2. Immunology/Inflammation
  3. Cyclic GMP-AMP Synthase
  4. PF-06928215

PF-06928215 is a cGAS (cyclic GMP-AMP Synthase) inhibitor with an IC50 of 4.9 μΜ. PF-06928215 has a high binding affinity of 0.2 μM (Kd).

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

PF-06928215 Chemical Structure

PF-06928215 Chemical Structure

CAS No. : 2378173-15-8

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 254 In-stock
Solution
10 mM * 1 mL in DMSO USD 254 In-stock
Solid
5 mg USD 231 In-stock
10 mg USD 340 In-stock
25 mg USD 640 In-stock
50 mg USD 960 In-stock
100 mg USD 1400 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

PF-06928215 Related Antibodies

Top Publications Citing Use of Products

    PF-06928215 purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2022 Nov 23;106577.  [Abstract]

    PF-06928215 (4, 20, 100 μM) and cGAMP (0.4, 2, 10 μM) dose-dependently reduce bindings of Biotin-Flu to cGAS and STING, in HEK293T cells transfected with Flag-tagged STING and Flag-tagged cGAS plasmids.

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PF-06928215 is a cGAS (cyclic GMP-AMP Synthase) inhibitor with an IC50 of 4.9 μΜ. PF-06928215 has a high binding affinity of 0.2 μM (Kd)[1].

    IC50 & Target

    IC50: 4.9 μM (cGAS)[1]
    Kd: 0.2 μM[1]
    In Vitro

    PF-06928215 displays no activity in cellular cGAS assays measuring dsDNA-induced IFN-beta expression[1].

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

    PF-06928215 Related Antibodies
    Molecular Weight

    380.40

    Formula

    C20H20N4O4
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    OC1=CC(C2=CC=CC=C2)=NC3=C(C(N[C@H]4CCCC[C@H]4C(O)=O)=O)C=NN13
    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 : 33.33 mg/mL (87.62 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 2.6288 mL 13.1441 mL 26.2881 mL
    5 mM 0.5258 mL 2.6288 mL 5.2576 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.

    • Molarity Calculator

    • Dilution Calculator

    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: ≥ 1.43 mg/mL (3.76 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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: ≥ 1.43 mg/mL (3.76 mM); Clear solution

      This protocol yields a clear solution of ≥ 1.43 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (14.3 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.
    Purity & Documentation

    Purity: 99.69%

    COA (258 KB) HNMR (306 KB) LCMS (268 KB)

    Handling Instructions (2659 KB)
    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, 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 2.6288 mL 13.1441 mL 26.2881 mL 65.7203 mL
    5 mM 0.5258 mL 2.6288 mL 5.2576 mL 13.1441 mL
    10 mM 0.2629 mL 1.3144 mL 2.6288 mL 6.5720 mL
    15 mM 0.1753 mL 0.8763 mL 1.7525 mL 4.3814 mL
    20 mM 0.1314 mL 0.6572 mL 1.3144 mL 3.2860 mL
    25 mM 0.1052 mL 0.5258 mL 1.0515 mL 2.6288 mL
    30 mM 0.0876 mL 0.4381 mL 0.8763 mL 2.1907 mL
    40 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6430 mL
    50 mM 0.0526 mL 0.2629 mL 0.5258 mL 1.3144 mL
    60 mM 0.0438 mL 0.2191 mL 0.4381 mL 1.0953 mL
    80 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8215 mL
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    PF-06928215 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.

    Keywords:

    PF-069282152378173-15-8PF06928215PF 06928215Cyclic GMP-AMP SynthasecGASInhibitorinhibitorinhibit

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    Product Name:
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    Cat. No.:
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