Search Result
Results for "
rat cortex
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-101333
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(RS)-CPPG
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mGluR
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Neurological Disease
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CPPG ((RS)-CPPG) is a potent group II/III mGlu receptors antagonist. CPPG exhibits some selectivity (approximately 20 fold) for group III (IC50=2.2 nM) over group II (IC50=46.2 nM) mGlu receptors in the rat cerebral cortex. CPPG has weak effects at group I mGlu receptors .
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- HY-P1212
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CST-14 (mouse, rat)
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Somatostatin Receptor
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Neurological Disease
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Cortistatin 14, mouse, rat (CST-14, human, rat), a neuropeptide with neuronal depressant and sleep modulating properties, can bind to all five cloned somatostatin receptors (SSTRs) and ghrelin receptor to exert its biological activities and co-exists with GABA within the cortex and hippocampus .
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- HY-103509
-
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GABA Receptor
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Neurological Disease
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NNC 05-2090 hydrochloride is a GABA uptake inhibitor and inhibitor of the β-GABA transporter (BGT-1) (IC50< /sub>: 10.6 μM). NNC 05-2090 hydrochloride also inhibits mGAT2 with a Ki value of 1.4 μM. NNC 05-2090 has anticonvulsant activity and can be used in the study of epilepsy and neurological diseases .
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- HY-121186
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- HY-107563
-
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Histamine Receptor
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Inflammation/Immunology
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ROS 234 is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 diaplays poor central access .
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- HY-107563A
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Histamine Receptor
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Inflammation/Immunology
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ROS 234 dioxalate is a potent H3 antagonist, with a pKB of 9.46 for Guinea-pig ileum H3-receptor, a pKi of 8.90 for Rat cerebral cortex H3-receptor, and a ED50 of 19.12 mg/kg (ip) in ex vivo of Rat cerebral cortex. ROS 234 dioxalate diaplays poor central access .
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- HY-106874B
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rel-RS-15385-197
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Adrenergic Receptor
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Neurological Disease
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rel-Delequamine (rel-RS-15385-197) is an orally active, brain-penetrant, potent and selective M2-adrenoceptor antagonist and α2-adrenoceptor antagonist. rel-Delequamine has a pKi of 9.45 for α2-adrenoceptors in the rat cortex. rel-Delequamine augments K +-evoked release of noradrenaline with an EC50 of 1 nM .
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- HY-P1588
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- HY-W203728
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- HY-107562
-
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Histamine Receptor
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Neurological Disease
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JNJ-10181457 is a neutral, potent, brain-penetrant and selective non-imidazole H3 antagonist which increases NE and ACh concentrations in rat frontal cortex. JNJ-10181457 can be used for neurological research .
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- HY-12959A
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BAY x 3702
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5-HT Receptor
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Neurological Disease
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Repinotan hydrochloride (BAY x 3702) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus Repinotan hydrochloride has a weak affinity for other related receptors. Repinotan hydrochloride has pronounced neuroprotective effects .
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- HY-12959
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BAY x 3702 free base
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5-HT Receptor
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Neurological Disease
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Repinotan (BAY x 3702 free base) is a potent, selective, brain-penetrant and orally active 5-HT1A receptor agonist, with Ki values of 0.19 nM (calf hippocampus), 0.25 nM (rat and human cortex), and 0.59 nM (rat hippocampus). Repinotan has a weak affinity for other related receptors. Repinotan has pronounced neuroprotective effects .
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- HY-160932
-
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Adrenergic Receptor
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Endocrinology
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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 .
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- HY-100481
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RPR101048
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Cholecystokinin Receptor
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Neurological Disease
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RP 72540 is a selective CCK-B receptor antagonist, with IC50 values of 2.4, 1.2, and 3.8 nM for CCK-B receptors in the guinea pig cerebral cortex, rat cerebral cortex, and mouse brain, respectively. RP 72540 effectively inhibits CCK-8-induced neuronal firing and dose-dependently inhibits gastric acid secretion, making it potentially valuable in studies of acid secretion. RP 72540 is an important tool for investigating the physiological functions of CCK B receptors .
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- HY-126862
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mAChR
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Others
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AQ-RA 721 is a muscarinic receptor antagonist with differential affinity for the m4 and M2 sites, which can be used to characterize muscarinic receptor subtypes. Other muscarinic receptor antagonists have differential affinity for the M1 (rat cerebral cortex), M2 (rat heart), M3 (rat submandibular gland), m4 (receptor expressed in Chinese hamster ovary cells transfected with CHO), and guinea pig uterine smooth muscle at the muscarinic binding site .
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- HY-119409
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- HY-121186R
-
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Adrenergic Receptor
Calcium Channel
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Neurological Disease
Metabolic Disease
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Bevantolol (hydrochloride) (Standard) is the analytical standard of Bevantolol (hydrochloride). This product is intended for research and analytical applications. Bevantolol hydrochloride is a selective β1 and α1-adrenergic receptor antagonist with pKi values of 7.83, 6.9 in rat cerebral cortex, respectively. Bevantolol hydrochloride is a potent Ca 2+ antagonist .
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- HY-113149
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Endogenous Metabolite
Reactive Oxygen Species
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Inflammation/Immunology
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Argininosuccinic acid participates in the fourth step of the urea cycle, with being cleaved to arginine and fumaric acid by argininosuccinic acid lyase (ASL). Argininosuccinic acid reduces reduced glutathione (GSH) level, and increases the production of reactive oxygen species in cerebral cortex and striatum. Argininosuccinic acid causes lipid peroxidation and protein oxidation, and induces oxidative stress in the developing rat brain .
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- HY-18138
-
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5-HT Receptor
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Neurological Disease
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PF-03382792 is a potent 5-HT4 partial agonist with a Ki of 2.7 nM and an EC50 of 0.9 nM for 5-HT4d. PF-03382792 can penetrate the brain. PF-03382792 produces moderate increases in cortical Ach in the rat prefrontal cortex .
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- HY-101075
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Phosphatase
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Others
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L-690330 is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 exhibits 10-fold more sensitive than mouse and rat IMPase .
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- HY-101075A
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Phosphatase
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Others
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L-690330 hydrate is a competitive inhibitor of inositol monophosphatase (IMPase) with Kis of 0.27 and 0.19 μM for recombinant human and bovine IMPase, 0.30 and 0.42 μM for human and bovine frontal cortex IMPase, respectively. L-690330 hydrate exhibits 10-fold more sensitive than mouse and rat IMPase .
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- HY-103133
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5-HT Receptor
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Neurological Disease
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WAY 208466 dihydrochloride is a potent and selective 5-HT6 receptor agonist (EC50=7.3 nM for the human 5-HT6 receptor). WAY-208466 dihydrochloride elevates cortical GABA levels in rat frontal cortex . WAY 208466 dihydrochloride exhibits antidepressant and anxiolytic-like effects .
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- HY-113149A
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Endogenous Metabolite
Reactive Oxygen Species
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Inflammation/Immunology
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Argininosuccinic acid disodium participates in the fourth step of the urea cycle and is cleaved into arginine and fumarate by argininosuccinate lyase (ASL). Argininosuccinic acid disodium reduces reduced glutathione (GSH) concentrations and increases reactive oxygen species production in the cerebral cortex and striatum. Argininosuccinic acid disodium causes lipid peroxidation and protein oxidation and also induces oxidative stress in the developing rat brain .
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- HY-117839
-
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Cholecystokinin Receptor
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Neurological Disease
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PD-135666 is a dipeptide inhibitor of cholecystokinin B (CCK B) receptors, binding to CCK B receptors in mouse cerebral cortex with IC50 of 0.1 nM. Its enantiomer, PD-140548, preferentially binds to CCK A receptors with IC50 of 2.8 nM in rat pancreas. PD-135666 exhibits anxiolytic effects in animal models .
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- HY-170409
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Trk Receptor
Apoptosis
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Neurological Disease
Inflammation/Immunology
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BNN27 is the agonist for TrkA receptor and p75NTR receptor, that exhibits neurotrophic and anti-apoptotic effects. BNN27 increases the levels of glutamate, GABA, and glutamine in the rat hippocampus and prefrontal cortex, improves glutamate turnover. BNN27 exhibits neuroprotective efficacy in mouse amyotrophic lateral sclerosis (ALS) model, exhibits anti-inflammatory efficacy in experimental autoimmune encephalomyelitis (EAE) model, exhibits retinal protective efficacy in rat diabete models. BNN27 is blood-brain barrier penetrable .
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- HY-114753
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CR-2249; XY-2401
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iGluR
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Neurological Disease
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Neboglamine (CR-2249; XY-2401) is a modulator for N-methyl-D-aspartate (NMDA) receptor. Neboglamine increases the levels of fos-like immunoreactivity (FLI)-positive cells in the prefrontal cortex, nucleus accumbens, and lateral septal nucleus in rat models, .restores NMDA (HY-17551) -mediated neurotransmitter release, and inhibits phencyclidine-induced hyperlocomotion .
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- HY-11051
-
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Opioid Receptor
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Inflammation/Immunology
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JNJ-20788560 is a selective and orally active delta opioid receptor agonist with an affinity of 2.0 nM for DOR (rat brain cortex binding assay). JNJ-20788560 also is a potent and efficacious antihyperalgesic agent that does not produce respiratory depression, pharmacologic tolerance, or physical dependence. JNJ-20788560 can be used for the research of the relief of inflammatory hyperalgesia .
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- HY-18730
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W1400
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NO Synthase
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a Kd value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation .
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- HY-W795507
-
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Adrenergic Receptor
5-HT Receptor
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Neurological Disease
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Cyanopindolol is an β3-adrenoceptor antagonist. Cyanopindolol is a potent and selective antagonist at the presynaptic serotonin autoreceptor in the rat brain cortex. Cyanopindolol has binding affinity for 5-HT1A and 5-HT1B receptor (Ki: 2.1 and 3 nM respectively) .
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- HY-116062
-
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Monoamine Transporter
Dopamine Transporter
Adrenergic Receptor
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Others
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JNJ-7925476 (hydrochloride) is a triple monoamine uptake inhibitor with the ability to regulate neurotransmitter levels and antidepressant activity. JNJ-7925476 (hydrochloride) can be rapidly absorbed into the plasma in rats, with a higher concentration in the brain than in plasma. It can induce an increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibits antidepressant activity in the mouse tail suspension test.
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- HY-105115
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ZK 112119
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GABA Receptor
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Neurological Disease
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Abecarnil (ZK 112119) is a ligand or a partial agonist for benzodiazepine (BZ) receptor. Abecarnil possesses anxiolytic and anticonvulsant properties. Abecarnil can act as a positive allosteric modulator of GABAA receptor. Abecarnil inhibits the binding of the BZ [3H]lormetazepam to rat cerebral cortex membranes, with an IC50 of 0.82 nM. Abecarnil can be used for epilepsy research .
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- HY-111066
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Dopamine Receptor
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Others
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JNJ-37822681 is a fast dissociating D2 antagonist with activity in inhibiting schizophrenia. JNJ-37822681 has high specificity for D2 receptors and is effective in animal models, inducing increased levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex, and exhibiting antidepressant activity in the mouse tail suspension test, while having a good brain distribution and lower prolactin release.
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- HY-10711A
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(R)-NFPS hydrochloride
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GlyT
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Neurological Disease
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ALX-5407 ((R)-NFPS) hydrochloride is a selective and orally active glycine transporter GlyT1 inhibitor with an IC50 value of 3 nM. ALX-5407 hydrochloride can be used the research of N-methyl-D-aspartate-receptor function and schizophrenia .
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- HY-168859
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JNK
GSK-3
Amyloid-β
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Neurological Disease
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JNK3 inhibitor-9 (Compound 24a) is a potent, selective and BBB-permeable JNK3 inhibitor with an IC50 value of 12 nM. JNK3 inhibitor-9 also potently inhibits GSK3α/β (IC50s: 14 and 35 nM, respectively) involved in Tau phosphorylation. JNK3 inhibitor-9 reduces c-Jun and APP phosphorylation. JNK3 inhibitor-9 protects neurons from Aβ1-42 toxicity .
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- HY-17550
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DM-235
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iGluR
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Neurological Disease
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Sunifiram (DM-235) is an ampakine-like compound and an agonist of AMPA receptor with oral activity. Sunifiram can increase the release of acetylcholine in the rat cerebral cortex and exhibits potent cognitive enhancement effects with better nootropic activity compared to piracetam (HY-B0585). Sunifiram is promising for research in neurodegenerative diseases such as mild cognitive impairment (MCI) and Alzheimer's disease (AD) .
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- HY-P3883
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- HY-18731
-
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NO Synthase
Apoptosis
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Cardiovascular Disease
Inflammation/Immunology
Cancer
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1400W dihydrochloride is the dihydrochloride form of 1400W (HY-18730). 1400W is a slow, tight binding, and highly selective inducible nitric-oxide synthase (iNOS) inhibitor, with a Kd value ≤ 7 nM. 1400W inhibits iNOS induction in microglial cells, and reduces generation of NO, thereby mitigating oxidative stress and neuronal cell apoptosis in the rat cerebral cortex, and improving the spatial memory dysfunction caused by acute hypobaric hypoxia-reoxygenation .
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- HY-59201A
-
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nAChR
5-HT Receptor
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Neurological Disease
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A-582941 dihydrochloride is a potent, selective and brain-penetrant partial agonist of α7 nAChR, with Kis of 10.8 and 16.7 nM in rat brain membranes and human frontal cortex, respectively. A-582941 dihydrochloride also binds to human 5-HT3 receptor with a Ki of 150 nM. A-582941 has the potential for cognitive deficits associated with various neurodegenerative and psychiatric disorders research .
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- HY-19651B
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TAK-147 fumarate
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Cholinesterase (ChE)
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Neurological Disease
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Zanapezil (TAK-147) fumarate is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil fumarate shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil fumarate shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil fumarate can be used for the research of early stages of Alzheimer's disease (AD) .
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- HY-19651A
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TAK-147
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Cholinesterase (ChE)
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Neurological Disease
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Zanapezil (TAK-147) is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil can be used for the research of early stages of Alzheimer's disease (AD) .
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- HY-106874
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RS-15385-197
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Adrenergic Receptor
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Neurological Disease
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Delequamine (RS-15385-197) is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine can be used for the study of erectile dysfunction .
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- HY-106874A
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RS-15385-197 hydrochloride
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Adrenergic Receptor
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Neurological Disease
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Delequamine (RS-15385-197) hydrochloride is an orally active and selective α2-adrenergic receptor antagonist with a pKi of 9.5 for α2-adrenoceptors in rat cortex. Delequamine hydrochloride shows >1000 fold selectivity against 5-HT1A receptors and α1-adrenoceptors. Delequamine hydrochloride can be used for the study of erectile dysfunction .
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- HY-129245
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Hoe 175
|
Endogenous Metabolite
|
Neurological Disease
|
Razobazam (Hoe 175) is a benzodiazepine derivative with cognitive activity. Razobazam has been shown to improve learning performance in socially deprived rats. Razobazam increased avoidance scores by 18% after training. Razobazam caused significant changes in the optical density of certain areas of the rat brain, including a 22% decrease in the lateral habenula and a 25% increase in the ventral tegmental area. Razobazam also caused a 13% increase in optical density in the prefrontal cortex of rats .
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- HY-19651
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TAK-147 free base
|
Cholinesterase (ChE)
|
Neurological Disease
|
Zanapezil (TAK-147) free base is a potent, reversible and selective acetylcholine esterase (AChE) inhibitor. Zanapezil free base shows a potent and reversible inhibition of AChE activity in homogenates of the rat cerebral cortex (IC50=51.2 nM). Zanapezil free base shows a moderate inhibition of muscarinic M1 and M2 receptor binding with Ki values of 234 and 340 nM, respectively. Zanapezil free base can be used for the research of early stages of Alzheimer's disease (AD) .
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- HY-17550R
-
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iGluR
|
Neurological Disease
|
Sunifiram (Standard) is the analytical standard of Sunifiram. This product is intended for research and analytical applications. Sunifiram (DM-235) is an ampakine-like compound and an agonist of AMPA receptor with oral activity. Sunifiram can increase the release of acetylcholine in the rat cerebral cortex and exhibits potent cognitive enhancement effects with better nootropic activity compared to piracetam (HY-B0585). Sunifiram is promising for research in neurodegenerative diseases such as mild cognitive impairment (MCI) and Alzheimer's disease (AD) .
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- HY-101046
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Quipazine dimaleate
|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
Quipazine dimaleate is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine dimaleate shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine dimaleate behaves as a 5-HT3R antagonist in peripheral models. Quipazine dimaleate can be used for neurological disease research .
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- HY-W028142
-
|
5-HT Receptor
SARS-CoV
|
Neurological Disease
|
Quipazine is a 5-HT agonist with a Ki value of 1.4 nM for displaces [3H]GR65630 from 5-HT3R in rat. Quipazine shows antiviral activity against SARS-CoV-2 with an EC50 of 31.64 μM. Quipazine behaves as a 5-HT3R agonist in peripheral models. Quipazine can be used for neurological disease research .
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-
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- HY-116062A
-
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Histone Methyltransferase
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Neurological Disease
|
JNJ-7925476 is a triple reuptake inhibitor that selectively and potently inhibits the activity of the serotonin transporter (SERT), norepinephrine transporter (NET), and dopamine transporter (DAT). JNJ-7925476 is rapidly absorbed into the blood and its concentration in the brain is 7-fold higher than that in plasma. The occupancy ED(50) values of JNJ-7925476 for SERT, NET, and DAT in the rat brain are 0.18, 0.09, and 2.4 mg/kg, respectively. JNJ-7925476 rapidly induces a significant increase in the levels of extracellular serotonin, dopamine, and norepinephrine in the rat cerebral cortex in a dose-dependent manner. JNJ-7925476 exhibits potent antidepressant-like activity in the mouse tail suspension test. These results suggest that JNJ-7925476 has in vivo efficacy in biochemical and behavioral models of depression .
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- HY-P3801
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DiMe-C7
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Neurokinin Receptor
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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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- HY-135115
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3,4-DHPEA-EA
|
α-synuclein
HDAC
Adrenergic Receptor
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Inflammation/Immunology
|
Oleuropein Aglycone (3,4-DHPEA-EA) is a polyphenol and the aglycone form of oleuropein (HY-N0292), formed by enzymatic, acidic or acetylated hydrolysis of oleuropein. Dietary intake of oleuropein Aglycone (50 mg/kg diet) increases the number of neuronal autophagic vesicles, reverses cognitive deficits in the TgCRND8 transgenic mouse model of Alzheimer's disease, and reduces the levels of histone deacetylase 2 (HDAC2) in the cortex and hippocampus. Oleuropein Aglycone increases urinary norepinephrine, interscapular brown adipose tissue epinephrine, and UCP1 protein levels, and reduced plasma leptin levels and total abdominal adipose tissue weight in a rat model of high-fat diet-induced obesity. Oleuropein Aglycone also reduced lung neutrophil infiltration, lipid peroxidation, and IL-1β levels in a mouse model of carrageenan-induced pleurisy.
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- HY-136693
-
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Adrenergic Receptor
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Neurological Disease
|
L-654284 is an α2-adrenergic receptor antagonist with significant selectivity. L-654284 competes with the binding of 3H-clonidine and 3H-rauwolscine in vitro and shows Ki values of 0.8 nM and 1.1 nM, respectively. L-654284 can block the protrusion effect of clonidine in isolated vas deferens in rats, with a pA2 value of 9.1. L-654284 exhibits remarkable selectivity for α2 and α1 adrenergic receptors, and exhibits a Ki of 110 nM in inhibiting 3H-prazosin binding. L-654284 can significantly increase the turnover rate of norepinephrine in rat cerebral cortex in vivo, showing α2-adrenergic receptor blocking activity in the central nervous system .
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Cat. No. |
Product Name |
Type |
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- HY-W203728
-
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Microbial Culture
|
L-β-Imidazolelactic acid is a histidine derivative and an oxidizing agent that can trigger antioxidant effects in the brain cortex of rats .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P1212
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CST-14 (mouse, rat)
|
Somatostatin Receptor
|
Neurological Disease
|
Cortistatin 14, mouse, rat (CST-14, human, rat), a neuropeptide with neuronal depressant and sleep modulating properties, can bind to all five cloned somatostatin receptors (SSTRs) and ghrelin receptor to exert its biological activities and co-exists with GABA within the cortex and hippocampus .
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- HY-P3801
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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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- HY-P1588
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- HY-P3883
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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