For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I010943 |
| CAS Number | 864756-35-4 |
| Synonyms | 4-[(4-fluorophenyl)methoxy]-1-[4-(2-pyrrolidin-1-ylethoxy)phenyl]pyridin-2-one |
| Molecular Formula | C24H25FN2O3 |
| Purity | ≥95% |
| InChI | InChI=1S/C24H25FN2O3/c25-20-5-3-19(4-6-20)18-30-23-11-14-27(24(28)17-23)21-7-9-22(10-8-21)29-16-15-26-12-1-2-13-26/h3-11,14,17H,1-2,12-13,15-16,18H2 |
| InChIKey | ANCFKYJMXNMYNZ-UHFFFAOYSA-N |
| SMILES | C1CCN(C1)CCOC2=CC=C(C=C2)N3C=CC(=CC3=O)OCC4=CC=C(C=C4)F |
| 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. |
