1. MAPK/ERK Pathway Apoptosis
  2. MAP3K Apoptosis
  3. Selonsertib

Selonsertib  (Synonyms: GS-4997)

Cat. No.: HY-18938 Purity: 99.05%
COA Handling Instructions

Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.

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

Selonsertib Chemical Structure

Selonsertib Chemical Structure

CAS No. : 1448428-04-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 101 In-stock
Solution
10 mM * 1 mL in DMSO USD 101 In-stock
Solid
5 mg USD 92 In-stock
10 mg USD 121 In-stock
50 mg USD 270 In-stock
100 mg USD 490 In-stock
200 mg USD 704 In-stock
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Customer Review

Based on 14 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Selonsertib purchased from MedChemExpress. Usage Cited in: Phytother Res. 2022 Nov 24.  [Abstract]

    Selonsertib (5 µM) alleviates TMAO-induced morphological changes and improve cellular viability in RTEC cells.

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    • Biological Activity

    • Purity & Documentation

    • References

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    Description

    Selonsertib (GS-4997), an orally bioavailable, selective apoptosis signal-regulating kinase 1 (ASK1) inhibitor with a pIC50 of 8.3, has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis.

    IC50 & Target[1]

    ASK1

    8.3 (pIC50)

    In Vitro

    Selonsertib (GS-4997) is a clinical stage ASK1 inhibitor, which has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis[1]. Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor that competes with ATP in the ASK1 catalytic kinase domain[2].

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

    Clinical Trial
    Molecular Weight

    445.49

    Formula

    C24H24FN7O

    CAS No.
    Appearance

    Solid

    Color

    Off-white to light yellow

    SMILES

    O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(N4C=C(C5CC5)N=C4)=C(C)C=C3F

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 31 mg/mL (69.59 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.2447 mL 11.2236 mL 22.4472 mL
    5 mM 0.4489 mL 2.2447 mL 4.4894 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, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

    • 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)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    C2

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    Volume (final)

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    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:  5% DMSO    95% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.62 mg/mL (5.88 mM); Clear solution

    • Protocol 2

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

      Solubility: ≥ 2.08 mg/mL (4.67 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.
    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.
    Purity & Documentation

    Purity: 99.05%

    References

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

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.2447 mL 11.2236 mL 22.4472 mL 56.1180 mL
    5 mM 0.4489 mL 2.2447 mL 4.4894 mL 11.2236 mL
    10 mM 0.2245 mL 1.1224 mL 2.2447 mL 5.6118 mL
    15 mM 0.1496 mL 0.7482 mL 1.4965 mL 3.7412 mL
    20 mM 0.1122 mL 0.5612 mL 1.1224 mL 2.8059 mL
    25 mM 0.0898 mL 0.4489 mL 0.8979 mL 2.2447 mL
    30 mM 0.0748 mL 0.3741 mL 0.7482 mL 1.8706 mL
    40 mM 0.0561 mL 0.2806 mL 0.5612 mL 1.4029 mL
    50 mM 0.0449 mL 0.2245 mL 0.4489 mL 1.1224 mL
    60 mM 0.0374 mL 0.1871 mL 0.3741 mL 0.9353 mL
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    Selonsertib Related Classifications

    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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    Product Name:
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    Cat. No.:
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