TC-MCH 7c

Research use only, not for human use.

TC-MCH 7c is an oral, selectable and blood-brain barrier penetrating MCH1R antagonist with IC50 performance of 5.6 nM against hMCH1R, and TC-MCH 7c is a phenylpyridone derivative with MCH1R Ki of 3.4 nM against human. In mice, MCH1R Ki was 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