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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.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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