Emricasan

Emricasan is a pan-caspase inhibitor. Ex vivo, emricasan (10 mg/kg) prevents cold ischemia-warm reperfusion-induced sinusoidal endothelial cell (SEC) apoptosis and inhibits caspase-3 activation in rat liver by 55 and 94%, respectively. In vivo, emricasan reduces alanine aminotransferase (ALT) levels (ED50s = <0.01-0.38 mg/kg) as well as apoptosis and caspase activity in a dose-dependent manner in the alpha-Fas mouse and D-Gln/LPS rat models of liver injury. Emricasan reduces caspase-3 and caspase-8 activity, serum ALT levels, hepatocyte apoptosis, and hepatic fibrogenesis in a mouse model of high-fat diet-induced non-alcoholic steatohepatitis (NASH). It also enhances islet engraftment and lowers post-transplant fasting glucose levels in a porcine islet autotransplant model.Formal Name: N-[2-(1,1-dimethylethyl)phenyl]-2-oxoglycyl-N-[(1S)-1-(carboxymethyl)-2-oxo-3-(2,3,5,6-tetrafluorophenoxy)propyl]-L-alaninamide. CAS Number: 254750-02-2. Synonyms: IDN-6556, PF-03491390. Molecular Formula: C26H27F4N3O7. Formula Weight: 569.5. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, Ethanol: 30 mg/ml. lambdamax: 266 nm. SMILES: CC(C)(C)C1=C(NC(C(N[C@@H](C)C(N[C@@H](CC(O)=O)C(COC2=C(F)C(F)=CC(F)=C2F)=O)=O)=O)=O)C=CC=C1. InChi Code: InChI=1S/C26H27F4N3O7/c1-12(31-24(38)25(39)32-16-8-6-5-7-13(16)26(2,3)4)23(37)33-17(10-19(35)36)18(34)11-40-22-20(29)14(27)9-15(28)21(22)30/h5-9,12,17H,10-11H2,1-4H3,(H,31,38)(H,32,39)(H,33,37)(H,35,36)/t12-,17-/m0/s1. InChi Key: SCVHJVCATBPIHN-SJCJKPOMSA-N.