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ATC 0065
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 0065图片
CAS NO:510732-84-0
包装与价格:
包装价格(元)
10mg电议
50mg电议

产品介绍
MCH1 antagonist,potent and selective
Cas No.510732-84-0
化学名N2-((1r,4r)-4-((4-bromo-2-(trifluoromethoxy)phenethyl)amino)cyclohexyl)-N4,N4-dimethylquinazoline-2,4-diamine dihydrochloride
Canonical SMILESBrC1=CC=C(C(OC(F)(F)F)=C1)CCN[C@@H](CC2)CC[C@H]2NC3=NC4=CC=CC=C4C(N(C)C)=N3.Cl.Cl
分子式C25H29BrF3N5O.2HCl
分子量625.35
溶解度Soluble in DMSO
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

ATC0065 is a selective and potent antagonist of the melanin-concentrating hormone receptor 1 (MCH1) with IC50 of 15.7 nM. This component also displays affinity for 5-HT1A and 5-HT2B receptors with IC50 of 62.9nM and 266 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 assay, ATC0065 bounds with high affinity to the MCH-R1 with IC50 value of 16 nMand showed good metabolic stability in liver microsomes isolated from human and rat 1.

In rodents, ATC0065 is potent and orally active MCHR1 antagonists with anxiolytic and antidepressant activity. ATC0065 treatmetn significantly reversed swim stress-induced anxiety in the stress-induced hyperthermia in mice and elevated plus-maze test in rats2. However, ATC0065 did not affect spontaneous locomotor activity or rotarod performance in rats 2.

References:
1.  Kanuma K, Omodera K, Nishiguchi M, et al. Identification of 4-amino-2-cyclohexylaminoquinazolines as metabolically stable melanin-concentrating hormone receptor 1 antagonists. Bioorganic & medicinal chemistry. 2006;14(10):3307-3319.
2.   Chaki S, Funakoshi T, Hirota-Okuno S, et al. Anxiolytic- and antidepressant-like profile of ATC0065 and ATC0175: nonpeptidic and orally active melanin-concentrating hormone receptor 1 antagonists. The Journal of pharmacology and experimental therapeutics. 2005;313(2):831-839.