pro34]-Neuropeptide Y(human,rat) TFA can increase blood pressure in anesthetized rats and increases food intake .
|
- HY-P3641
-
|
|
GnRH Receptor
|
Neurological Disease
Metabolic Disease
|
|
Kisspeptin 13 inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
|
- HY-P2263
-
|
|
Peptides
|
Inflammation/Immunology
|
|
KLD-12 is a 12-residue self-assembling peptide that is used in tissue-engineering. KLD-12 combined with SDF-1 self-assembled polypeptide enhances chondrogenic differentiation of bone marrow stromal cells (BMSCs). KLD-12 hydrogel can fill full-thickness osteochondral defects in situ and improve cartilage repair .
|
- HY-P10269
-
|
|
GLP Receptor
|
Metabolic Disease
|
|
GZR18 is an analog of glucagon-like peptide-1 (GLP-1), which exhibits agonistic activity for GLP-1 receptor, with an EC50 of 0.677 nM. GZR18 ameliorates type 2 diabetes .
|
- HY-P1723A
-
|
Neuropeptide Q TFA
|
Neuropeptide Y Receptor
|
Metabolic Disease
|
|
Spexin TFA is a potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Spexin TFA exhibits no significant activity at galanin receptor 1. Spexin TFA is an endogenous satiety-inducing peptide; Spexin TFA inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Spexin TFA attenuates LH secretion in goldfish. Spexin TFA exhibits anxiolytic effects in vivo.
|
- HY-P4683
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats .
|
- HY-P4683A
-
|
|
Vasopressin Receptor
|
Cardiovascular Disease
|
|
(Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin is a potent vasopressin V1 receptor (VP V1R) antagonist. (Phenylac1,D-Tyr(Et)2,Lys6,Arg8,des-Gly9)-Vasopressin significantly decreases the mean arterial pressure (MAP) in rats .
|
- HY-158055
-
|
|
Keap1-Nrf2
|
Inflammation/Immunology
|
|
Keap1-Nrf2-IN-20 (Compound ZC9) is an inhibitor for Keap-Nrf2 pathway with KD2 of 51 nM. Keap1-Nrf2-IN-20 exhibits good cell permeability, cell activity, and metabolic stability (serum t1/2 > 24 h) .
|
- HY-P5155
-
|
|
Potassium Channel
|
Neurological Disease
|
|
Stromatoxin 1 is an inhibitor of Potassium Channel, a peptide which can be isolated from tarantulas. Stromatoxin 1 selectively inhibits K(V)2.1, K(V)2.2, K(V)4.2, and K(V)2.1/9.3 channels. K(V)2.1 and K(V)2.2, but not K(V)4.2, channel subunits play a key role in opposing both myogenic and neurogenic urinary bladder smooth muscle (UBSM) contractions in rats .
|
- HY-106224
-
|
Hypocretin-1 (human, rat, mouse)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)), a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
- HY-P3206
-
|
Thymulin; Thymic factor
|
ERK
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Serum thymic factor (Thymulin) is a zinc-dependent immunomodulatory peptide hormone, which can be produced by the thymic epithelial cells. Serum thymic factor stimulates the release of hormones from the pituitary gland, exhibits hypophysiotropic activity. Serum thymic factor protects rats from Cephaloridine (HY-B2072)-induced nephrotoxicity by inhibiting ERK activation. Serum thymic factor exhibits anti-diabetic, anti-inflammatory and analgesic effects. Serum thymic factor can be used in research about endocrine, reproductive, neurodegenerative and inflammatory diseases .
|
- HY-P3247
-
|
|
Insulin Receptor
|
Neurological Disease
Metabolic Disease
|
|
[D-Ala2]-GIP (human) is a GIP receptor agonist. [D-Ala2]-GIP (human) improves glucose tolerance. [D-Ala2]-GIP (human) shows neuroprotective activity in MPTP-induced Parkinson's disease model. [D-Ala2]-GIP (human) also improves cognitive function and hippocampal synaptic plasticity in obese diabetic rats. [D-Ala2]-GIP (human) can be used for research of type 2 diabetes, Parkinson's disease, etc
|
- HY-106224A
-
|
Hypocretin-1 (human, rat, mouse) (TFA)
|
Orexin Receptor (OX Receptor)
|
Neurological Disease
|
|
Orexin A (human, rat, mouse) (Hypocretin-1 (human, rat, mouse)) TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A (human, rat, mouse) TFA binds and activates two types of G protein-coupled receptors, the orexin-1 receptor (OX1R) and the orexin-2 receptor (OX2R). Orexin A (human, rat, mouse) TFA has a role in the regulation of feeding behavior. Orexin A (human, rat, mouse) TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats .
|
- HY-P1556
-
|
|
PKG
|
Cardiovascular Disease
|
|
Vasonatrin Peptide (VNP) is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway .
|
- HY-P1556A
-
|
|
PKG
|
Metabolic Disease
|
|
Vasonatrin Peptide (VNP) TFA is a chimera of atrial natriuretic peptide (ANP) and C-type natriuretic peptide (CNP). Vasonatrin peptide TFA possesses the venodilating actions of CNP, the natriuretic actions of ANP, and unique arterial vasodilating actions not associated with either ANP or CNP. Vasonatrin Peptide TFA protects the diabetic heart against ischemia-reperfusion injury by inhibiting ER stress via the cGMP-PKG signaling pathway .
|
- HY-P3641A
-
|
|
GnRH Receptor
|
Neurological Disease
Metabolic Disease
|
|
Kisspeptin 13 TFA is the TFA salt form of Kisspeptin 13 (HY-P3641). Kisspeptin-13 TFA inhibits glucose-induced insulin secretion with an IC50 of 1.2 nM. Kisspeptin 13 TFA activates the hypothalamic-pituitary-adrenal (HPA) axis, causes hyperthermia, motor behavior and anxiety in rats. Kisspeptin 13 TFA interacts with α2-adrenergic and 5-HT2 serotonin receptors, exhibits antidepressant efficacy. Kisspeptin 13 TFA is an activator for GPR54 and GnRH receptor, which enhances memory and can be used in Alzheimer's disease research .
|
- HY-P5875A
-
|
|
Protease Activated Receptor (PAR)
|
Cardiovascular Disease
Inflammation/Immunology
|
|
P4pal10 TFA is the TFA salt form of P4pal10 (HY-P5875). P4pal10 TFA is an antagonist for protease-activated receptor 4 (PAR4). P4pal10 TFA inhibits the platelet aggregation, inhibits tissue factor (TF)-induced thrombin generation, and exhibits anticoagulant and antithrombotic activities. P4pal10 TFA reduces the oedema and the granulocyte infiltration induced by Carrageenan (HY-125474). P4pal10 TFA ameliorates the injury in rats myocardial ischemia/reperfusion (I/R) models .
|
- HY-P3206A
-
|
Thymulin acetate; Thymic factor acetate
|
ERK
|
Neurological Disease
Inflammation/Immunology
Endocrinology
|
|
Serum thymic factor acetate (Thymulin acetate) is the acetate salt form of Serum thymic factor (HY-P3206). Serum thymic factor acetate is a zinc-dependent immunomodulatory peptide hormone, which can be produced by the thymic epithelial cells. Serum thymic factor acetate stimulates the release of hormones from the pituitary gland, exhibits hypophysiotropic activity. Serum thymic factor acetate protects rats from Cephaloridine (HY-B2072)-induced nephrotoxicity by inhibiting ERK activation. Serum thymic factor acetate exhibits anti-diabetic, anti-inflammatory and analgesic effects. Serum thymic factor acetate can be used in research about endocrine, reproductive, neurodegenerative and inflammatory diseases .
|
- HY-P10301
-
|
|
Peptides
|
Cancer
|
|
CXCL9(74-103) is a derivative peptide of CXCL9 that has a high affinity for glycosaminoglycans (GAGs) and can bind to GAGs. CXCL9(74-103) possesses anti-angiogenic properties, capable of reducing EGF, VEGF165, and FGF-2-mediated angiogenesis processes in vitro, without exhibiting cytotoxicity .
|
- HY-P3801
-
|
DiMe-C7
|
Neurokinin Receptor
|
Others
Neurological Disease
Metabolic Disease
|
|
[Glp5,(Me)Phe8,Sar9] Substance P (5-11) (DiMe-C7) is a Substance P (HY-P0201) analogue that has approximately the same effects as Substance P (HY-P0201) on neurokinin 1 receptor (NK1R) in rat brain, but with a much longer duration of action. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) selectively activates dopamine metabolism in the mesencephalon and midbrain cortex of the rat brain. [Glp5,(Me)Phe8,Sar9] Substance P (5-11) also increases motor activity and induces recovery of addictive agent-seeking behavior in rats .
|
| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-145633
-
|
OPT 302; VGX-300
|
VEGFR
|
Cardiovascular Disease
|
|
Sozinibercept (OPT 302; VGX-300) is a soluble form of VEGFR-3, potently inhibits the activity of VEGF-C/D, which are the proangiogenic factors, inhibiting angiogenesis and vascular leakage. Sozinibercept also inhibits diabetic retinal edema in rats .
|
-
- HY-P990093
-
|
CM310
|
Interleukin Related
|
Inflammation/Immunology
|
|
Stapokibart (CM310) is a humanised monoclonal antibody targeting IL-4Rα and efficiently blocks the interaction of cytokines IL-4 and IL-13 with their co-receptor subunit IL-4Rα. Stapokibart has the capacity to interact with IL-4Rα in humans, cynomolgus monkeys, and rats .
|
-
- HY-P990679
-
|
|
Inhibitory Antibodies
|
Others
Cancer
|
|
Rat IgG2a kappa, Isotype Control is a monoclonal antibody derived from rats, representing the immunoglobulin G2a (IgG2a) subclass with a kappa light chain. Rat IgG2a kappa, Isotype Control exhibits high efficiency in inducing K cell mediated cytotoxicity. Rat IgG2a kappa, Isotype Control is utilized in research investigating the roles of different immunoglobulin subclasses in tumor immunology .
|
-
- HY-P99615
-
|
SB 209763; RSHZ19
|
RSV
|
Infection
|
|
Felvizumab (SB 209763) is a humanized IgG1κ monoclonal antibody directed to distinct neutralizing epitopes on the F glycoprotein of RSV .
|
| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
-
- HY-123298
-
-
-
- HY-B0747
-
-
-
- HY-B1331
-
|
Cyromazin; CGA-72662
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Endogenous Metabolite
Parasite
|
|
Cyromazine (CGA-72662) is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects. Cyromazine reduced the number of germ cells by interfering with the Ecdysone (HY-N0179) signaling pathway. Cyromazine induces renal toxicity attenuated and restored by green tea extract in rats .
|
-
-
- HY-W096159
-
-
-
- HY-W011873
-
-
-
- HY-113329
-
-
-
- HY-N4209
-
-
-
- HY-126758
-
|
|
Source classification
Artemisia sieversiana Ehrhart ex Willd.
Plants
Compositae
|
Apoptosis
Glutathione Peroxidase
|
|
Ludartin a sesquiterpene lactone, which can be isolated from the plant Artemisia carruthii Wood. Ludartin reduces the expression of myeloperoxidase and malondialdehyde, enhances the expression of glutathione and superoxide dismutase in spinal cord tissue. Ludartin inhibits neuronal apoptosis. Ludartin inhibits the upregulation of tumor necrosis factor-α, interleukin-1β, and interleukin-6. Ludartin improves the motor function of rats with spinal cord injury .
|
-
-
- HY-B1331R
-
|
|
Structural Classification
Natural Products
Source classification
Endogenous metabolite
|
Endogenous Metabolite
Parasite
|
|
Cyromazine (Standard) is the analytical standard of Cyromazine. This product is intended for research and analytical applications. Cyromazine (CGA-72662) is a triazine insect growth regulator used as an insecticide and an acaricide. It is a cyclopropyl derivative of melamine. Cyromazine works by affecting the nervous system of the immature larval stages of certain insects. Cyromazine reduced the number of germ cells by interfering with the Ecdysone (HY-N0179) signaling pathway. Cyromazine induces renal toxicity attenuated and restored by green tea extract in rats .
|
-
-
- HY-N1115
-
-
-
- HY-N11503
-
-
-
- HY-N13127
-
-
-
- HY-129208
-
-
-
- HY-N9226
-
-
-
- HY-N0300
-
-
-
- HY-B1247
-
-
-
- HY-N0300A
-
-
-
- HY-N11449
-
-
-
- HY-N7981
-
-
-
- HY-126848
-
-
-
- HY-N7515
-
-
-
- HY-P1742
-
-
-
- HY-W751152
-
-
-
- HY-N8931
-
|
Lithospermic acid monomethyl ester
|
Structural Classification
Labiatae
Source classification
Samanea saman (Jacq.) Merr.
Phenols
Polyphenols
Plants
|
Akt
|
|
Monomethyl lithospermate activates the PI3K/AKT pathway, which plays a protective role in nerve injury. Monomethyl lithospermate can improve the survival ability of SHSY-5Y cells, inhibit the breakdown of mitochondrial membrane potential (MMOP) and inhibit cell apoptosis. Monomethyl lithospermate also reduced the level of oxidative stress in the brain tissue of rats with middle artery occlusion (MCAO) and improved nerve damage in rats with ischemic stroke (IS) .
|
-
-
- HY-118383
-
-
-
- HY-127152
-
-
-
- HY-N9363
-
-
-
- HY-N6910
-
-
-
- HY-121401A
-
-
-
- HY-N0300R
-
-
-
- HY-107248
-
-
-
- HY-N0723
-
-
-
- HY-N2531
-
-
-
- HY-127166
-
-
-
- HY-N0691
-
-
-
- HY-75087
-
-
-
- HY-N2196
-
-
-
- HY-N9113
-
-
-
- HY-N2388
-
-
-
- HY-N3202
-
-
-
- HY-N2388R
-
|
|
Structural Classification
other families
Source classification
Coumarins
Phenylpropanoids
Plants
|
MMP
PPAR
Bacterial
|
|
Auraptene (Standard) is the analytical standard of Auraptene. This product is intended for research and analytical applications. Auraptene is an orally active geranyloxycoumarin that can be isolated from plants in the Brassicaceae family, antibacterial, anti-pathogen, antioxidant, anti-tumor, and neuroprotective effects. Auraptene plays an important role in the treatment of various chronic diseases such as hypertension and cystic fibrosis .
|
-
-
- HY-W012946
-
-
-
- HY-N10226
-
-
-
- HY-N4009
-
-
-
- HY-B0770
-
-
-
- HY-135319
-
-
-
- HY-N2086
-
-
-
- HY-N1131
-
-
-
- HY-N1131B
-
-
-
- HY-Z0478
-
-
- HY-N3015
-
-
- HY-N0495
-
-
- HY-N8196
-
-
- HY-D1056
-
-
- HY-N0723R
-
-
- HY-N0691R
-
-
- HY-119741
-
-
- HY-N0157
-
-
- HY-N2026
-
-
- HY-N0157A
-
-
- HY-N2026A
-
-
- HY-125540
-
-
- HY-N0264
-
|
Chuanxiongzine; Tetramethylpyrazine
|
Cardiovascular Disease
Structural Classification
Natural Products
Neurological Disease
Classification of Application Fields
Source classification
Metabolic Disease
Dicerothamnus rhinocerotis
Umbelliferae
Plants
Inflammation/Immunology
Disease Research Fields
|
Apoptosis
|
|
Ligustrazine (Chuanxiongzine), an alkylpyrazine isolated from Ligusticum chuanxiong Hort. (Chuan Xiong) , is present in french fries, bread, cooked meats, tea, cocoa, coffee, beer, spirits, peanuts, filberts, dairy products and soy products as fragrance and flavouring ingredienexhibits. Ligustrazine also has potential nootropic and anti-inflammatory activities in rats .
|
-
- HY-N6952
-
-
- HY-W012977
-
-
- HY-W012946R
-
-
- HY-121624
-
-
- HY-W027951
-
-
- HY-116807
-
-
- HY-N0495R
-
-
- HY-B0226
-
|
Nitrofural
|
Microorganisms
Source classification
|
Bacterial
Antibiotic
|
|
Nitrofurazone (Nitrofural) is a broad spectrum antibiotic that has oral activity. Nitrofurazone is a nitro-aromatic drug. Nitrofurazone is active against both Gram-positive and Gram-negative bacteria .
|
-
- HY-B0226R
-
|
|
Microorganisms
Source classification
|
Bacterial
Antibiotic
|
|
Nitrofurazone (Standard) is the analytical standard of Nitrofurazone. This product is intended for research and analytical applications. Nitrofurazone (Nitrofural) is a broad spectrum antibiotic that has oral activity. Nitrofurazone is a nitro-aromatic drug. Nitrofurazone is active against both Gram-positive and Gram-negative bacteria .
|
-
- HY-76006
-
-
- HY-N0157R
-
-
- HY-N2026R
-
-
- HY-129143
-
|
Dp3‐Sam chloride
|
Malvaceae
Structural Classification
Flavonoids
Hibiscus sabdariffa Linn.
Plants
Other Flavonoids
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Others
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Delphinidin-3-sambubioside (Dp3‐Sam) chloride is an anthocyanin that has orally active anti-inflammatory activity. Delphinidin-3-sambubioside chloride inhibits LPS-induced inflammatory factors release. Delphinidin-3-sambubioside chloride also alleviates hepatic lipid accumulation in HFD rats. Delphinidin-3-sambubioside chloride can be isolated from Hibiscus sabdariffa L. .
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- HY-N0264R
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Structural Classification
Natural Products
Source classification
Dicerothamnus rhinocerotis
Umbelliferae
Plants
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Apoptosis
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Ligustrazine (Standard) is the analytical standard of Ligustrazine. This product is intended for research and analytical applications. Ligustrazine (Chuanxiongzine), an alkylpyrazine isolated from Ligusticum chuanxiong Hort. (Chuan Xiong) , is present in french fries, bread, cooked meats, tea, cocoa, coffee, beer, spirits, peanuts, filberts, dairy products and soy products as fragrance and flavouring ingredienexhibits. Ligustrazine also has potential nootropic and anti-inflammatory activities in rats .
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- HY-N7697F
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- HY-N7860
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Structural Classification
Animals
Ketones, Aldehydes, Acids
Source classification
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Others
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Δ2-cis Eicosenoic acid is an α,β-unsaturated fatty acid that has been extracted from fresh water clams and purified. A related compound, 2-octadecenoic acid, has been shown to improve liver function and decrease blood sugar in streptozocin-induced diabetic rats. Δ2-cis Eicosenoic acid and its salts have potential medicinal use for treating diabetes and improving lipid metabolism.
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- HY-W015309
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- HY-N1964
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- HY-116807R
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Human Gut Microbiota Metabolites
Microorganisms
Source classification
Endogenous metabolite
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Reactive Oxygen Species
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Dihydrolipoic Acid (Standard) is the analytical standard of Dihydrolipoic Acid. This product is intended for research and analytical applications. Dihydrolipoic Acid (DHLA) is an excellent antioxidant capable of scavenging almost any oxygen-centered radical . Dihydrolipoic acid exhibits anti-inflammatory properties in various diseases. Dihydrolipoic Acid exerts a preventive effect via ERK/Nrf2/HO-1/ROS/NLRP3 pathway in LPS-induced sickness behavior rats. Dihydrolipoic Acid can be used for the reaserch of depression .
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- HY-B1350A
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- HY-W009732
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- HY-100978
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- HY-N12445
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- HY-N0378
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- HY-111827
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- HY-Y0946
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- HY-N0171B
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- HY-106353
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- HY-W015309R
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Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
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iGluR
Tyrosinase
c-Met/HGFR
Glutaminase
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Decanoic acid (Standard) is the analytical standard of Decanoic acid. This product is intended for research and analytical applications. Decanoic acid is a key component of the medium-chain triglyceride (MCT) found in coconut oil. Decanoic acid is a brain-penetrant and non-competitive inhibitor of AMPA receptor showing antiseizure activity in rats. Decanoic acid reduces tyrosinase activity and inhibits melanosome maturation. Decanoic acid suppresses the phosphorylation of c-Met and induced apoptosis in hepatocellular carcinoma (HCC) cells by inhibiting the expression of various oncogenic proteins, which is promising for research in the field of mTORC1 signaling, HCC and epilepsy .
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- HY-B1232R
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Structural Classification
Alkaloids
Source classification
Pyridine Alkaloids
Endogenous metabolite
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Endogenous Metabolite
Cytochrome P450
Autophagy
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Metyrapone (Standard) is the analytical standard of Metyrapone. This product is intended for research and analytical applications. Metyrapone (Su-4885) is a potent and orally active 11β-hydroxylase inhibitor and an autophagy activator, also inhibits the production of aldosterone. Metyrapone inhibits synthesis of endogenous adrenal corticosteroid, decreases glucocorticoid levels, and also affects behavior and emotion. In addition, Metyrapone increases the efficiency of autophagic process via downregulation of mTOR pathway, and interacts with Pseudomonas putida cytochrome P-450. Metyrapone can be used for researching Cushing's syndrome and depression .
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- HY-B1232
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- HY-B1232A
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- HY-59291
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- HY-N0194
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- HY-N1940
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- HY-N0807
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- HY-N0507
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Structural Classification
Simple Phenylpropanols
Rhodiola rosea Linn.
Crassulaceae
Source classification
Phenylpropanoids
Plants
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TNF Receptor
Interleukin Related
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Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
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- HY-N0194R
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Triterpenes
Structural Classification
Terpenoids
Source classification
Tagetes lucida Cav.
Umbelliferae
Plants
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Apoptosis
Parasite
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Asiatic acid (Standard) is the analytical standard of Asiatic acid. This product is intended for research and analytical applications. Asiatic acid, a pentacyclic triterpene found in Centella asiatica (Centella asiatica), has anticancer activity. Asiatic acid induces apoptosis in melanoma cells and has barrier protective effects on human aortic endothelial cells (HAEC). Asiatic acid also has anti-inflammatory activity and inhibits tumor necrosis factor (TNF)-α-induced endothelial barrier dysfunction. Asiatic acid also inhibits NLRP3 inflammasome activation and NF-κB pathway, effectively inhibits inflammation in rats, and has neuroprotective effects in rat spinal cord injury (SCI) model .
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- HY-N7690
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Structural Classification
Flavonoids
Classification of Application Fields
Flavones
Metabolic Disease
Plants
Disease Research Fields
Zingiberaceae
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Calcium Channel
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3,5,7,3’,4’-Pentamethoxyflavone is a Ca 2+ channel inhibitor. 3,5,7,3’,4’-Pentamethoxyflavone can protect DNA from oxidative damage. 3,5,7,3’,4’-Pentamethoxyflavone can induce relaxation of the human corpus cavernosum through calcium mobilization-related mechanisms. 3,5,7,3’,4’-Pentamethoxyflavone can promote the expression of eNOS and cystathionine gamma lyase CSE proteins in middle-aged male rats and regulate vascular function. 3,5,7,3’,4’-Pentamethoxyflavone can be used in research related to diabetes and cardiovascular diseases .
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- HY-N0108
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- HY-N0507R
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Structural Classification
Simple Phenylpropanols
Rhodiola rosea Linn.
Crassulaceae
Source classification
Phenylpropanoids
Plants
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TNF Receptor
Interleukin Related
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Rosavin (Standard) is the analytical standard of Rosavin. This product is intended for research and analytical applications. Rosavin, an orally bioactive phenylpropanoid from Rhodiola rosea L. (RRL), is an adaptogen that enhances the body’s response to environmental stress. Rosavin significantly influences bone tissue metabolism by inhibiting osteoclastogenesis and promoting osteoblast differentiation, also impacts various diseases, demonstrating antidepressant, adaptogenic, and anxiolytic effects in mouse models. Additionally, Rosavin improves survival, reducing intestinal damage in irradiated rats and Ischemia-reperfusion(I/R)-induced cerebral injury in vivo by regulating inflammation and oxidative stress, making it a promising candidate for research in radiation-induced intestinal injury, I/R-induced cerebral injury and osteoporosis .
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- HY-N2983
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- HY-W010201
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- HY-101392
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Harmane
1 Publications Verification
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Alkaloids
Structural Classification
other families
Source classification
Pyridine Alkaloids
Plants
Indole Alkaloids
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Imidazoline Receptor
Monoamine Oxidase
Adrenergic Receptor
nAChR
GABA Receptor
Opioid Receptor
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Harmane is an inhibitor that binds to benzodiazepine receptors (with an IC50 value of 7 μM), has an IC50 of 24 μM for muscarinic acetylcholine receptors (QNB), an IC50 of 2.8 μM for opioid receptors, and IC50 values of 163 and 101 μM for spironolactone and serotonin, respectively. Harmane is a selective monoamine oxidase inhibitor (with IC50 values of 0.5 μM for MAO A and 5 μM for MAO B). Harman inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing levodopa (L-DOPA)-induced toxicity in PC12 cells. Harmane lowers blood pressure in rats through the I1 imidazoline receptor (I1 receptor) and has antidepressant, anxiolytic, anticonvulsant, and analgesic effects. Harmane enhances the mutagenicity induced by 2-acetylaminofluorene (AAF) .
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- HY-W010201R
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- HY-N7140
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- HY-N6996
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- HY-N6996R
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- HY-B0328
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- HY-W017113
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Structural Classification
Natural Products
Classification of Application Fields
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
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Endogenous Metabolite
Aryl Hydrocarbon Receptor
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2-Mercaptobenzothiazole is an activator of the aryl hydrocarbon receptor (AhR) , inhibiting thyroid hormone synthesis and dopamine beta-hydroxylase activity . 2-Mercaptobenzothiazole promotes bladder cancer cell invasion by altering the conformation of the AhR ligand binding domain (LBD), activating AhR transcription, and upregulating the mRNA and protein expression of target genes CYP1A1 and CYP1B1 . 2-Mercaptobenzothiazole inhibits thyroid peroxidase (TPO) with an IC50 value of 11.5 μM, induces histological changes such as follicular cell hypertrophy in Xenopus laevis tadpoles, delaying metamorphosis . 2-Mercaptobenzothiazole increases chromosomal aberrations and sister chromatid exchanges (SCEs) in Chinese hamster ovary (CHO) cells, and enhances carcinogenicity in F344/N rats . 2-Mercaptobenzothiazole inhibits norepinephrine synthesis in mice and completely blocks the conversion of exogenous dopamine to norepinephrine in rat cardiomyocytes .
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- HY-14608R
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Structural Classification
Microorganisms
Source classification
Disease markers
Endocrine diseases
Amino acids
Nervous System Disorder
Endogenous metabolite
Cardiovascular System Disorder
Cancer
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Endogenous Metabolite
iGluR
Ferroptosis
Apoptosis
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L-Glutamic acid (Standard) is the analytical standard of L-Glutamic acid. This product is intended for research and analytical applications. L-Glutamic acid is an excitatory amino acid neurotransmitter that acts as an agonist for all subtypes of glutamate receptors (metabolic rhodophylline, NMDA, and AMPA). L-Glutamic acid has an agonist effect on the release of DA from dopaminergic nerve endings. L-Glutamic acid can be used in the study of neurological diseases .
IC50 & Target:DA .
In Vitro: L-Glutamic acid (120, 500, 750, 1000 mg/dL) can reduce the harmful effect of lithium on the embryonic development of Xenopus Xenopus .
L-Glutamic acid (2, 5, 10, 20 mM, 24-48 h) can induce neuroexcitotoxicity in neuroblastoma .
In Vivo: L-Glutamic acid (3 g/kg, subcutaneous injection) can promote excitotoxic degeneration of retinal ganglion cells in mice .
L-Glutamic acid (750 mg/kg, intraperitoneal injection) can reduce and inhibit oxidative stress induced by chlorpyrifos (CPF) in rats .
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- HY-N0124
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- HY-30004
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Structural Classification
Microorganisms
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
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Endogenous Metabolite
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1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
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- HY-N6792
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T-2 Mycotoxin
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Structural Classification
Microorganisms
Classification of Application Fields
Terpenoids
Sesquiterpenes
Source classification
Metabolic Disease
Disease Research Fields
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Apoptosis
DNA/RNA Synthesis
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T-2 Toxin (T-2 Mycotoxin) is a toxic trichothecene mycotoxin produced by various Fusarium species in feedstuffs and cereal grains, LD50 values of T-2 Toxin in mice and rats are 5.2 and 1.5 mg/kg BW a,respectively . T-2 Toxin (T-2 Mycotoxin) can be transformed into a variety of metabolite, the typical metabolites of T-2 toxin in animals are HT-2 toxin and T-2-triol, which are hydrolysates . T-2 Toxin (T-2 Mycotoxin) is an inhibitor of protein synthesis resulting from binding peptidyltransferase, which is an integral part of the 60s ribosomal subunit. T-2 Toxin (T-2 Mycotoxin) inhibits the synthesis of DNA and RNA, interferes with the metabolism of membrane phospholipids, and increases the level of liver lipid peroxides . T-2 Toxin (T-2 Mycotoxin) induces apoptosis in the immune system, gastrointestinal tissues, and fetal tissues .
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- HY-B0442C
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- HY-B0442R
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Structural Classification
Natural Products
Source classification
Endogenous metabolite
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Phosphodiesterase (PDE)
Endogenous Metabolite
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Vardenafil (Standard) is the analytical standard of Vardenafil. This product is intended for research and analytical applications. Vardenafil is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
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- HY-B0442
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- HY-B0442A
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- HY-B0442B
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- HY-Y0966R
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- HY-N0469R
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Structural Classification
Microorganisms
Source classification
Disease markers
Endocrine diseases
Amino acids
Nervous System Disorder
Endogenous metabolite
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Endogenous Metabolite
Virus Protease
HSV
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L-Lysine (Standard) is the analytical standard of L-Lysine. This product is intended for research and analytical applications. L-lysine is an essential amino acid for humans with orally activity. L-lysine can inhibit the occurrence of HSV infections and is used in herpes research. L-lysine increases calcium absorption, reduces diabetes-related diseases, improves gut health, and alleviates pancreatic inflammation. L-lysine can be used in research on metabolism, infection, and inflammation .
IC50 & Target:L-lysine (150 mg/kg) promotes, but not initiates, bladder cancer. The administration of L-lysine to rats submitted to colovesical cystoplasty accelerates the development of transitional metaplasia of the intestinal epithelium .
L-lysine (10 mg/kg) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity .
In Vivo:L-lysine (10?mg/kg, p.o., pre-treated or post-treated, administration duration 15 days) treatment attenuates pancreatic tissue injury induced by L-arginine by inhibiting the release of the inflammatory cytokine IL-6 and enhance antioxidant activity in acute pancreatitis mice model .
L-lysine (5 or 10?mg/kg, p.o., 45 days) ameliorates sepsis-induced acute lung injury in a lipopolysaccharide (HY-D1056)-induced mouse model .
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| Cat. No. |
Product Name |
Chemical Structure |
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- HY-135761S
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Penconazole-d7 is the deuterium labeled Penconazole[1]. Penconazole is a typical triazole fungicide, and mainly applied on apples, grapes, and vegetables to control powdery mildew. Penconazole inhibits sterol biosynthesis in fungi. Penconazole decrease AChE activity in the cerebrum and cerebellum of rats[2][3].
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- HY-B0476S
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Phenacetin-d5 is the deuterium labeled Phenacetin. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[1][2][3].
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- HY-N2026S1
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Propylparaben-d4 is the deuterium labeled Propylparaben[1]. Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats[2][3][4].
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- HY-B0476S1
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Phenacetin- 13C is the 13C labeled Phenacetin[1]. Phenacetin (Acetophenetidin) is a non-opioid analgesic/antipyretic agent. Phenacetin is a selective COX-3 inhibitor. Phenacetin is used as probe of cytochrome P450 enzymes CYP1A2 in human liver microsomes and in rats[2][3][4].
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- HY-B1984S
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p,p'-DDD-d8 is the deuterium labeled p,p'-DDD[1]. p,p'-DDD is a major metabolite of p,p'-DDT. p,p'-DDD occurs in the feces and livers of rats, that are given p,p'-DDT by stomach tube, but not of rats injected intraperitoneally with p,p'-DDT[2][3].
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- HY-B1448AS
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(Rac)-Benidipine-d7 is the deuterium labeled Benidipine[1]. Benidipine is a potent and orally active calcium channel antagonist[2]. Benidipine shows anti-apoptosis effects in ischaemic/reperfused myocardial cells[3]. Benidipine increases the activity of endothelial cell-type nitric oxide synthase and improves coronary circulation in hypertensive rats[4].
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- HY-W012946S
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2-Furoic acid-d3 is the deuterium labeled 2-Furoic acid[1]. 2-Furoic acid (Furan-2-carboxylic acid) is an organic compound produced through furfural oxidation[2]. 2-Furoic acid exhibits hypolipidemic effet, lowers both serum cholesterol and serum triglyceride levels in rats[3].
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- HY-W011873S
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Palmitoleic acid-d14 is the deuterium labeled Palmitoleic acid. Palmitoleic acid, a composition of fatty acid, is implicated in the prevention of death from cerebrovascular disorders in SHRSP rats.
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- HY-W011873S1
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Palmitoleic acid-d13 is the deuterium labeled Palmitoleic acid. Palmitoleic acid, a composition of fatty acid, is implicated in the prevention of death from cerebrovascular disorders in SHRSP rats.
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- HY-W011873S2
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Palmitoleic acid- 13C16 is the 13C labeled Palmitoleic acid. Palmitoleic acid, a composition of fatty acid, is implicated in the prevention of death from cerebrovascular disorders in SHRSP rats.
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- HY-N0157S1
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Orotic acid- 13C, 15N2 (monohydrate) is the 13C and 15N labeled Orotic acid[1]. Orotic acid (6-Carboxyuracil), a precursor in biosynthesis of pyrimidine nucleotides and RNA, is released from the mitochondrial dihydroorotate dehydrogenase (DHODH) for conversion to UMP by the cytoplasmic UMP synthase enzyme. Orotic acid is a marker for measurement in routine newborn screening for urea cycle disorders. Orotic acid can induce hepatic steatosis and hepatomegaly in rats[2][3][4].
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- HY-B1971S
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Deltamethrin-d5 is the deuterium labeled Deltamethrin. Deltamethrin (Decamethrin), a neurotoxic pyrethroid insecticide, produces a reversible sequence of motor symptoms in rats involving hind limb rigidity and choreoathetosis[1][2].
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- HY-B0099S
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Edaravone-d5 is a deuterium labeled Edaravone. Edaravone is a strong novel free radical scavenger, and inhibits MMP-9-related brain hemorrhage in rats treated with tissue plasminogen activator[1][2][3][4].
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- HY-N1131S
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Triacetonamine-d17 (2,2,6,6-Tetramethyl-4-piperidone-d17) is the deuterium labeled Triacetonamine. Triacetonamine has oral activity and can induce acute liver failure (ALF) in rats .
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- HY-A0039S1
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Eletriptan-d5 is the deuterium labeled Eletriptan[1]. Eletriptan (UK-116044) is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan can be used for researching migraine[2].
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- HY-N2026S
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Propylparaben-d7 (Propyl parahydroxybenzoate-d7)is the deuterium labeledPropylparaben(HY-N2026) . Propylparaben (Propyl parahydroxybenzoate) is an antimicrobial preservative which can be produced naturally by plants and bacteria. Propylparaben is prevalently used in cosmetics, pharmaceuticals, and foods. Propylparaben disrupts antral follicle growth and steroidogenic function by altering the cell-cycle, apoptosis, and steroidogenesis pathways. Propylparaben also decreases sperm number and motile activity in rats .
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- HY-A0039S2
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Eletriptan-d5 (hydrochloride) is the deuterium labeled Eletriptan hydrochloride[1]. Eletriptan (UK-116044) hydrochloride is a highly selective and orally active serotonin 5-HT1B and 5-HT1D receptor agonist, with pKi values of 8.0 and 8.9, respectively. Eletriptan hydrochloride has inhibitory effects on markers of neurogenic inflammation in rats. Eletriptan hydrochloride can be used for researching migraine[2].
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- HY-76569S1
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(R)-Hydroxytolterodine-d14 is deuterated labeled Desfesoterodine (HY-76569). Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively . Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053) . Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats .
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- HY-B0442AS
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Vardenafil-d5 hydrochloride is deuterated labeled Vardenafil hydrochloride (HY-B0442A). Vardenafil hydrochloride is a selective and orally active inhibitor of phosphodiesterase-5 (PDE5), with an IC50 of 0.7 nM. Vardenafil hydrochloride shows inhibitory towards PDE1, PDE6 with IC50s of 180 nM, and 11 nM, while IC50s are >1000 nM for PDE3 and PDE4 . Vardenafil hydrochloride competitively inhibits cyclic guanosine monophosphate (cGMP) hydrolysis and thus increases cGMP levels . Vardenafil hydrochloride can be used for the research of erectile dysfunction, hepatitis, diabetes [1]-[6].
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| Cat. No. |
Product Name |
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Classification |
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- HY-120276
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GR3027
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Alkynes
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Golexanolone is a GABAA receptor modulating steroid antagonist. Golexanolone reduces peripheral inflammation and neuroinflammation and improves cognitive and motor function in hyperammonemic rats .
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- HY-121528
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Nylestriol; EE3CPE
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Alkynes
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Nilestriol is a estriol derivative, which inhibits osteoporosis on ovariectomized rats or postmenopausal women .
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- HY-118950
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Alkynes
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J 628 is an estrogen derivative used to study antifertility effects after sexual intercourse in mice, rats, and rabbits .
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- HY-117076
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R 2858
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Alkynes
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Moxestrol (R 2858) is a synthetic estrogen, which effectively induces proliferation of pituitary cells even in very young rats, without without affecting hormone release .
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- HY-120329
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Alkynes
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Lu 26-046 is the agonist for muscarinic M1 receptor and M2 receptor and a weak antagonist for M3 receptor, with Ki of 0.51, 26 and 5 nM, respectively. Lu 26-046 exhibits specific stimulus property, that can be recognized by rats .
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| Cat. No. |
Product Name |
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Classification |
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- HY-152927
-
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Release-retarding Agents
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Hydroxypropylmethyl cellulose acetate succinate (Mw: 20-100k Da) is a cosolvent for preparing SDDs of low-solubility agents. Hydroxypropylmethyl cellulose acetate succinate (Mw: 20-100k Da) exhibits no acute/subchronic/chronic toxicity in rats, with oral activity and LD50 >2.5 g/kg .
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- HY-153808B
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Adjuvant
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Complete Freund's adjuvant (CFA, 1 mg/ml) is an immunoadjuvant emulsified with antigen that can enhance an animal's immune response to an antigen. Complete Freund's adjuvant (CFA, 1 mg/ml) is also an inducer of the Th1 immune response and a ligand of TLRs. Complete Freund's adjuvant (CFA, 1 mg/ml) contains heat-killed inactive tuberculosis bacilli and consists of a paraffin oil-in-water emulsion. Complete Freund's adjuvant (CFA, 1 mg/ml) stimulates a strong and durable immune response and can be used to induce rheumatoid arthritis in rats, and more .
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- HY-Y0966
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Glycine
5 Publications Verification
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Fillers
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Glycine is an inhibitory neurotransmitter in the CNS and also acts as a co-agonist along with glutamate, facilitating an excitatory potential at the glutaminergic N-methyl-D-aspartic acid (NMDA) receptors. Glycine is orally active. Glycine can be used to study cell protection, cancer, neurological diseases, and angiogenesis .
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- HY-W250580
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Others
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Dimethicone is an orally active biochemical assay reagents consisting of a fully methylated linear siloxane polymer whose ends are blocked by trimethylsiloxane units. Dimethicone can lubricate hair and physically block the respiratory system of lice to remove lice. Dimethicone has potential applications in cosmetics and daily cleaning products .
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- HY-150214
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CpG ODNs
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ODN MT01 was designed based on human mitochondrial DNA sequences, which is an inhibitory ODN that promotes osteocyte differentiation. ODN MT01 could promote osteoblast maturation and activation in rats, reduce rat alveolar bone absorption caused by periodontitis, regulate the expression levels of osteogenesis-related factors.
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- HY-150214A
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CpG ODNs
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ODN MT01 sodium was designed based on human mitochondrial DNA sequences, which is an inhibitory ODN that promotes osteocyte differentiation. ODN MT01 sodium could promote osteoblast maturation and activation in rats, reduce rat alveolar bone absorption caused by periodontitis, regulate the expression levels of osteogenesis-related factors.
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