2. Apoptosis
    Anti-infection
  3. Caspase
    Influenza Virus
  4. Emricasan

Emricasan  (Synonyms: PF 03491390; IDN-6556)

Cat. No.: HY-10396 Purity: 99.59%
COA Handling Instructions

Emricasan (PF 03491390) is an orally active and irreversible pan-caspase inhibitor. Emricasan inhibits Zika virus (ZIKV)-induced increases in caspase-3 activity and protected human cortical neural progenitors.

For research use only. We do not sell to patients.

Emricasan Chemical Structure

Emricasan Chemical Structure

CAS No. : 254750-02-2

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10 mM * 1 mL in DMSO USD 135 In-stock
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Customer Review

Based on 25 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Emricasan purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Jun 5;10(6):442.   [Abstract]

    Morphology examination of infected monocytes with or without IDN treatment at 12hpi. Representative images of immunofluorescence stained influenza A NP protein (green, upper) and bright field (BF, lower) images of the cells.

    Emricasan purchased from MCE. Usage Cited in: Cell Death Dis. 2019 Jun 5;10(6):442.   [Abstract]

    Western blot determined cleavage of caspase-8, -9, -3 in H7N9-infected monocytes treated or untreated with IDN at 3, 6 and 12hpi. β-actin protein is used as the control for sample loading.

    Emricasan purchased from MCE. Usage Cited in: J Exp Med. 2018 Jul 2;215(7):1839-1852.  [Abstract]

    Immunoblotting analyses of enteroid cultures treated with 4-OHT for 24 h in the presence of Nec1s or Emricasan or Mock, followed by 0.25 ng/mL TNF for 3 h. Cell lysates are immunoblotted with the antibodies indicated on the right.

    Emricasan purchased from MCE. Usage Cited in: J Virol. 2018 Apr 27;92(10). pii: e00078-18.  [Abstract]

    Cell lysates are collected at day 5 post reactivation and subjected to western blot analysis for p-IRF3 (Ser396), total IRF3, and β-actin (as a loading control).

    Emricasan purchased from MCE. Usage Cited in: Nat Protoc. 2015 May;10(5):807-21.  [Abstract]

    The 18F-FHBG uptake is prohibited after adding the caspase inhibitor IDN6556 during 0.5 μg/mL Dox treatment for 24 h.

    View All Caspase Isoform Specific Products:

    View All Isoforms
    Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Emricasan (PF 03491390) is an orally active and irreversible pan-caspase inhibitor. Emricasan inhibits Zika virus (ZIKV)-induced increases in caspase-3 activity and protected human cortical neural progenitors[1].

    IC50 & Target

    Caspase

     

    In Vitro

    Emricasan (PF 03491390; IDN-6556) (50 μM; 24 hours) directly improves hepatocytes phenotype in primary rat cirrhotic hepatocytes[1].
    Emricasan (10-50 μM) has hepatoprotective effects in human liver cells[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    Emricasan (PF 03491390; IDN-6556) is orally active that is retained in the liver for prolonged period of time. TUNEL-positive cells are considerably increased by five-fold in mice fed a HFD and are reduced under Emricasan treatment. In accordance with this observation caspase-3 and -8 are increased in HFD-fed mice by 1.5- and 1.3-fold respectively and are significantly decreased by Emricasan treatment[2].
    When comparing efficacy by multiple routes of administration, Emricasan is administered i.p., p.o., i.m., or i.v. (0.03-3 mg/kg). Caspase 3-like activities, measured as DEVD-AMC cleavage, dose dependently decreased with a 92.5% reduction after the highest dose of Emricasan (3 mg/kg). Emricasan is initially tested in the α-Fas model of liver injury, marked hepatocellular apoptosis, and peak ALT activities within 6 h. Emricasan is administered i.p. immediately after administration of α-Fas, ALT activities, measured 6 h later, decreased in a dose-dependent manner with an ED50 value of 0.08 (0.06-0.12) mg/kg[3].
    Emricasan is a highly selective pan-caspase inhibitor demonstrating irreversible inhibition and a significant first-pass effect. In both syngeneic mouse islets and human islets transplanted into immunodeficient mice, Emricasan (i.p., 20 mg/kg) given for 7 days post-transplant led to a significantly enhanced rate of diabetes reversal as compared to vehicle[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    569.50

    Appearance

    Solid

    Formula

    C26H27F4N3O7
    CAS No.
    SMILES

    FC1=C(C(F)=C(C=C1F)F)OCC([[email protected]@H](NC([[email protected]@H](NC(C(NC2=C(C=CC=C2)C(C)(C)C)=O)=O)C)=O)CC(O)=O)=O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (175.59 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: 2.5 mg/mL (4.39 mM); Suspended solution; Need ultrasonic

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (4.39 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (4.39 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.59%

    COA (247 KB) HNMR (285 KB) LCMS (267 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [2][3]

    Mice[2]
    The male C57BL/6J mice are age-matched and used at approximately 12-16 weeks of age. Four groups are studied (n=60) with 15 mice per group. Groups 1 and 3 receive regular chow. Groups 2 and 4 receive HFD and 50 g/L (Sucrose) is added to drinking water for 20 weeks. Groups 3 and 4 receive Emricasan 0.3 mg/kg/day per os, and Group 1 and 2 receive the vehicle. The oral administration of Emricasan at doses of 0.3 mg/kg corresponds to the ED90 value to prevent liver injury in the model of α-Fas-induced liver injury. Total body weight is measured at 0, 5, 10, 15 and 20 weeks.
    Rats[3]
    The male Sprague-Dawley rats are used. Blood (100 μL/sample) is taken from the carotid cannula 2 to 240 min after administration of Emricasan (i.v., s.c., p.o., or i.p.). Serum is prepared and frozen immediately until analysis. In studies measuring drug concentrations in portal and systemic blood, individual rats are bled (three animals per time point) simultaneously from the portal vein and inferior vena cava. In the biliary excretion study, bile is collected from the common bile duct after i.v. and p.o. administration of Emricasan (10 mg/kg) over a 24-h period on ice and frozen until analysis.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Emricasan254750-02-2PF 03491390 IDN-6556PF03491390PF-03491390IDN6556IDN 6556IDN-6556CaspaseInfluenza VirusInhibitorinhibitorinhibit

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