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BMS 193885
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BMS 193885图片
CAS NO:679839-66-8
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
Competitive NPY Y1 receptor antagonist
Cas No.679839-66-8
化学名(S)-2-hydroxypropanoic acid compound with (Z)-N-(3-(3,5-bis(methoxycarbonyl)-2,6-dimethyl-1,4-dihydropyridin-4-yl)phenyl)-N'-(3-(4-(3-methoxyphenyl)piperidin-1-yl)propyl)carbamimidic acid (1:1)
Canonical SMILESCC(N1)=C(C(OC)=O)C(C(C(OC)=O)=C1C)C2=CC(N/C(O)=N/CCCN3CCC(C4=CC(OC)=CC=C4)CC3)=CC=C2.C[C@@](O)([H])C(O)=O
分子式C33H42N4O6.C3H6O3
分子量680.79
溶解度<68.08mg/ml in DMSO;<13.62mg/ml in Water
储存条件Desiccate at RT
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BMS-193885 is a potent and selective neuropeptide Y1 receptor antagonist with IC50 of 5.9nM.

Neuropeptide Y receptor 1 is G-protein coupled receptors and implicated in the modulation of food intake and energy homeostasis. Neuropeptide Y1 is expressed in many tissues including the hippocampus, hypothalamus, amygdala and the cortex of the brain as well as in peripheral tissues heart, kidney, skeletal muscle. The localization and expression suggests their involvement in the regulation of food intake and body weight.

In cellular culture, BMS-193885 displayed functional antagonism of Neuropeptide Y1 in a

forskolin-stimulated c-AMP production assay using CHO cells expressing the human Y(1) receptor 1.

In vivo, administration of BMS-193885 at a dosage of 10mg/kg leads to 1h neuropeptide Y-induced food intake in rat and the spontaneous overnight food consumpetion 2 . Chronic administration of BMS-193885 (10 mg/kg) i.p. for 44 days significantly reduced food intake and the rate of body weight gain as compared to their control without developing tolerance or affecting water intake 2.

References:
1.  Poindexter GS, Bruce MA, LeBoulluec KL, et al. Dihydropyridine neuropeptide Y Y(1) receptor antagonists. Bioorganic & medicinal chemistry letters. 2002;12(3):379-382.
2.   Antal-Zimanyi I, Bruce MA, Leboulluec KL, et al. Pharmacological characterization and appetite suppressive properties of BMS-193885, a novel and selective neuropeptide Y(1) receptor antagonist. European journal of pharmacology. 2008;590(1-3):224-232.