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SNAP 94847 hydrochloride Sale

目录号 : GC17846

An antagonist of MCH1

SNAP 94847 hydrochloride Chemical Structure

Cas No.:487051-12-7

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10mg
¥1,457.00
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50mg
¥6,120.00
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产品描述

SNAP 94847 is a novel, high affinity selective melanin-concentrating hormonereceptor1 (MCHR1) antagonist with (Ki= 2.2 nM, Kd=530 pM), it displays >80-fold and >500-fold selectivity over MCHα1A and MCHD2 receptors respectively. SNAP 94847 binds with high affinity to the mouse and rat MCHR1 with minimal cross-reactivity to other GPCR, ion channels, enzymes, and transporters[1][3].

SNAP 94847 (oral gavage; 20 mg/kg; 14 days) shows an exaggerated locomotor response to acute quinpirole [treatment: F(2,19)=11.31, treatment × time: F(34,323) = 4.061], the effect of SNAP 94847 on quinpirole-evoked ambulations over the entire observation period is significant compared to the untreated animals[2].SNAP 94847 (oral administration; 20 mg/kg; 21 days) in drink water, produces a significant increase in ambulation relative to untreated animals [treatment: F(3,28) = 8.971; treatment × time: F(51,476)=11.50]. shows a marked increase in locomotion is apparent after 40 min in the SNAP 94847-treated group,this effect is significant over 180 min[2].SNAP 94847 (oral administration; 10 mg/kg), has a good bioavailability (59%), low plasma and blood clearances of 4.2 L/hr/kg and 3.3 L/hr/kg, respectively, and the half-life was shown to be 5.2 h in rats in a PK study[3].

References:
[1]. David DJ, et al. Efficacy of the MCHR1 antagonist N-[3-(1-{[4-(3,4-difluorophenoxy)phenyl]methyl}(4-piperidyl))-4-methylphenyl]-2-methylpropanamide (SNAP 94847) in mouse models of anxiety and depression following acute and chronic administration is independent of hippocampal neurogenesis. J Pharmacol Exp Ther. 2007 Apr;321(1):237-48. Epub 2007 Jan 19.
[2]. Nair SG, et al. Effects of the MCH1 receptor antagonist SNAP 94847 on high-fat food-reinforced operant responding and reinstatement of food seeking in rats.Psychopharmacology (Berl). 2009 Jul;205(1):129-40.

Chemical Properties

Cas No. 487051-12-7 SDF
化学名 (Z)-N-(3-(1-(4-(3,4-difluorophenoxy)benzyl)piperidin-4-yl)-4-methylphenyl)isobutyrimidic acid hydrochloride
Canonical SMILES CC(/C(O)=N/C1=CC(C2CCN(CC3=CC=C(OC4=CC(F)=C(F)C=C4)C=C3)CC2)=C(C=C1)C)C.Cl
分子式 C29H32F2N2O2.HCl 分子量 515.03
溶解度 <51.5mg/ml in DMSO; <51.5mg/ml in ethanol 储存条件 Desiccate at RT
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1 mg 5 mg 10 mg
1 mM 1.9416 mL 9.7082 mL 19.4163 mL
5 mM 0.3883 mL 1.9416 mL 3.8833 mL
10 mM 0.1942 mL 0.9708 mL 1.9416 mL
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