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ATC 0175 hydrochloride
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。
ATC 0175 hydrochloride图片
CAS NO:510733-97-8
包装与价格：
包装价格(元)
10mg电议
50mg电议

产品介绍
ATC 0175 hydrochloride 是一种有效的、选择性的、具有口服活性的黑色素浓缩激素 1 受体拮抗剂，对 MCH1R、MCH2R 的 IC50 分别为 13.5、>10000 nM。
Cas No.510733-97-8
化学名N-((1s,4s)-4-((4-(dimethylamino)quinazolin-2-yl)amino)cyclohexyl)-3,4-difluorobenzamide hydrochloride
Canonical SMILESFC1=CC(C(N[C@H]2CC[C@H](CC2)NC3=NC4=CC=CC=C4C(N(C)C)=N3)=O)=CC=C1F.Cl
分子式C23H25F2N5O.HCl
分子量461.94
溶解度<11.55mg/ml in ethanol
储存条件Store at -20℃
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

ATC0175 hydrochloride is a potent, selective and orally active antagonist of melanin-concentrating hormone receptor 1 (MCH1) with IC50 of 13 nM for MCH1. It was also shown to have affinity for 5-HT2B and 5-HT1A receptors with IC50 of 9.66 nM and 16.9 nM respectively.

Melanin-concentrating hormone receptor (MCH1), a member of the G protein-coupled receptor family 1, is an integral plasma membrane protein which binds melanin-concentrating hormone. The protein can inhibit cAMP accumulation and stimulate intracellular calcium flux, and is probably involved in the neuronal regulation of food consumption.

In vitro, assays showed that this compound is a potent antagonist with a high affinity for MCH1R. The receptor binding and the functional assay (MCH-induced increase in [Ca2+]) indicated that ATC0175 is a noncompetitive antagonist at MCH1Rs 1.

In vivo, ATC0175 displayed anxiolytic effects in numerous animal models of anxiety including the social interaction test, elevated plus-maze test, maternal separation-induced vocalization and stress-induced hyperthermia. In addition, ATC0175 treatment also exhibited antidepressant effects in the forced swimming test 2.

References:
1.  Semple G, Tran TA, Kramer B, et al. Pyrimidine-based antagonists of h-MCH-R1 derived from ATC0175: in vitro profiling and in vivo evaluation. Bioorganic & medicinal chemistry letters. 2009;19(21):6166-6171.
2.   Chaki S, Yamaguchi J, Yamada H, et al. ATC0175: an orally active melanin-concentrating hormone receptor 1 antagonist for the potential treatment of depression and anxiety. CNS drug reviews. 2005;11(4):341-352.