1. Apoptosis
  2. Caspase
  3. Emricasan

Emricasan (Synonyms: PF 03491390; IDN-6556)

Cat. No.: HY-10396 Purity: 99.88%
Handling Instructions

Emricasan (PF 03491390) is an irreversible pan-caspase inhibitor.

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
Estimated Time of Arrival: December 31
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Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 540 In-stock
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100 mg USD 972 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

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

    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: J Exp Med. 2018 Jul 2;215(7):1839-1852.

    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: Nat Protoc. 2015 May;10(5):807-21.

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

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

    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: Cell Death Dis. 2019 Jun 5;10(6):442. 

    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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Emricasan (PF 03491390) is an irreversible pan-caspase inhibitor.

    IC50 & Target[1]

    Caspase

     

    In Vivo

    Emricasan (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[1].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[2]. 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[3].

    Molecular Weight

    569.50

    Formula

    C₂₆H₂₇F₄N₃O₇

    CAS No.

    254750-02-2

    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 : ≥ 42 mg/mL (73.75 mM)

    *"≥" means soluble, but saturation unknown.

    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); Clear solution

    • 2.

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

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

    • 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 provided by MCE.
    References
    Animal Administration
    [1][2]

    Mice[1]
    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[2]
    The male Sprague-Dawley rats are cannulated in the carotid artery under isoflurane anesthesia and allowed to recover for at least 1 day before drug administration. 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

    Purity: 99.88%

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    Product Name:
    Emricasan
    Cat. No.:
    HY-10396
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