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ATC 0175 hydrochloride Sale

目录号 : GC10700

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。

ATC 0175 hydrochloride Chemical Structure

Cas No.:510733-97-8

规格 价格 库存 购买数量
10mg
¥3,077.00
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50mg
¥12,926.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

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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.

Chemical Properties

Cas No. 510733-97-8 SDF
化学名 N-((1s,4s)-4-((4-(dimethylamino)quinazolin-2-yl)amino)cyclohexyl)-3,4-difluorobenzamide hydrochloride
Canonical SMILES FC1=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°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
Shipping Condition 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。

溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.1648 mL 10.8239 mL 21.6478 mL
5 mM 0.433 mL 2.1648 mL 4.3296 mL
10 mM 0.2165 mL 1.0824 mL 2.1648 mL
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