Emricasan is an irreversible and highly selective pan-caspase inhibitor, demonstrating irreversible inhibition and a significant first-pass effect (Tian J, et al). Emricasan has been found to directly improve hepatocytes phenotype in primary rat cirrhotic hepatocytes and has hepatoprotective effects in human liver cells (Barreyro et al). Emricasan, formerly known as IDN-6556, in combination with birinapan, has been used to treat acute myeloid leukemia.. (Brumatti G, et al.)
Emricasan has been used in clinical trials for the treatment of non-alcoholic steatohepatitis (NASH) with advanced fibrosis (scarring) and cirrhosis. Emricasan has also been shown to protect infected astrocytes from ZIKV-induced cell death. This small molecule irreversible inhibitor is under clinical investigation to reduce hepatic injury and liver fibrosis.
|Size||5 mg (SML21A) or 10 mg (SML21B)|
|Alternative Names||PF 03491390; IDN-6556|
|Chemical Name||L-Alaninamide, N-[2-(1,1-dimethylethyl) phenyl]-2-oxoglycyl-N-[(1S)-1-(carboxymethyl)-2-oxo-3-(2,3,5,6-tetrafluorophenoxy) propyl]-|
|Purity||≥98% by LCMS|
|Physical Appearance||White to off-white (Solid)|
|Shelf-Life||≥ 2 years (powder)|
|Storage||Store at -20°C|
|Quality Statement||This product is for Research Use Only and is not intended for therapeutic or diagnostic use.|
References and Publications
- Brumatti G, et al. 2016. The caspase-8 inhibitor emricasan combines with the SMAC mimetic birinapant to induce necroptosis and treat acute myeloid leukemia. Science Translational Medicine, 8, 339ra69-339ra69
- Gracia-Sancho J, et al. 2019. Emricasan Ameliorates Portal Hypertension and Liver Fibrosis in Cirrhotic Rats Through a Hepatocyte-Mediated Paracrine Mechanism. Hepatol Commun.
- Tian J, et al. 2017. Combination of Emricasan with AP24534 Synergistically Reduces Ischemia/Reperfusion Injury in Rat Brain Through Simultaneous Prevention of Apoptosis and Necroptosis. Transl Stroke Res.
- Xu M, et al. 2016. Identification of small-molecule inhibitors of Zika virus infection and induced neural cell death via a drug repurposing screen. Nat Med.
- Barreyro FJ, et al. 2015. The pan-caspase inhibitor Emricasan (IDN-6556) decreases liver injury and fibrosis in a murine model of non-alcoholic steatohepatitis. Liver Int.
- Hoglen NC, et al.2004. Characterization of IDN-6556 (3-[2-(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]-4-oxo-5-(2,3,5,6-te trafluoro-phenoxy)-pentanoic acid): a liver-targeted caspase inhibitor. J Pharmacol Exp Ther.