Search Result
Results for "
Sprague-Dawley rat
" in MedChemExpress (MCE) Product Catalog:
1
Biochemical Assay Reagents
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-121123
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2-Aminoadamantane-2-carboxylic acid
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Aminopeptidase
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Cancer
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Adamantanine (2-Aminoadamantane-2-carboxylic acid) inhibits the transport of methionine (Ki is 0.76 mM) and leucine into Ehrlich ascites carcinoma cells. Adamantanine inhibits proliferation of P388 lymphocytic leukemia cells with an IC50 of >1 mM. Adamantanine inhibits the leucine aminopeptidase with an I/S0.5 of 10.5 .
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- HY-10704
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- HY-N11925
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Others
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Cardiovascular Disease
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(+)-Osbeckic acid is a vasorelaxatant that can be isolated from Tartary Buckwheat. (+)-Osbeckic acid has a potent vasorelaxant effect in Sprague-Dawley rat thoracic aorta rings with an EC50 of 887 μM .
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- HY-P5130
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Endothelin Receptor
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Cardiovascular Disease
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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 .
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- HY-N15252
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VEGFR
ERK
Akt
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Cardiovascular Disease
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Eutypenes I (Compound 9) inhibits the secretion of VEGF-A, inhibits the activation of VEGFR and the downstream Erk/Akt signaling pathway. Eutypenes I inhibits the migration of cell HMEC-1, and exhibits anti-angiogenic activity in Sprague-Dawley’s rat models .
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- HY-151360
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Sodium Channel
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Metabolic Disease
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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 .
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- HY-N2196
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Others
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Inflammation/Immunology
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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 .
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- HY-117443
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Guanylate Cyclase
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Cardiovascular Disease
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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 .
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- HY-127125
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COX
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Inflammation/Immunology
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Diclofenac ethyl ester is the prodrug of Diclofenac (HY-15036), that is encapsulated in polymer micelles in vitro, and released with prolonged circulation time and reduced drug concentrations in the heart and kidneys in vivo .
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- HY-172147
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Somatostatin Receptor
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Neurological Disease
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SSTR4 agonist 5 (Compound 5) is the orally active agonist for somatostatin receptor 4 (SSTR4) with an EC50 of 0.228 nM. SSTR4 agonist 5 exhibits good stability in human/rat liver microsomes. SSTR4 agonist 5 inhibits mechanical hyperalgesia in rat models .
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- HY-P5875A
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Protease Activated Receptor (PAR)
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Cardiovascular Disease
Inflammation/Immunology
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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-N13714
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- HY-50692
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LPL Receptor
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Inflammation/Immunology
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CAY10734 is the agonist for sphingosine-1-phosphate receptor 1 (S1P1) with an IC50 of 1.3 nM. CAY10734 promotes the recirculation of peripheral blood lymphocytes, and is a potential immunosuppressant .
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- HY-P1134
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5-HT Receptor
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Neurological Disease
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Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the 5-HT1A receptor in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks .
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- HY-169986S
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JAK
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Inflammation/Immunology
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TyK2-IN-21-d3 (Compound 3c) is the orally active prodrug of the tyrosine kinase 2. TyK2-IN-21-d3 exhibits good chemical stability in aqueous system under different pHs. TyK2-IN-21-d3 alleviates the effect of gastric acid changes on drug absorption and improve the drug bioavailability in rat model .
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- HY-169963
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Phosphodiesterase (PDE)
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Others
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PDE1-IN-8 (Compound 3f) is the inhibitor for PDE1 with an IC50 of 11 nM. PDE1-IN-8 inhibits cAMP and cGMP signaling pathway, inhibits the differentiation and proliferation of cells into myofibroblast, and exhibits anti-fibrotic efficacy in Bleomycin (HY-17565)-induced rat pulmonary fibrosis model .
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- HY-120287
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Somatostatin Receptor
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Endocrinology
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L-054522 is an agonist for somatostatin receptor subtype 2 with Kd of 0.01 nM. L-054522 inhibits growth hormone release from rat primary pituitary cell (IC50=0.05 nM) and glucagon and insulin release from isolated mouse pancreatic islet cell (IC50=0.05 nM and 12 nM) .
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- HY-159062
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Biochemical Assay Reagents
NO Synthase
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Neurological Disease
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Goji Extract is a natural product with anti-aging, antioxidant, and neuroprotective effects. The antioxidant effect of Goji Extract has a positive impact on erectile dysfunction and can be used in research to improve erectile function .
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- HY-P10767
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Neurotensin Receptor
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Neurological Disease
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MD01-67 is a selective macrocyclic compound targeting the neurotensin receptor type 2 (NTS2), with Ki of 2.9 nM. MD01-67 exhibits analgesic and tactile hypersensitivity reducing activity in rats acute/persistent/chronic inflammatory pain models .
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- HY-163998
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Toll-like Receptor (TLR)
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Inflammation/Immunology
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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 .
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- HY-161784
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GABA Receptor
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Neurological Disease
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GABAA receptor modulator-5 (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 modulator-5 exhibits good pharmacokinetic characteristics in rats. GABAA receptor modulator-5 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 .
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- HY-W931056
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TRP Channel
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Neurological Disease
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AMG-628 is an orally active inhibitor for TRPV1, that inhibits Capsaicin (HY-10448) or acid (pH 5)-induced Ca 2+ influx into TRPV1- expressing CHO cell with IC50 of 4.9 and 3.1 nM. AMG-628 exhibits analgesic activity in Capsaicin (HY-10448)-induced rat model, and exhibits a half-life of 2.4 h in rats .
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- HY-168333
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5-HT Receptor
mTOR
CDK
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Neurological Disease
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5-HT6 inverse agonist 1 (Compound 33) is an antagonist for 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. 5-HT6 inverse agonist 1 inhibits the 5-HT6R mediated Cdk5 and mTOR signaling pathway. 5-HT6 inverse agonist 1 reduces tactile hypersensitivity in spinal nerve ligation (SNL)-induced rat model .
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- HY-B1573A
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AY-23,028; dl-Butaclamol hydrochloride
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Adrenergic Receptor
Dopamine Receptor
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Neurological Disease
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(±)-Butaclamol hydrochloride (AY-23,028) is the antagonist for adrenergic receptor and dopamine receptor. (±)-Butaclamol hydrochloride antagonizes amphetamine or Apomorphine (HY-12723)-induced stereotyped behaviors and emesis, inhibits discriminative avoidance behavior, and induces catalepsy in rats models .
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- HY-168068
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Others
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Neurological Disease
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Res-Glu3 is the derivative of Resveratrol (HY-16561). Res-Glu3 mitigates the ROS accumulation, and exhibits neuroprotective efficacy against H2O2-caused cellular damage in PC12. Res-Glu3 exhibits antioxidant activity in rats ischemia reperfusion models .
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- HY-162963
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PPAR
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Inflammation/Immunology
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PPARδ agonist 11 (Compound 11) is a selective agonist for PPARδ with an EC50 of 20 nM. PPARδ agonist 11 reduces the levels of nitrite oxide (NO), proinflammatory cytokines TNFα and IL-6 in LPS (HY-D1056)-stimulated RAW264.7 cell, and exhibits anti-inflammatory efficacy via NF-κB pathway. PPARδ agonist 11 exhibits good stability in human liver microsomes and plasma. PPARδ agonist 11 ameliorates Carrageenan (HY-125474)-induced foot edema .
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- HY-170586
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- HY-161925
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TGF-β Receptor
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Neurological Disease
Inflammation/Immunology
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sTGFBR3 antagonist 1 (Compound p24) is an antagonist for soluble transforming growth factor beta receptor 3 (sTGFBR3), thus activates TGF-β signaling pathway, and inhibits IκBα/NF-κB signaling pathway. sTGFBR3 antagonist 1 inhibits NO-release in LPS (HY-D1056) -induced BV2 cells with an IC50 of 0.52 μM. sTGFBR3 antagonist 1 exhibits anti-inflammatory and neuroprotective activities with blood brain barrier (BBB) permeability. sTGFBR3 antagonist 1 can be used in Alzheimer’s Disease research .
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- HY-B1258
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Aminomethylbenzoic acid; α-Amino-p-toluic acid
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Amino Acid Derivatives
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Cancer
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4-(Aminomethyl)benzoic acid is a competitive inhibitor of PepT1 and has antifibrinolytic activity .
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- HY-10716A
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GlyT
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Neurological Disease
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PF-03463275 is a centrally penetrant, orally available, selective, and competitive GlyT1 (glycine transporter-1) reversible inhibitor, with a Ki of 11.6 nM. PF-03463275 has the potential for Schizophrenia research .
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- HY-164040
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Somatostatin Receptor
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Metabolic Disease
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Zavolosotine (Compound 1) is an orally active agonist for somatostatin receptor type 5 (SST5) with EC50 <1 nM. Zavolosotine inhibits insulin and glucagon secretion, increases levels of glucagon in blood in rat model .
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- HY-151066
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PD-1/PD-L1
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Cancer
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BMS-1233 is an orally active inhibitor for programmed cell death-ligand 1 (PD-L1), with IC50 of 14.5 nM. BMS-1233 promotes cell death of HepG2 in a Jurkat T cell and HepG2 cell co-culture model, exhibits antitumor activity against melanoma in mouse model .
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- HY-164320
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Others
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Cancer
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Anticancer agent 245 (Compound 115) inhibits proliferation of cancer cell SKOV3, MDA-MB-231 and HCT-116 with IC50 of 0.021, 0.056 and 0.11 μM, respectively. Anticancer agent 245 exhibits antitumor efficacy in mice and good pharmacokinetic characteristics in rat models .
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- HY-160959
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nAChR
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Neurological Disease
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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) .
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- HY-160023
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D3S-001
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Ras
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Cancer
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Elisrasib is an orally active inhibitor for KRAS. Elisrasib inhibits the proliferation of KRAS G12C mutant H358 and MIA-PA-CA-2 with an IC50 of 0.6 and 0.44 nM. Elisrasib exhibits good metabolic stability in hepatocytes, liver microsomes, plasma and whole blood in various species. D3S-001 exhibits good pharmacokinetic characteristics and antitumor efficacy in mice .
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- HY-19590
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Ro 15-1570
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Drug Derivative
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Cancer
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Etarotene (Ro 15-1570) is a derivative of Arotinoid (HY-106735). Etarotene is an orally active antitumor agent against DMBA (HY-W011845)-induced mammary tumor and causes toxic symptoms of hypervitaminosis A in rat model .
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- HY-120476
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TRP Channel
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Neurological Disease
Inflammation/Immunology
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JNJ-39729209 is an antagonist for transient receptor potential vanilloid 1 (TRPV1) with pIC50 of 7.9, 8.5, 7.9 and 7.7 for TRPV1 from human, rat, canine and guinea pig. JNJ-39729209 inhibits Capsaicin (HY-10448)-induced hypotension and inhibit thereby hypothermia. JNJ-39729209 exhibits anti-inflammatory and analgesic activities in Carrageenan (HY-125474)- and CFA (HY-153808)-induced thermal hyperalgesia rat models. JNJ-39729209 exhibits anti-cough effects in guinea pigs .
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- HY-172200
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PD-1/PD-L1
HDAC
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Cancer
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PD-L1/HDAC6-IN-1 (Compound HP29) is the inhibitor for PD-L1 and HDAC6 that inhibits the PD-L1/PD-1 interaction and HDAC6 with an IC50 of 26.8 nM and 69 nM. PD-L1/HDAC6-IN-1 enhances the killing ability of Jurkat T cells against HepG2 cells with an IC50 of 3.4 μM. PD-L1/HDAC6-IN-1 exhibits good pharmacokinetics characteristics in rats with a drug exposure of 871.62 ng·h/mL, and exhibits antitumor activity in mouse B16-F10 xenograft models .
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- HY-169177
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JNK
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Inflammation/Immunology
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JNK-1-IN-4 (Compound E1) is an inhibitor for JNK, that inhibits JNK-1, JNK-2 and JNK-3 with IC50s of 2.7, 19.0 and 9.0 nM, respectively. JNK-1-IN-4 inhibits the phosphorylation of c-Jun, and reduces the expression of TGF-β1-induced EMT marker proteins, such as fibronectin and α-SMA. JNK-1-IN-4 exhibits good pharmacokinetic characteristics with a bioavailability of 69%. JNK-1-IN-4 exhibits anti-fibrotic effect in Bleomycin (HY-17565)-induced mice idiopathic pulmonary fibrosis models .
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- HY-P10587
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JNJ-77242113; JNJ-2113; PN-235
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Interleukin Related
STAT
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Inflammation/Immunology
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Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. In addition, Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
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- HY-161705
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Apoptosis
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Neurological Disease
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Anti-apoptotic agent 1 (Compound B4) exhibits neuroprotective activity and good pharmacokinetic properties. Anti-apoptotic agent 1 inhibits apoptosis, prevents stroke recurrence in photothrombotic rat model .
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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-164010
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- HY-P3641
-
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GnRH Receptor
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Neurological Disease
Metabolic Disease
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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 .
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Cat. No. |
Product Name |
Type |
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- HY-159062
-
|
Carbohydrates
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Goji Extract is a natural product with anti-aging, antioxidant, and neuroprotective effects. The antioxidant effect of Goji Extract has a positive impact on erectile dysfunction and can be used in research to improve erectile function .
|
Cat. No. |
Product Name |
Target |
Research Area |
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- HY-100801A
-
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Peptides
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Others
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DL-threo-3-Hydroxyaspartic acid is a glutamate uptake inhibitor that can block glutamate transport in cannulated sprague dawley rat .
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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-P10587
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JNJ-77242113; JNJ-2113; PN-235
|
Interleukin Related
STAT
|
Inflammation/Immunology
|
Icotrokinra (JNJ-77242113) is an orally available, selective antagonist of the IL-23 receptor. Icotrokinra inhibits IL-23-induced STAT3 phosphorylation in peripheral blood mononuclear cells (IC50=5.6 pM) and inhibits IL-23-induced interferon IFN-γ production in NK cells with an IC50 of 18.4 pM. In addition, Icotrokinra exhibits anti-inflammatory activity in a rat TNBS-induced colitis model. Icotrokinra can be used in the study of psoriasis, psoriatic arthritis, and inflammatory bowel disease .
|
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- HY-P3641A
-
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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 .
|
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- HY-P5130
-
|
Endothelin Receptor
|
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 .
|
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- HY-P1134
-
|
5-HT Receptor
|
Neurological Disease
|
Galanin (1-15) (porcine, rat) is the N-terminal 15 amino acids peptide fragment of the neuropeptide galanin. Galanin (1-15) (porcine, rat) interacts with the 5-HT1A receptor in the dorsal hippocampus of the rat brain, reduces the affinity of 5-HT1A receptors, and regulates the serotonin neuronal networks .
|
-
- HY-P10767
-
|
Neurotensin Receptor
|
Neurological Disease
|
MD01-67 is a selective macrocyclic compound targeting the neurotensin receptor type 2 (NTS2), with Ki of 2.9 nM. MD01-67 exhibits analgesic and tactile hypersensitivity reducing activity in rats acute/persistent/chronic inflammatory pain models .
|
-
- 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 .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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