For research use only. Not for therapeutic Use.
Emricasan(Cat No.:I002870)is a small molecule inhibitor of caspases, specifically targeting caspase-1 and caspase-3, which are involved in apoptosis and inflammation. It has been investigated primarily for its potential therapeutic applications in liver diseases, including non-alcoholic steatohepatitis (NASH) and cirrhosis, as well as for its role in reducing liver fibrosis. By inhibiting caspases, emricasan can prevent excessive cell death and inflammation, which are key contributors to liver damage. Clinical trials have explored its efficacy in improving liver function and fibrosis, although more studies are needed to confirm its long-term safety and effectiveness in treating these conditions.
Catalog Number | I002870 |
CAS Number | 254750-02-2 |
Molecular Formula | C26H27F4N3O7 |
Purity | ≥95% |
Target | Anti-infection |
Solubility | DMSO: ≥ 42 mg/mL |
Storage | Store at -20°C |
IC50 | 10 mg/kg was required to prevent liver injury |
IUPAC Name | (3S)-3-[[(2S)-2-[[2-(2-tert-butylanilino)-2-oxoacetyl]amino]propanoyl]amino]-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid |
InChI | 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 |
InChIKey | SCVHJVCATBPIHN-SJCJKPOMSA-N |
SMILES | C[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)COC1=C(C(=CC(=C1F)F)F)F)NC(=O)C(=O)NC2=CC=CC=C2C(C)(C)C |
Reference | </br>1:The caspase-8 inhibitor emricasan combines with the SMAC mimetic birinapant to induce necroptosis and treat acute myeloid leukemia. Brumatti G, Ma C, Lalaoui N, Nguyen NY, Navarro M, Tanzer MC, Richmond J, Ghisi M, Salmon JM, Silke N, Pomilio G, Glaser SP, de Valle E, Gugasyan R, Gurthridge MA, Condon SM, Johnstone RW, Lock R, Salvesen G, Wei A, Vaux DL, Ekert PG, Silke J.Sci Transl Med. 2016 May 18;8(339):339ra69. doi: 10.1126/scitranslmed.aad3099. PMID: 27194727 </br>2:Carcinogenicity assessment of the pan-caspase inhibitor, emricasan, in Tg.rasH2 mice. Elbekai RH, Paranjpe MG, Contreras PC, Spada A.Regul Toxicol Pharmacol. 2015 Jul;72(2):169-78. doi: 10.1016/j.yrtph.2015.04.007. Epub 2015 Apr 17. PMID: 25896096 </br>3:The pan-caspase inhibitor Emricasan (IDN-6556) decreases liver injury and fibrosis in a murine model of non-alcoholic steatohepatitis. Barreyro FJ, Holod S, Finocchietto PV, Camino AM, Aquino JB, Avagnina A, Carreras MC, Poderoso JJ, Gores GJ.Liver Int. 2015 Mar;35(3):953-66. doi: 10.1111/liv.12570. Epub 2014 Jun 6. PMID: 24750664 |