TC-MCH 7c

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

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。TC-MCH 7c 对人和小鼠 MCH1R 的 Ki 分别为 3.4 nM 和 3.0 nM。

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 Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively.

TC-MCH 7c has an IC50 of 9.7 μM for MCH1R in [Ca2+]i mobilization. TC-MCH 7c has IC50s of 23 nM and 9.0 μM for FLIPR and hERG, respectively.

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. 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.

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GPCR/G Protein

MCHR

Melanin-concentrating Hormone Receptor (MCHR)

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864756-35-4

408.47

C24H25FN2O3

>98% (HPLC)

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Fc1ccc(COc2ccn(-c3ccc(OCCN4CCCC4)cc3)c(=O)c2)cc1

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(-20℃)

With Ice Pack

≥ 2 years