Emricasan
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.
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Chemical Information
| Name | Emricasan |
|---|---|
| Iupac Chemical Name | (S)-3-((S)-2-(2-((2-(tert-butyl)phenyl)amino)-2-oxoacetamido)propanamido)-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid |
| Synonyms | IDN-6556;IDN6556;PF 03491390;PF-03491390;Emricasan;PF03491390 |
| Molecular Formula | C26H27F4N3O7 |
| Molecular Weight | 569.51 |
| 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 |
| InChi | InChI=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 |
| CAS Number | 254750-02-2 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white powder |
|---|---|
| Purity | 98% |
| Storage | -20 ºC for 3 years |
| Solubility | Soluble in DMSO |
| Handling | |
| Shipping Condition | Shipped under ambient temperature |
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| Mechanism | |
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| Clinical study |
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.
Chemical Structure
