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TC-MCH 7c

黑色素聚集激素受体1（MCH1R）拮抗剂,TC-MCH 7c 是一种苯基吡啶酮衍生物，一种口服有效的，选择性的且可穿透血脑屏障的 MCH1R 拮抗剂，对 hMCH1R 的 IC50 为 5.6 nM。

目录号: PC10989 纯度: ≥98%

CAS No. :864756-35-4

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中文名称

TC-MCH 7c

英文名称

TC-MCH 7c

英文别名

TC-MCH 7c;4-[(4-Fluorobenzyl)oxy]-1-{4-[2-(1-pyrrolidinyl)ethoxy]phenyl}-2( 1H)-pyridinone;4-[(4-Fluorophenyl)methoxy]-1-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-2(1H)-pyridinone;BDBM50301081;4-(4-Fluoro-benzyloxy)-1-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-1H-pyridin-2-one;4-(4-fluorobenzyloxy)-1-(4-(2-(pyrrolidin-1-yl)ethoxy)phenyl)pyridin-2(1H)-one

Cas No.

864756-35-4

分子式

C₂₄H₂₅FN₂O₃

分子量

408.47

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

TC-MCH 7c, a phenylpyridone derivative, is an orally available, selective and brain-penetrable MCH₁R antagonist with an IC₅₀ of 5.6 nM for hMCH₁R. TC-MCH 7c has K_is of 3.4 nM and 3.0 nM of human and mouse MCH₁R, respectively.

性状

Solid

IC50 & Target[1][2]

IC50: 5.6 nM (hMCH₁R)
Ki: 3.4 nM (hMCH₁R) and 3.0 nM (mouse MCH₁R)

体外研究(In Vitro)

TC-MCH 7c has an IC₅₀ of 9.7 μM for MCH₁R in [Ca]i mobilization.
TC-MCH 7c has IC₅₀s of 23 nM and 9.0 μM for FLIPR and hERG, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

TC-MCH 7c (oral; 3-30 mg/kg; once-daily for 1.5 months) exhibits excellent body weight reduction in a dose-dependent manner in DIO mice model.
TC-MCH 7c (oral; 3-30 mg/kg) with 30 mg/kg has plasma concentrations of 5.1, 1.8, and 0.7 μM at 2, 15, and 24 hours, respectively.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6J DIO mice
Dosage:	3, 10 and 30 mg/kg
Administration:	Oral; once-daily for 1.5 months
Result:	Exhibited excellent body weight reduction in a dose-dependent manner.

Animal Model:	Diet-induced obesity mice
Dosage:	3, 10 and 30 mg/kg (Pharmacokinetic Analysis)
Administration:	Oral
Result:	Plasma concentrations at 2, 15, and 24 hours were 5.1, 1.8, and 0.7 μM, respectively.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Ito M, et al. Melanin-concentrating hormone 1-receptor antagonist suppresses body weight gain correlated with high receptor occupancy levels in diet-induced obesity mice. Eur J Pharmacol. 2009 Dec 10;624(1-3):77-83. [Information]

[2]. Haga Y, et al. Discovery of novel phenylpyridone derivatives as potent and selective MCH1R antagonists. Bioorg Med Chem. 2011 Jan 15;19(2):883-93. [Information]

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2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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