| Bioactivity | Emricasan (PF 03491390) is an orally active and irreversible pan-caspase inhibitor. Emricasan inhibits Zika virus (ZIKV)-induced increases in caspase-3 activity and protected human cortical neural progenitors[1]. | ||||||||||||
| Invitro | Emricasan (PF 03491390; IDN-6556) (50 μM; 24 hours) directly improves hepatocytes phenotype in primary rat cirrhotic hepatocytes[1]. Emricasan (10-50 μM) has hepatoprotective effects in human liver cells[1]. | ||||||||||||
| In Vivo | Emricasan (PF 03491390; IDN-6556) is orally active that is retained in the liver for 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[2]. 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[3]. 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[4]. | ||||||||||||
| Name | Emricasan | ||||||||||||
| CAS | 254750-02-2 | ||||||||||||
| Formula | C26H27F4N3O7 | ||||||||||||
| Molar Mass | 569.50 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Gracia-Sancho J, et al. Emricasan Ameliorates Portal Hypertension and Liver Fibrosis in Cirrhotic Rats Through a Hepatocyte-Mediated Paracrine Mechanism. Hepatol Commun. 2019 Apr 22;3(7):987-1000. [2]. Barreyro FJ, et al. The pan-caspase inhibitor Emricasan (IDN-6556) decreases liver injury and fibrosis in a murine model of non-alcoholic steatohepatitis. Liver Int. 2015 Mar;35(3):953-66. [3]. Hoglen NC, et al. 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. 2004 May;309(2):634-40. [4]. McCall M, et al. The caspase inhibitor IDN-6556 (PF3491390) improves marginal mass engraftment after islet transplantation in mice. Surgery. 2011 Jul;150(1):48-55. [5]. Tian J, et al. Combination of Emricasan with AP24534 Synergistically Reduces Ischemia/Reperfusion Injury in Rat Brain Through Simultaneous Prevention of Apoptosis and Necroptosis. Transl Stroke Res. 2017 Nov 4. [6]. Xu M, et al. Identification of small-molecule inhibitors of Zika virus infection and induced neural cell death via a drug repurposing screen. Nat Med. 2016 Oct;22(10):1101-1107. |
Emricasan
CAS: 254750-02-2 F: C26H27F4N3O7 W: 569.50
Emricasan (PF 03491390) is an orally active and irreversible pan-caspase inhibitor. Emricasan inhibits Zika virus (ZIKV)
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