Emricasan

SKU: orb1300430

Description

Emricasan

Research Area

Stem Cell & Developmental Biology

Key Properties

• CAS Number: 254750-02-2
• MW: 569.5
• Purity: >98%
• Formula: C₂₆H₂₇F₄N₃O₇
• SMILES: C[C@H](NC(=O)C(=O)Nc1ccccc1C(C)(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)COc1c(F)c(F)cc(F)c1F
• Target: Protease
• Solubility: Soluble in DMSO (up to at least 20 mg/ml)

Bioactivity

• Target IC50:
  Caspase-8:0.4 nM|THP-1 cells:0.27 μM|Caspase-3:0.31 nM|JFas cells:0.025 μM
• In Vivo:
  METHODS: To study the effects on chronic liver disease, Emricasan (10 mg/kg, 0.9% dimethylcarboxycellulose) was administered orally once daily for seven days to rats with advanced cirrhosis due to chronic CCl4 administration. RESULTS: Emricasan ameliorated hepatic sinusoidal microvascular dysfunction in cirrhotic patients, resulting in significant improvement in fibrosis, portal hypertension and liver function. METHODS: To investigate the effects on cirrhosis, Emricasan (10 mg/kg) was administered intraperitoneally once daily for 10-20 days to C57BL/6 mice with secondary biliary cirrhosis induced by bile duct ligation (BDL). RESULTS: Emricasan treatment improved survival and portal hypertension (PHT) in a mouse model of long-term BDL.
• In Vitro:
  METHODS: Primary rat cirrhotic hepatocytes were treated with Emricasan (50 µM) for 24 h, and mRNA expression levels were measured. RESULTS: Emricasan directly improved the expression of hepatocyte-specific markers. METHODS: Human cervical cancer cells HeLa were pretreated with Emricasan (10 µM) for 1 h, then treated with vincristine (20 nM) for 44 h. Cell death was detected by Flow Cytometry. RESULTS: Emricasan eliminated 95% of vincristine-mediated cell death.
• Cell Research:
  Astrocytes are mock-infected, treated with DMSO or treated with 2 μM niclosamide, 92 μM PHA-690509, 9 μM emricasan, or a combination of 92 μM PHA-690509 and 9 μM emricasan for 1 h before infection with PRVABC59 (MOI = 0.5). Cells are fixed 24 h after infection and stained for ZIKVE and nuclei.(Only for Reference)

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

IDN-6556; PF-03491390

Compound Identifiers

PubChem CID

12000240