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CAS No. : 254750-02-2
MCE 国际站:Emricasan
产品活性:Emricasan (PF 03491390) 是一种口服有效的 不可逆 pan-caspase 抑制剂。Emricasan 抑制 Zika 病毒 (ZIKV) 诱导的 caspase-3 活性增加并保护了人类皮层神经祖细胞。
研究领域:Apoptosis | Anti-infection
作用靶点:Caspase | Influenza Virus
In Vitro: Emricasan (PF 03491390; IDN-6556) (50 μM; 24 hours) directly improves hepatocytes phenotype in primary rat cirrhotic hepatocytes.
?Emricasan (10-50 μM) has hepatoprotective effects in human liver cells.
In Vivo: Emricasan (PF 03491390; IDN-6556) is orally active that is retained in the liver for a prolonged period of time. TUNEL-positive cells are considerably increased by five-fold in mice fed a HFD and are reduced under Emricasan treatment. In accordance with this observation caspase-3 and -8 are increased in HFD-fed mice by 1.5- and 1.3-fold respectively and are significantly decreased by Emricasan treatment.
?When comparing efficacy by multiple routes of administration, Emricasan is administered i.p., p.o., i.m., or i.v. (0.03-3 mg/kg). Caspase 3-like activities, measured as DEVD-AMC cleavage, dose dependently decreased with a 92.5% reduction after the highest dose of Emricasan (3 mg/kg). Emricasan is initially tested in the α-Fas model of liver injury, marked hepatocellular apoptosis, and peak ALT activities within 6 h. Emricasan is administered i.p. immediately after administration of α-Fas, ALT activities, measured 6 h later, decreased in a dose-dependent manner with an ED50 value of 0.08 (0.06-0.12) mg/kg.
?Emricasan is a highly selective pan-caspase inhibitor demonstrating irreversible inhibition and a significant first-pass effect. In both syngeneic mouse islets and human islets transplanted into immunodeficient mice, Emricasan (i.p., 20 mg/kg) given for 7 days post-transplant led to a significantly enhanced rate of diabetes reversal as compared to vehicle.
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