Emricasan (IDN-6556)

Catalog No.S7775 Synonyms: PF 03491390, PF-03491390

For research use only.

Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.

Emricasan (IDN-6556) Chemical Structure

CAS No. 254750-02-2

Selleck's Emricasan (IDN-6556) has been cited by 24 publications

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Biological Activity

Description Emricasan (IDN-6556, PF 03491390, PF-03491390) is a potent irreversible pan-caspase inhibitor. Emricasan is an inhibitor of Zika virus infection.
Targets
caspase [1]
In vitro

Emricasan, also called IDN-6556 or PF-03491390, is an inhibitor of activated caspases, and it has sub- to nanomolar activity in vitro. Emricasan shows neuroprotective activity for hNPCs but does not suppress ZIKV replication[2].

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Jurkat E6-1 NXTXSYsyTnWwY4Tpc44h[XO|YYm= Mk\0TY5pcWKrdHnvckBw\iCDboTpMWZieyCjboTpZo9lgS2rbnT1Z4VlKGOjc4Dhd4UuOyCjY4Tpeol1gSCrbjDoeY1idiCMdYLrZZQhTTZvMTDj[YxteyC3c3nu[{BC[y2GRW\EMWFOSyC|dXLzeJJifGViYomg[ox2d3Knc3PlcoNmKGKjc3XkJIF{e2G7LDDJR|UxKD1iMD6wNFYh|ryPLh?= MWe8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTZ3MEK4O{c,Ojl4NUCyPFc9N2F-
JFas Mo\lSpVv[3Srb36gZZN{[Xl? MX;Jcohq[mm2b4L5JINwdmOnboTyZZRqd25iYXfhbY5{fCCMRnHzJINmdGy|LDDJR|UxKD1iMD6wNlUh|ryPLh?= NVPCUnZFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[yOVA3OzVpPkG2NlUxPjN3PD;hQi=>
THP-1 M4LLcmZ2dmO2aX;uJIF{e2G7 M4jB[WlvcGmkaYTvdpkh[2:wY3XueJJifGmxbjDh[4FqdnO2IGTIVE0yKGOnbHzzMEBKSzVyIE2gNE4zPyEQvF2u NWL6NmdFRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMU[yOVA3OzVpPkG2NlUxPjN3PD;hQi=>
A673 M3nPOpFJXFNiYYPzZZk> NGLDV5ZyUFSVIH;mJJBm\GmjdILpZ{Bk[W6lZYKgZ4VtdCCuaX7ld{B1dyCrZHXueIlngSCvdXz0bZBt\SCxcIDvdpR2dmm2aXXzJIZweiCmcoXnJJJmeHW{cH;zbY5oQiCScnntZZJ6KHOlcnXlckBnd3JiQU[3N{Bk\Wyucx?= MX28ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Saos-2 NWDpeYt3eUiWUzDhd5NigQ>? MXLxTHRUKG:oIIDl[IlifHKrYzDjZY5k\XJiY3XscEBtcW6nczD0c{Bq\GWwdHnmfUBufWy2aYDs[UBweHCxcoT1col1cWW|IH\vdkBlenWpIILldJVzeG:|aX7nPkBRemmvYYL5JJNkemWnbjDmc5IhW2Gxcz2yJINmdGy| MXO8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
MG 63 (6-TG R) M3jYdJFJXFNiYYPzZZk> M{\BbZFJXFNib3[gdIVlcWG2cnnjJINidmOncjDj[YxtKGyrbnXzJJRwKGmmZX70bYZ6KG23bITpdIxmKG:ycH;yeJVvcXSrZYOg[o9zKGS{dXegdoVxfXKyb4Ppcoc7KFC{aX3hdpkhe2O{ZXXuJIZweiCPRzC2N{ApPi2WRzDSLUBk\Wyucx?= NIDzU4o9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OUSzOVE{QSd-Mkm0N|UyOzl:L3G+
NB1643 Mne0dWhVWyCjc4PhfS=> NVXmT5A6eUiWUzDv[kBx\WSrYYTybYMh[2GwY3XyJINmdGxibHnu[ZMhfG9iaXTlcpRq\nlibYXseIlxdGVib4Dwc5J1fW6rdHnld{Bnd3JiZIL1[{Bz\XC3coDvd4lv\zpiUILpcYFzgSC|Y4Ll[Y4h\m:{IF7CNVY1OyClZXzsdy=> MnLSQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjl2M{WxN|koRjJ7NEO1NVM6RC:jPh?=
SK-N-MC MXvxTHRUKGG|c3H5 MonLdWhVWyCxZjDw[YRq[XS{aXOgZ4Fv[2W{IHPlcIwhdGmwZYOgeI8hcWSnboTp[pkhdXWudHnwcIUhd3Cyb4L0eY5qfGmnczDmc5Ih\HK3ZzDy[ZB2enCxc3nu[|ohWHKrbXHyfUB{[3KnZX6g[o9zKFONLV6tUWMh[2WubIO= MWq8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQTR|NUGzPUc,Ojl2M{WxN|k9N2F-
Assay
Methods Test Index PMID
Growth inhibition assay Cell viability 27571349
In vivo Emricasan decreases liver injury but not metabolic derangement in NASH. It also ameliorates inflammation. In the murine NASH model, stellate cell activation and hepatic fibrogenesis are attenuated by administration of the pan-caspase inhibitor Emricasan[1]. Emricasan is currently being evaluated in phase 2 clinical trials for the reduction of hepatic injury and liver fibrosis caused by chronic HCV infection[2].

Protocol (from reference)

Cell Research:[2]
  • Cell lines: Astrocytes
  • Concentrations: 9 μM
  • Incubation Time: 1 h
  • Method: Astrocytes are mock-infected, treated with DMSO or treated with 2 μM niclosamide, 92 μM PHA-690509, 9 μM emricasan, or a combination of 92 μM PHA-690509 and 9 μM emricasan for 1 h before infection with PRVABC59 (MOI = 0.5). Cells are fixed 24 h after infection and stained for ZIKVE and nuclei.
Animal Research:[1]
  • Animal Models: C57BL/6J mice
  • Dosages: 0.3mg/kg/day
  • Administration: i.g.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 569.50
Formula

C26H27F4N3O7

CAS No. 254750-02-2
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC(C(=O)NC(CC(=O)O)C(=O)COC1=C(C(=CC(=C1F)F)F)F)NC(=O)C(=O)NC2=CC=CC=C2C(C)(C)C

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03205345 Unknown status Drug: Emricasan (25 mg)|Drug: Emricasan (5 mg)|Drug: Placebo Decompensated Cirrhosis Conatus Pharmaceuticals Inc. June 28 2017 Phase 2
NCT01653899 Completed Drug: IDN-6556 Diabetes University of Alberta|Conatus Pharmaceuticals Inc. June 2012 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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