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SAR-20347

🥰Excellent
Catalog No. T4210Cas No. 1450881-55-6
Alias SAR20347

SAR-20347 is an inhibitor of TYK2 and JAK1/2/3, with IC50 values of 0.6 nM, 23 nM, 26 nM, and 41 nM, respectively.

SAR-20347

SAR-20347

🥰Excellent
Purity: 99.77%
Catalog No. T4210Alias SAR20347Cas No. 1450881-55-6
SAR-20347 is an inhibitor of TYK2 and JAK1/2/3, with IC50 values of 0.6 nM, 23 nM, 26 nM, and 41 nM, respectively.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$30In StockIn Stock
5 mg$73In StockIn Stock
10 mg$118In StockIn Stock
25 mg$239In StockIn Stock
50 mg$372In StockIn Stock
100 mg$619In StockIn Stock
200 mg$862In StockIn Stock
1 mL x 10 mM (in DMSO)$80In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.77%
Appearance:Solid
Color:White to Yellow
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Product Introduction

Bioactivity
Description
SAR-20347 is an inhibitor of TYK2 and JAK1/2/3, with IC50 values of 0.6 nM, 23 nM, 26 nM, and 41 nM, respectively.
Targets&IC50
JAK2:26nM, JAK1:23nM, TYK2:0.6 nM, JAK3:41 nM
In vitro
SAR-20347 effectively inhibits IL-12-mediated STAT4 phosphorylation (TYK2-dependent, IC50: 126 nM) when NK-92 cells are stimulated with IL-12. In the culture media, cells without IL-12 have no measurable IFN-γ, while cells incubated with IL-12 and SAR-20347 demonstrate dose-dependent inhibition of IFN-γ production. SAR-20347 (maximum effect: 5 μM) dose-dependently inhibits the production of secreted embryonic alkaline phosphatase (SEAP).
In vivo
Compared to vehicle-treated animals, SAR-20347 (60 mg/kg) inhibits the production of IFN-γ in the serum by 91%, demonstrating that SAR-20347 can inhibit TYK2 signaling in vivo. SAR-20347 markedly reduces IL-17 production as measured by average signal intensity, consistent with the gene expression analysis.
Kinase Assay
Kinases are prepared in Base Reaction Buffer (20 mM Hepes pH 7.5, 10 mM MgCl2, 1 mM EGTA, 0.02% Brij35, 0.02 mg/mL BSA, 0.1 mM Na3VO4, 2 mM DTT, 1% DMSO) and substrate is added with 1.5 mM CaCl2, 16 μg/mL Calmodulin, and 2 mM MnCl2. Varying concentrations of SAR-20347 in DMSO are added to the kinase reaction along with 10 μM 33P-ATP (activity 0.01 μCi/μL final) for IC50 determination[1].
Cell Research
Cells are plated in a 96-well v-bottom plate in starvation medium, incubated with SAR-20347 (0.5% DMSO) for 20 minutes at 37°C, 5% CO2, and stimulated with individual cytokines. P-STAT levels are measured in duplicate using MSD plates following the manufacturer's instructions (MSD)[1].
Animal Research
Female 7 to 9-week old C57BL/6 mice are used. Mice are administered vehicle or 50 mg/kg SAR-20347 by oral gavage 30 minutes prior to application of 62.5 mg 5% imiquimod cream or control cream. Another dose of vehicle or 50 mg/kg SAR-20347 is given 5.5 hours following the first dose. This treatment is repeated for 5 days and on day 3 and 4, animals are injected with 100 uL saline to prevent dehydration. On the 6th day, the animals are euthanized and photographs are taken[1].
SynonymsSAR20347
Chemical Properties
Molecular Weight444.84
FormulaC21H18ClFN4O4
Cas No.1450881-55-6
SmilesNC(=O)c1nc(oc1Nc1ccc(cc1)C(=O)N1CCOCC1)-c1c(F)cccc1Cl
Relative Density.1.445 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 55 mg/mL (123.64 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (4.5 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.2480 mL11.2400 mL22.4800 mL112.4000 mL
5 mM0.4496 mL2.2480 mL4.4960 mL22.4800 mL
10 mM0.2248 mL1.1240 mL2.2480 mL11.2400 mL
20 mM0.1124 mL0.5620 mL1.1240 mL5.6200 mL
50 mM0.0450 mL0.2248 mL0.4496 mL2.2480 mL
100 mM0.0225 mL0.1124 mL0.2248 mL1.1240 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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