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Emricasan

Catalog No.: 16071024
Cas No.: 254750-02-2
Purity : 98%
16071024 - Emricasan | CAS 254750-02-2

Catalog number : 16071024

CAS number : 254750-02-2

分子式 : C26H27F4N3O7 

分子量 : 569.51 

Iupac 化学名称 : (S)-3-((S)-2-(2-((2-(tert-butyl)phenyl)amino)-2-oxoacetamido)propanamido)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid 

Smile : C(C)(C)(C)C1=C(C=CC=C1)NC(C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(COC1=C(C(=CC(=C1F)F)F)F)=O)C)=O

InChiKey : SCVHJVCATBPIHN-SJCJKPOMSA-N

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同义词IDN-6556;IDN6556;PF 03491390;PF-03491390;Emricasan;PF03491390
英文同义词IDN-6556;IDN6556;PF 03491390;PF-03491390;Emricasan;PF03491390
分子式C26H27F4N3O7 
分子量569.51 
外观Off-white powder 
纯度98%
可溶性Soluble in DMSO 
存储-20 ºC for 3 years 
运输条件Shipped under ambient temperature 
SmileC(C)(C)(C)C1=C(C=CC=C1)NC(C(=O)N[C@H](C(=O)N[C@@H](CC(=O)O)C(COC1=C(C(=CC(=C1F)F)F)F)=O)C)=O
InChiKeySCVHJVCATBPIHN-SJCJKPOMSA-N
InChiInChI=1S/C26H27F4N3O7/c1-12(31-24(38)25(39)32-16-8-6-5-7-13(16)26(2,3)4)23(37)33-17(10-19(35)36)18(34)11-40-22-20(29)14(27)9-15(28)21(22)30/h5-9,12,17H,10-11H2,1-4H3,(H,31,38)(H,32,39)(H,33,37)(H,35,36)/t12-,17-/m0/s1
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Emricasan (IDN-6556, PF-03491390) is a potent irreversible pan-caspase inhibitor with the ability to rapidly reduce elevated levels of serum ALT, AST and caspase mediated cleavage of cytokeratin-18 in HCV infected patients. 1,2,3 To date, emricasan has been studied in more than 550 individuals and has exhibited a safety profile similar to placebo. 

Emricasan is currently in three Phase 2 clinical trials, including two trials in patients with liver cirrhosis. Here we report the effect of emricasan in healthy volunteers on measures of serum caspase activity and apoptosis. These results are compared with the effect of emricasan in subjects with varying degrees of hepatic impairment, as well as the effect of emricasan in subjects with severe renal impairment.

 

1.       Frenette CT1, Morelli G2, Shiffman ML3, etc.Emricasan Improves Liver Function in PatientsWith Cirrhosis and High Model for End-Stage Liver Disease Scores Compared With Placebo. Clin Gastroenterol Hepatol. 2019 Mar;17(4):774-783.e4. doi: 10.1016/j.cgh.2018.06.012. Epub 2018 Jun 18.

2.       Khurana S1, Khara HS1. Is Emricasan (IDN-6556), an oral pan-caspase inhibitor, ready for controlled trials? Hepatology. 2019 May 2. doi: 10.1002/hep.30683.


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