A pan-caspase inhibitor; prevents cold ischemia-warm reperfusion-induced SEC apoptosis and inhibits caspase-3 activation in rat liver at 10 mg/kg ex vivo; reduces ALT levels (ED50s =

Emricasan – 5 mg

Brand:
Cayman
CAS:
254750-02-2
Storage:
-20
UN-No:
Non-Hazardous - /

Emricasan is a pan-caspase inhibitor.{42093,42094,42095,42096} 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.{42093} 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 α-Fas mouse and D-Gln/LPS rat models of liver injury.{42094} 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).{42095} It also enhances islet engraftment and lowers post-transplant fasting glucose levels in a porcine islet autotransplant model.{42096}  

 

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Description

A pan-caspase inhibitor; prevents cold ischemia-warm reperfusion-induced SEC apoptosis and inhibits caspase-3 activation in rat liver at 10 mg/kg ex vivo; reduces ALT levels (ED50s = <0.01-0.38 mg/kg) as well as apoptosis and caspase activity in a dose-dependent manner in the α-Fas mouse and D-Gln/LPS rat models of liver injury; reduces caspase-3 and caspase-8 activity, serum ALT levels, hepatocyte apoptosis, and hepatic fibrogenesis in a mouse model of high-fat diet-induced NASH; 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

Synonyms:  IDN-6556|PF-03491390

Molecular weight: 569.5

CAS: 254750-02-2

Purity: ≥95%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Caspases||Research Area|Cell Biology|Cell Death|Apoptosis||Research Area|Cell Biology|Cell Death|Pyroptosis||Research Area|Cell Biology|Proteolysis|Cytosolic & Secreted Proteases||Research Area|Endocrinology & Metabolism|Metabolic Diseases|Diabetes||Research Area|Endocrinology & Metabolism|Metabolic Diseases|NAFLD & NASH||Research Area|Immunology & Inflammation

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