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.

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.

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

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.

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

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.

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

• . 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.  [Content Brief]

  . 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.  [Content Brief]