TC-MCH 7c 

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 K_is of 3.4 nM and 3.0 nM of human and mouse MCH₁R, respectively^[2].

IC50: 5.6 nM (hMCH₁R)^[1]
Ki: 3.4 nM (hMCH₁R) and 3.0 nM (mouse MCH₁R)^[1]

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].

MCE 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^[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].

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

408.47

C₂₄H₂₅FN₂O₃

864756-35-4

固体

Light yellow to yellow

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [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.  [Content Brief]