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AZD1979 Sale

目录号 : GC31643

AZD1979是一个Melanin-concentratinghormonereceptor1(MCHr1)拮抗剂,其IC50值约为12nM。

AZD1979 Chemical Structure

Cas No.:1254035-84-1

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Sample solution is provided at 25 µL, 10mM.

Description

AZD1979 is a Melanin-concentrating hormone receptor 1 (MCHr1) antagonist with an IC50 of ~12 nM.

In DIO mice, initial AZD1979-mediate body weight loss is driven by decreasing food intake, but an additional component of preserving energy expenditure is apparent in pair-feeding and indirect calorimetry studies. AZD1979 also dose-dependently reduces body weight in dogs[1].

[1]. Ploj K, et al. Effects of a novel potent melanin-concentrating hormone receptor 1 antagonist, AZD1979, on body weight homeostasis in mice and dogs. Br J Pharmacol. 2016 Sep;173(18):2739-51.

实验参考方法

Animal experiment:

Three weeks after the light-dark cycle have been reversed, all mice are sham dosed by p.o. gavage for 6 days to habituate the animals to the procedure, randomized into experimental groups base on average body weights and dosed p.o. with AZD1979 (20, 40 or 60 μmol/kg twice daily at 8:00 h and 15:00 h) or vehicle (0.5% HPMC, 0.1% Tween twice daily) for 21 days (n=6 per group). Three mice per group are then dosed once more with the respective doses of AZD1979 (20, 40 or 60 μmol/kg p.o.) and killed after 17 h by administration of an overdose of isoflurane (anaesthesia)[1].

References:

[1]. Ploj K, et al. Effects of a novel potent melanin-concentrating hormone receptor 1 antagonist, AZD1979, on body weight homeostasis in mice and dogs. Br J Pharmacol. 2016 Sep;173(18):2739-51.

化学性质

Cas No. 1254035-84-1 SDF
Canonical SMILES O=C(C1=NN=C(C2=CC=C(OC)C=C2)O1)N3CC(OC4=CC=C(CN(C5)CC65COC6)C=C4)C3
分子式 C25H26N4O5 分子量 462.5
溶解度 DMSO : 33.33 mg/mL (72.06 mM; ultrasonic and warming and heat to 60°C) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.1622 mL 10.8108 mL 21.6216 mL
5 mM 0.4324 mL 2.1622 mL 4.3243 mL
10 mM 0.2162 mL 1.0811 mL 2.1622 mL
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