| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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Purity: ≥98%
Emricasan (formerly also known as IDN-6556 and PF 03491390) is a potent, first-in-class and irreversible pan-caspase inhibitor. It is being tested in clinical studies to treat liver diseases. In a murine model of non-alcoholic steatohepatitis, emricasan lessens liver damage and fibrosis. In a porcine islet autotransplant model, emricasan promotes marginal mass islet engraftment. Patients with chronic hepatitis C who take Emricasan orally may have less active aminotransferases. In a mouse model of alpha-fas-induced liver injury, oral PF-03491390 is retained in the liver for an extended amount of time with minimal systemic exposure, acting as a hepatoprotective agent.
| Targets |
Caspase
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|---|---|
| ln Vitro |
Emricasan, also known as IDN-6556 or PF-03491390, is a sub- to nanomolar active inhibitor of activated caspases. While Emricasan exhibits neuroprotective activity for hNPCs, ZIKV replication is not prevented[2].
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| ln Vivo |
Emricasan reduces NASH-related liver damage but not metabolic disturbance. It lessens inflammation as well. The pan-caspase inhibitor Emricasan reduces hepatic fibrogenesis and stellate cell activation in the murine NASH model[1]. Phase 2 clinical trials are currently being conducted on emricasan to determine whether it can lessen the hepatic damage and liver fibrosis brought on by chronic HCV infection[2].
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| Cell Assay |
Astrocytes are mock-infected, treated with DMSO, or treated with 2 M niclosamide, 92 M PHA-690509, 9 μM emricasan, or a combination of 92 μM PHA-690509 and 9 M emricasan for 1 h prior to infection with PRVABC59 (MOI = 0.5). Following infection for 24 hours, cells are fixed and stained for ZIKVE and nuclei.
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| References |
| Molecular Formula |
C26H27F4N3O7
|
|---|---|
| Molecular Weight |
569.5021
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| Exact Mass |
569.18
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| Elemental Analysis |
C, 54.83; H, 4.78; F, 13.34; N, 7.38; O, 19.66
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| CAS # |
254750-02-2
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| Related CAS # |
254750-02-2;
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| Appearance |
white solid powder
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| SMILES |
C[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)COC1=C(C(=CC(=C1F)F)F)F)NC(=O)C(=O)NC2=CC=CC=C2C(C)(C)C
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| InChi Key |
SCVHJVCATBPIHN-SJCJKPOMSA-N
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| InChi Code |
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
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| Chemical Name |
(3S)-3-[[(2S)-2-[[2-(2-tert-butylanilino)-2-oxoacetyl]amino]propanoyl]amino]-4-oxo-5-(2,3,5,6-tetrafluorophenoxy)pentanoic acid
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| Synonyms |
Emricasan; PF 03491390; PF-03491390; PF03491390; IDN-6556; IDN6556; IDN 6556
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL (~175.6 mM)
Ethanol: ~25 mg/mL (~43.9 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (4.39 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (4.39 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.39 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 5%DMSO+40%PEG300+5%Tween80+50%ddH2O: 5mg/ml |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7559 mL | 8.7796 mL | 17.5593 mL | |
| 5 mM | 0.3512 mL | 1.7559 mL | 3.5119 mL | |
| 10 mM | 0.1756 mL | 0.8780 mL | 1.7559 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02960204 | Completed | Drug: Emricasan Drug: Placebo |
Cirrhosis Portal Hypertension |
Histogen | October 17, 2016 | Phase 2 |
| NCT02230683 | Completed | Drug: IDN-6556 | Liver Cirrhosis | Conatus Pharmaceuticals Inc. | August 2014 | Phase 2 |
| NCT02686762 | Completed | Drug: Emricasan (5 mg) Drug: Emricasan (50 mg) |
Fibrosis Liver Diseases |
Conatus Pharmaceuticals Inc. | January 26, 2016 | Phase 2 |
| NCT04803227 | Terminated | Drug: Emricasan Other: Placebo |
Covid19 | Histogen | March 11, 2021 | Phase 1 |
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