WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 510230

CAS#: 254750-02-2

Description: Emricasan, also known as IDN 6556 and PF 03491390, is a first-in-class caspase inhibitor in clinical trials for the treatment of liver diseases. Emricasan (IDN-6556) decreases liver injury and fibrosis in a murine model of non-alcoholic steatohepatitis. IDN6556 facilitates marginal mass islet engraftment in a porcine islet autotransplant model. Oral IDN-6556 may lower aminotransferase activity in patients with chronic hepatitis C. Orally-administered PF-03491390 is retained in the liver for prolonged periods with low systemic exposure, exerting a hepatoprotective effect against alpha-fas-induced liver injury in a mouse model.

Chemical Structure

CAS# 254750-02-2

Theoretical Analysis

MedKoo Cat#: 510230
Name: Emricasan
CAS#: 254750-02-2
Chemical Formula: C26H27F4N3O7
Exact Mass: 569.17851
Molecular Weight: 569.51
Elemental Analysis: C, 54.83; H, 4.78; F, 13.34; N, 7.38; O, 19.66

Size Price Shipping out time Quantity
10mg USD 90 Same day
25mg USD 150 Same day
50mg USD 250 Same day
100mg USD 450 Same day
200mg USD 750 Same day
500mg USD 1650 Same day
1g USD 2850 Same day
2g USD 5050 Same day
Inquire bulk and customized quantity

Pricing updated 2021-02-25. Prices are subject to change without notice.

Emricasan, purity > 98%, is in stock.

Synonym: IDN-6556; IDN6556; IDN 6556; PF 03491390; PF-03491390; PF03491390; 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


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

SMILES Code: O=C(O)C[C@H](NC([C@H](C)NC(C(NC1=CC=CC=C1C(C)(C)C)=O)=O)=O)C(COC2=C(F)C(F)=CC(F)=C2F)=O

white solid powder

>98% (or refer to the Certificate of Analysis)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL

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1: Rotman Y, Sanyal AJ. Current and upcoming pharmacotherapy for non-alcoholic fatty liver disease. Gut. 2016 Sep 19. pii: gutjnl-2016-312431. doi: 10.1136/gutjnl-2016-312431. [Epub ahead of print] Review. PubMed PMID: 27646933.

2: Xu M, Lee EM, Wen Z, Cheng Y, Huang WK, Qian X, Tcw J, Kouznetsova J, Ogden SC, Hammack C, Jacob F, Nguyen HN, Itkin M, Hanna C, Shinn P, Allen C, Michael SG, Simeonov A, Huang W, Christian KM, Goate A, Brennand KJ, Huang R, Xia M, Ming GL, Zheng W, Song H, Tang H. 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. doi: 10.1038/nm.4184. PubMed PMID: 27571349.

3: Brumatti G, Ma C, Lalaoui N, Nguyen NY, Navarro M, Tanzer MC, Richmond J, Ghisi M, Salmon JM, Silke N, Pomilio G, Glaser SP, de Valle E, Gugasyan R, Gurthridge MA, Condon SM, Johnstone RW, Lock R, Salvesen G, Wei A, Vaux DL, Ekert PG, Silke J. The caspase-8 inhibitor emricasan combines with the SMAC mimetic birinapant to induce necroptosis and treat acute myeloid leukemia. Sci Transl Med. 2016 May 18;8(339):339ra69. doi: 10.1126/scitranslmed.aad3099. PubMed PMID: 27194727.

4: Elbekai RH, Paranjpe MG, Contreras PC, Spada A. Carcinogenicity assessment of the pan-caspase inhibitor, emricasan, in Tg.rasH2 mice. Regul Toxicol Pharmacol. 2015 Jul;72(2):169-78. doi: 10.1016/j.yrtph.2015.04.007. Epub 2015 Apr 17. PubMed PMID: 25896096.

5: Barreyro FJ, Holod S, Finocchietto PV, Camino AM, Aquino JB, Avagnina A, Carreras MC, Poderoso JJ, Gores GJ. 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. doi: 10.1111/liv.12570. Epub 2014 Jun 6. PubMed PMID: 24750664.

6: Haddad JJ. Current opinion on 3-[2-[(2-tert-butyl-phenylaminooxalyl)-amino]-propionylamino]- 4-oxo-5-(2,3,5,6-tetrafluoro-phenoxy)-pentanoic acid, an investigational drug targeting caspases and caspase-like proteases: the clinical trials in sight and recent anti-inflammatory advances. Recent Pat Inflamm Allergy Drug Discov. 2013 Sep;7(3):229-58. Review. PubMed PMID: 23859695.

7: McCall MD, Maciver AM, Kin T, Emamaullee J, Pawlick R, Edgar R, Shapiro AM. Caspase inhibitor IDN6556 facilitates marginal mass islet engraftment in a porcine islet autotransplant model. Transplantation. 2012 Jul 15;94(1):30-5. doi: 10.1097/TP.0b013e318257745d. PubMed PMID: 22706322.

8: McCall M, Toso C, Emamaullee J, Pawlick R, Edgar R, Davis J, Maciver A, Kin T, Arch R, Shapiro AM. The caspase inhibitor IDN-6556 (PF3491390) improves marginal mass engraftment after islet transplantation in mice. Surgery. 2011 Jul;150(1):48-55. doi: 10.1016/j.surg.2011.02.023. Epub 2011 May 18. PubMed PMID: 21596412.

9: Shiffman ML, Pockros P, McHutchison JG, Schiff ER, Morris M, Burgess G. Clinical trial: the efficacy and safety of oral PF-03491390, a pancaspase inhibitor - a randomized placebo-controlled study in patients with chronic hepatitis C. Aliment Pharmacol Ther. 2010 May;31(9):969-78. doi: 10.1111/j.1365-2036.2010.04264.x. Epub 2010 Feb 16. PubMed PMID: 20163376.

10: Pockros PJ. Antifibrotics for chronic hepatitis C. Clin Liver Dis. 2009 Aug;13(3):365-73. doi: 10.1016/j.cld.2009.05.005. Review. PubMed PMID: 19628154.

11: Fischer U, Janssen K, Schulze-Osthoff K. Does caspase inhibition promote clonogenic tumor growth? Cell Cycle. 2007 Dec 15;6(24):3048-53. Epub 2007 Oct 2. Review. PubMed PMID: 18073530.

12: Ueno Y, Ohmi T, Yamamoto M, Kato N, Moriguchi Y, Kojima M, Shimozono R, Suzuki S, Matsuura T, Eda H. Orally-administered caspase inhibitor PF-03491390 is retained in the liver for prolonged periods with low systemic exposure, exerting a hepatoprotective effect against alpha-fas-induced liver injury in a mouse model. J Pharmacol Sci. 2007 Oct;105(2):201-5. Epub 2007 Oct 6. PubMed PMID: 17928737.

13: Pockros PJ, Schiff ER, Shiffman ML, McHutchison JG, Gish RG, Afdhal NH, Makhviladze M, Huyghe M, Hecht D, Oltersdorf T, Shapiro DA. Oral IDN-6556, an antiapoptotic caspase inhibitor, may lower aminotransferase activity in patients with chronic hepatitis C. Hepatology. 2007 Aug;46(2):324-9. PubMed PMID: 17654603.

14: Georgiev P, Clavien PA, Gores GJ. Liver graft protection by antiapoptotic drugs: a step further. Liver Transpl. 2007 Mar;13(3):318-20. PubMed PMID: 17318874.

15: Hoglen NC, Anselmo DM, Katori M, Kaldas M, Shen XD, Valentino KL, Lassman C, Busuttil RW, Kupiec-Weglinski JW, Farmer DG. A caspase inhibitor, IDN-6556, ameliorates early hepatic injury in an ex vivo rat model of warm and cold ischemia. Liver Transpl. 2007 Mar;13(3):361-6. PubMed PMID: 17318854.

16: Baskin-Bey ES, Washburn K, Feng S, Oltersdorf T, Shapiro D, Huyghe M, Burgart L, Garrity-Park M, van Vilsteren FG, Oliver LK, Rosen CB, Gores GJ. Clinical Trial of the Pan-Caspase Inhibitor, IDN-6556, in Human Liver Preservation Injury. Am J Transplant. 2007 Jan;7(1):218-25. PubMed PMID: 17227570.

17: Davis GL. New therapies: oral inhibitors and immune modulators. Clin Liver Dis. 2006 Nov;10(4):867-80. Review. PubMed PMID: 17164122.

18: Leung-Toung R, Zhao Y, Li W, Tam TF, Karimian K, Spino M. Thiol proteases: inhibitors and potential therapeutic targets. Curr Med Chem. 2006;13(5):547-81. Review. PubMed PMID: 16515521.

19: Linton SD, Aja T, Armstrong RA, Bai X, Chen LS, Chen N, Ching B, Contreras P, Diaz JL, Fisher CD, Fritz LC, Gladstone P, Groessl T, Gu X, Herrmann J, Hirakawa BP, Hoglen NC, Jahangiri KG, Kalish VJ, Karanewsky DS, Kodandapani L, Krebs J, McQuiston J, Meduna SP, Nalley K, Robinson ED, Sayers RO, Sebring K, Spada AP, Ternansky RJ, Tomaselli KJ, Ullman BR, Valentino KL, Weeks S, Winn D, Wu JC, Yeo P, Zhang CZ. First-in-class pan caspase inhibitor developed for the treatment of liver disease. J Med Chem. 2005 Nov 3;48(22):6779-82. PubMed PMID: 16250635.

20: Quadri SM, Segall L, de Perrot M, Han B, Edwards V, Jones N, Waddell TK, Liu M, Keshavjee S. Caspase inhibition improves ischemia-reperfusion injury after lung transplantation. Am J Transplant. 2005 Feb;5(2):292-9. PubMed PMID: 15643988.

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