For research use only. Not for therapeutic Use.
PF-06471553 is a potent, selective and orally available monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM.
PF-06471553 (6f) is a potent and selective monoacylglycerol acyltransferase 3 (MGAT3) inhibitor, with an IC50 of 92 nM, and shows >160 fold in vitro selectivity for MGAT3 over DGAT1 (IC50, >50 μM), DGAT2 (IC50, >100 μM), MGAT1 (IC50, 14.9 μM), and MGAT2 (IC50, 19.8 μM). PF-06471553 exhibits inhibitory activity against MGAT3 in HEK-293 cells with an IC50 of 205 nM (pIC50, 6.69)[1].
PF-06471553 (200 mg/kg, p.o.) in addition with (DGAT1 and DGAT2) inhibitors shows additional inhibition of glycerol-d5 incorporated triolein in hMGAT3 mice, and with no effect on WT mice[1].
| Catalog Number | I008690 |
| CAS Number | 1808094-07-6 |
| Synonyms | N-(2-cyclobutyltriazol-4-yl)-2-[2-(3-methoxyphenyl)acetyl]-1,3-dihydroisoindole-5-sulfonamide |
| Molecular Formula | C23H25N5O4S |
| Purity | ≥95% |
| InChI | InChI=1S/C23H25N5O4S/c1-32-20-7-2-4-16(10-20)11-23(29)27-14-17-8-9-21(12-18(17)15-27)33(30,31)26-22-13-24-28(25-22)19-5-3-6-19/h2,4,7-10,12-13,19H,3,5-6,11,14-15H2,1H3,(H,25,26) |
| InChIKey | GRXCLNMCJWKTAT-UHFFFAOYSA-N |
| SMILES | COC1=CC=CC(=C1)CC(=O)N2CC3=C(C2)C=C(C=C3)S(=O)(=O)NC4=NN(N=C4)C5CCC5 |
| Reference | [1]. Huard K, et al. Discovery of Selective Small Molecule Inhibitors of Monoacylglycerol Acyltransferase 3. J Med Chem. 2015 Sep 24;58(18):7164-72. |
