TC-MCH 7c_product_DataBase

Bioactivity

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[1]. TC-MCH 7c has Kis of 3.4 nM and 3.0 nM of human and mouse MCH1R, respectively[2].

Target

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

Invitro

TC-MCH 7c has an IC50 of 9.7 μM for MCH1R in [Ca2+]i mobilization[1]. TC-MCH 7c has IC50s of 23 nM and 9.0 μM for FLIPR and hERG, respectively[2].

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[1]. 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[2]. Animal Model:

Name

TC-MCH 7c

CAS

864756-35-4

Formula

C24H25FN2O3

Molar Mass

408.47

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

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

Reference

[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. [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.

PeptideDB

TC-MCH 7c

CAS: 864756-35-4 F: C24H25FN2O3 W: 408.47