Forskolin

Forskolin

Emricasan

As low as $105.00
In stock
SKU
SML21
Description

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.)

Application

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.

Specifications
Molecular NameEmricasan
Size5 mg (SML21A) or 10 mg (SML21B)
FormPowder
Alternative NamesPF 03491390; IDN-6556
Chemical NameL-Alaninamide, N-[2-(1,1-dimethylethyl) phenyl]-2-oxoglycyl-N-[(1S)-1-(carboxymethyl)-2-oxo-3-(2,3,5,6-tetrafluorophenoxy) propyl]-
Chemical FormulaC₂₆H₂₇F₄N₃O₇
Molecular Weight569.50
CAS Number254750-02-2
Purity≥98% by LCMS
Physical AppearanceWhite to off-white (Solid)
TargetCaspase; Apoptosis
Shelf-Life≥ 2 years (powder)
ShippingRoom Temperature
StorageStore at -20°C
Quality StatementThis product is for Research Use Only and is not intended for therapeutic or diagnostic use.
Documents
References and Publications
  1. 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
  2. Gracia-Sancho J, et al. 2019. Emricasan Ameliorates Portal Hypertension and Liver Fibrosis in Cirrhotic Rats Through a Hepatocyte-Mediated Paracrine Mechanism. Hepatol Commun.
  3. 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.
  4. 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.
  5. 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.
  6. 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.
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