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Description: Potent pan-caspase inhibitor
Chemical Name: N-[2-(1,1-Dimethylethyl)phenyl]-2-oxoglycyl-N-[(1S)-1-(carboxymethyl)-2-oxo-3-(2,3,5,6-tetrafluorophenoxy)propyl]-L-alaninamide
Purity: ≥98% (HPLC)
Biological Activity for Emricasan
Emricasan is a potent caspase inhibitor (IC50 values are 0.3, 0.4, 2, 4, 6, 6 and 20 nM for caspase-9, -1, -3, -6, -7, -8, and -2, respectively). Emricasan is antiapoptotic by inhibiting caspase 8. It also preserves cell viability after infection with several strains of Zika. Emricasan promotes survival of pluripotent stem cells in culture when used in combination with Chroman-1 (Cat. No. 7163), trans-ISRIB (Cat. No. 5284) and Polyamine Supplement x1000 (lyophilized) (Cat. No. 7739), a combination known as CEPT. When used as part of the CEPT cocktail, Emricasan improves survival of differentiated cells following cryopreservation. The compound also reduces hepatic inflammation in an animal model of liver injury. Orally bioavailable.
Compound Libraries for Emricasan
Emricasan is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.
Technical Data for Emricasan
| M. Wt | 569.51 |
| Formula | C26H27F4N3O7 |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 254750-02-2 |
| PubChem ID | 12000240 |
| InChI Key | SCVHJVCATBPIHN-SJCJKPOMSA-N |
| Smiles | N(C(C(N[C@H](C(N[C@H](C(COC1=C(F)C(F)=CC(F)=C1F)=O)CC(O)=O)=O)C)=O)=O)C2=C(C(C)(C)C)C=CC=C2 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Emricasan
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 56.95 | 100 | |
| ethanol | 28.48 | 50 |
Preparing Stock Solutions for Emricasan
The following data is based on the product molecular weight 569.51. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.76 mL | 8.78 mL | 17.56 mL |
| 5 mM | 0.35 mL | 1.76 mL | 3.51 mL |
| 10 mM | 0.18 mL | 0.88 mL | 1.76 mL |
| 50 mM | 0.04 mL | 0.18 mL | 0.35 mL |
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Product Datasheets for Emricasan
References for Emricasan
References are publications that support the biological activity of the product.
Chen et al (2021) A versatile polypharmacology platform promotes cytoprotection and viability of human pluripotent and differentiated cells. Nat.Methods 18 528 PMID: 33941937
Canbay et al (2004) The caspase inhibitor IDN-6556 attenuates hepatic injury and fibrosis in the bile duct ligated mouse. J.Pharmacol.Exp.Ther. 308 1191 PMID: 14617689
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Citations for Emricasan
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Literature in this Area
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