Name: JMV3002
Rating: 5 (10 reviews)

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HIT ID:HIT214320785
Cas No:925239-03-8
常用名:JMV3002
别名:JMV3002
IUPAC:N-[(1R)-1-{4-[(2,4-dimethoxyphenyl)methyl]-5-(2-phenylethyl)-4H-1,2,4-triazol-3-yl}-2-(1H-indol-3-yl)ethyl]pyridine-2-carboxamide
IUPAC:N-[(1R)-1-{4-[(2,4-dimethoxyphenyl)methyl]-5-(2-phenylethyl)-4H-1,2,4-triazol-3-yl}-2-(1H-indol-3-yl)ethyl]pyridine-2-carboxamide
InChI key:UMGBPWZCCHVQAY-WJOKGBTCSA-N

分子式:C35H34N6O3
分子量:586.696
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)c(OC)c1
SMILES:COc1ccc(Cn2c(CCc3ccccc3)nnc2[C@@H](Cc2c[nH]c3ccccc23)NC(=O)c2ccccn2)c(OC)c1

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. At 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.

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