Q-VD-OPh [1135695-98-5]

Referência HY-12305-5mg

Tamanho : 5mg

Marca : MedChemExpress

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Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.

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Q-VD-OPh Chemical Structure

Q-VD-OPh Chemical Structure

CAS No. : 1135695-98-5

This product is a controlled substance and not for sale in your territory.

Based on 59 publication(s) in Google Scholar

Other Forms of Q-VD-OPh:

  • (R)-Q-VD-OPh Obtenir un devis

    Q-VD-OPh purchased from MedChemExpress. Usage Cited in: Cancer Sci. 2019 May;110(5):1746-1759.  [Abstract]

    Cells are treated with RA in the presence or absence of the caspase inhibitor Q-VD-OPh, and cleaved caspase-3 and caspase-8 and total and cleaved PARP were analyzed.

    Voir tous les produits spécifiques à Isoform Caspase:

    Voir toutes les isoformes
    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

    Voir tous les produits spécifiques à Isoform HIV:

    Voir toutes les isoformes
    HIV HIV-1 HIV-2
    Description

    Q-VD-OPh is an irreversible pan-caspase inhibitor with potent antiapoptotic properties; inhibits caspase 7 with an IC50 of 48 nM and 25-400 nM for other caspases including caspase 1, 3, 8, 9, 10, and 12. Q-VD-OPh can inhibits HIV infection. Q-VD-OPh is able to cross the blood-brain barrier.

    IC50 & Target[1]

    Caspase-7

    48 nM (IC50)

    Caspase-3

    25-400 nM (IC50)

    Caspase-1

    25-400 nM (IC50)

    Caspase-8

    25-400 nM (IC50)

    Caspase-9

    25-400 nM (IC50)

    Caspase-10

    25-400 nM (IC50)

    Caspase-12

    25-400 nM (IC50)

    In Vitro

    Q-VD-OPh is a potent inhibitor of caspase-7 with an IC50 of 48 nM utilizing a cell-free assay consisting of human recombinant caspase-7, Q-VD-OPh, and the substrate AMC-DEVD-pNa[1]. Q-VD-OPh fully inhibits caspase-3 and -7 activity at 0.05 μM. Caspase-8 is also inhibited at low Q-VD-OPh concentrations. The cleavage of PARP-1 is fully prevented at 10 μM Q-VD-OPh. DNA fragmentation and disruption of the cell membrane functionality are both prevented at 2 μM Q-VD-OPh[2]. Q-VD-OPh is significantly more effective in preventing apoptosis than the widely used inhibitors, ZVAD-fmk and Boc-D-fmk, and is also equally effective in preventing apoptosis mediated by the three major apoptotic pathways, caspase 9/3, caspase 8/10, and caspase12. Q-VD-OPh is not toxic to cells even at extremely high concentrations[3]. QVD is also able to increase the expression of differentiation markers in acute myeloid leukemia (AmL) blasts. QVD alone or combined with VDDs increases differentiation and HPK1-cJun signaling in AmL cell context-dependent manner[4].

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

    In Vivo

    Chronic treatment with Q-VD-OPh prevents caspase-7 activation and limits the pathological changes associated with tau, including caspase cleavage. Q-VD-OPh could be a potential therapeutic compound for the treatment of Alzheimer's disease[1].

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

    Masse moléculaire

    513.49

    Formule

    C26H25F2N3O6

    CAS No.

    1135695-98-5

    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(O)C[C@H](NC([C@@H](NC(C1=NC2=CC=CC=C2C=C1)=O)C(C)C)=O)C(COC3=C(F)C=CC=C3F)=O

    Livraison

    Room temperature in continental US; may vary elsewhere.

    Stockage
    Powder -20°C 3 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvant et solubilité
    In Vitro: 

    DMSO : 100 mg/mL (194.75 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 1.9475 mL 9.7373 mL 19.4746 mL
    5 mM 0.3895 mL 1.9475 mL 3.8949 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Calculateur de molarité

    • Calculateur de dilution

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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: ≥ 2.08 mg/mL (4.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.05 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    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.
    Pureté et documentation

    Purity: 99.78%

    Références
    • [1]. Rohn TT, et al. Caspase activation in transgenic mice with Alzheimer-like pathology: results from a pilot study utilizing the caspase inhibitor, Q-VD-OPh. Int J Clin Exp Med. 2009 Nov 5;2(4):300-8.  [Content Brief]

      [2]. Kuzelová K, et al. Dose-dependent effects of the caspase inhibitor Q-VD-OPh on different apoptosis-related processes. J Cell Biochem. 2011 Nov;112(11):3334-42.  [Content Brief]

      [3]. Caserta TM, et al. Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties. Apoptosis. 2003 Aug;8(4):345-52.  [Content Brief]

      [4]. Chen-Deutsch X, et al. Leuk Res. 2012 Jul;36(7):884-8. The pan-caspase inhibitor Q-VD-OPh has anti-leukemia effects and can interact with vitamin D analogs to increase HPK1 signaling in AML cells.  [Content Brief]

      [5]. Laforge M, et al. The anti-caspase inhibitor Q-VD-OPH prevents AIDS disease progression in SIV-infected rhesus macaques. J Clin Invest. 2018 Apr 2;128(4):1627-1640.  [Content Brief]

    Administration animale
    [1]

    Mouse: Stock solutions of Q-VD-OPh are prepared in DMSO and diluted in sterile PBS solution prior to injection. A final concentration of 10 mg/kg is chosen indicating neuroprotection at this concentration of Q-VD-OPh. Three-month old mice are divided into two groups: control, vehicle (n=3) or treated (n=2). Mice are injected i.p. three times a week with either Q-VD-OPh or vehicle for a total time period of 3 months[1].

    MCE n'a pas confirmé de manière indépendante l'exactitude de ces méthodes. Ils sont pour référence seulement.

    Références
    • [1]. Rohn TT, et al. Caspase activation in transgenic mice with Alzheimer-like pathology: results from a pilot study utilizing the caspase inhibitor, Q-VD-OPh. Int J Clin Exp Med. 2009 Nov 5;2(4):300-8.  [Content Brief]

      [2]. Kuzelová K, et al. Dose-dependent effects of the caspase inhibitor Q-VD-OPh on different apoptosis-related processes. J Cell Biochem. 2011 Nov;112(11):3334-42.  [Content Brief]

      [3]. Caserta TM, et al. Q-VD-OPh, a broad spectrum caspase inhibitor with potent antiapoptotic properties. Apoptosis. 2003 Aug;8(4):345-52.  [Content Brief]

      [4]. Chen-Deutsch X, et al. Leuk Res. 2012 Jul;36(7):884-8. The pan-caspase inhibitor Q-VD-OPh has anti-leukemia effects and can interact with vitamin D analogs to increase HPK1 signaling in AML cells.  [Content Brief]

      [5]. Laforge M, et al. The anti-caspase inhibitor Q-VD-OPH prevents AIDS disease progression in SIV-infected rhesus macaques. J Clin Invest. 2018 Apr 2;128(4):1627-1640.  [Content Brief]

    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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 1.9475 mL 9.7373 mL 19.4746 mL 48.6864 mL
    5 mM 0.3895 mL 1.9475 mL 3.8949 mL 9.7373 mL
    10 mM 0.1947 mL 0.9737 mL 1.9475 mL 4.8686 mL
    15 mM 0.1298 mL 0.6492 mL 1.2983 mL 3.2458 mL
    20 mM 0.0974 mL 0.4869 mL 0.9737 mL 2.4343 mL
    25 mM 0.0779 mL 0.3895 mL 0.7790 mL 1.9475 mL
    30 mM 0.0649 mL 0.3246 mL 0.6492 mL 1.6229 mL
    40 mM 0.0487 mL 0.2434 mL 0.4869 mL 1.2172 mL
    50 mM 0.0389 mL 0.1947 mL 0.3895 mL 0.9737 mL
    60 mM 0.0325 mL 0.1623 mL 0.3246 mL 0.8114 mL
    80 mM 0.0243 mL 0.1217 mL 0.2434 mL 0.6086 mL
    100 mM 0.0195 mL 0.0974 mL 0.1947 mL 0.4869 mL
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    Q-VD-OPh Related Classifications

    Help & FAQs

    Keywords:

    Q-VD-OPh1135695-98-5QVD-OPH Quinoline-Val-Asp-DifluorophenoxymethylketoneCaspaseHIVHuman immunodeficiency virusInhibitorinhibitorinhibit

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