2. Apoptosis Anti-infection
  3. Caspase Flavivirus
  4. Emricasan

Emricasan  (Synonyms: PF 03491390; IDN-6556)

製品番号: HY-10396 純度: 99.81%
COA 取扱説明書 Technical Support

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.

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CAS 番号 : 254750-02-2

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>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 135 在庫あり
Solution
10 mM * 1 mL in DMSO USD 135 在庫あり
Solid
5 mg $108 在庫あり
10 mg $180 在庫あり
25 mg $360 在庫あり
50 mg $540 在庫あり
100 mg $750 在庫あり
500 mg $1875 在庫あり
1 g $2950 在庫あり
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カスタマーレビュー

Based on 52 publication(s) in Google Scholar

Other Forms of Emricasan:

Emricasan 関連抗体

Top Publications Citing Use of Products

顧客検証

Apoptosis Analysis
WB
IF

    Emricasan purchased from MedChemExpress. Usage Cited in: Cell Death Differ. 2022 Aug;29(8):1486-1499.  [Abstract]

    Flow cytometry of CD4 and CD8 T cells expressing caspase activity in the absence (Med) or presence of Q-VD-Oph (Q-VD) (10 μM) (Top). Inhibition of caspase activity (preventive effect) in the presence of IDN-6556 (10 μM), VX-765 (10 μM), Q-VD and MCC950. Percentages were calculated as follows: (Med-Inh/Med)*100. Each dot represents one individual (Middle). Flow cytometry of CD4 and CD8 T cells expressing annexin V in the absence (Med) or presence of Q-VD (Bottom).

    Emricasan purchased from MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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 MedChemExpress. 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.

    Caspase アイソフォーム固有の製品をすべて表示:

    すべてのアイソフォームを表示
    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

    • 生物活性

    • プロトコル

    • 純度とドキュメンテーション

    • 参考文献

    • カスタマーレビュー

    製品説明

    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[1]

    Caspase

     

    Cellular Effect
    Cell Line Type Value Description References
    Jurkat IC50
    0.025 3
    Compound: 1
    Inhibitory concentration against JFas cells
    Inhibitory concentration against JFas cells
    		[PMID: 16250635]
    THP-1 IC50
    0.27 3
    Compound: 1
    Inhibitory concentration against THP-1 cells
    Inhibitory concentration against THP-1 cells
    		[PMID: 16250635]
    Jurkat IC50
    0.025 3
    Compound: 1
    Inhibitory concentration against JFas cells
    Inhibitory concentration against JFas cells
    		[PMID: 16250635]
    THP-1 IC50
    0.27 3
    Compound: 1
    Inhibitory concentration against THP-1 cells
    Inhibitory concentration against THP-1 cells
    		[PMID: 16250635]
    体外実験

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Emricasan 関連抗体
    体内実験

    Emricasan (PF 03491390; IDN-6556) is orally active that is retained in the liver for a 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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    臨床実験
    分子量

    569.50

    分子式

    C26H27F4N3O7
    CAS 番号
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    FC1=C(C(F)=C(C=C1F)F)OCC([C@@H](NC([C@@H](NC(C(NC2=C(C=CC=C2)C(C)(C)C)=O)=O)C)=O)CC(O)=O)=O
    輸送条件

    Room temperature in continental US; may vary elsewhere.
    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : 100 mg/mL (175.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始）

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    体積 （開始）

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    体内:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 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

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 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

      This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

      Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
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    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    純度とドキュメンテーション

    純度: 99.81%

    COA (247 KB) HNMR (272 KB) RP-HPLC (244 KB) LCMS (97 KB) Elemental Analysis Report (106 KB)

    取扱説明書 (2659 KB)
    参考文献
    動物実験
    [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.

    MedChemExpress (MCE) はこれらの方法の精度を確認していません。 こちらは参照専用です。
    参考文献

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.7559 mL 8.7796 mL 17.5593 mL 43.8982 mL
    5 mM 0.3512 mL 1.7559 mL 3.5119 mL 8.7796 mL
    10 mM 0.1756 mL 0.8780 mL 1.7559 mL 4.3898 mL
    15 mM 0.1171 mL 0.5853 mL 1.1706 mL 2.9265 mL
    20 mM 0.0878 mL 0.4390 mL 0.8780 mL 2.1949 mL
    25 mM 0.0702 mL 0.3512 mL 0.7024 mL 1.7559 mL
    30 mM 0.0585 mL 0.2927 mL 0.5853 mL 1.4633 mL
    40 mM 0.0439 mL 0.2195 mL 0.4390 mL 1.0975 mL
    50 mM 0.0351 mL 0.1756 mL 0.3512 mL 0.8780 mL
    60 mM 0.0293 mL 0.1463 mL 0.2927 mL 0.7316 mL
    80 mM 0.0219 mL 0.1097 mL 0.2195 mL 0.5487 mL
    100 mM 0.0176 mL 0.0878 mL 0.1756 mL 0.4390 mL
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    Emricasan Related Classifications

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    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます：C1V1 = C2V2

    濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
    × = ×
    C1   V1   C2   V2
    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.

    Keywords:

    Emricasan254750-02-2PF 03491390 IDN-6556PF03491390PF-03491390IDN6556IDN 6556IDN-6556CaspaseFlavivirusInhibitorinhibitorinhibit

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    製品名:
    Emricasan
    製品番号:
    HY-10396
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