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SAR-20347

SKU: orb1303059

Description

SAR-20347 is a potent small molecule inhibitor targeting the TYK2, JAK1, JAK2, and JAK3 kinases with respective IC50 values of 0.6, 23, 26, and 41 nM. This compound is a valuable research tool for investigating JAK/STAT signaling pathways in both cellular and animal models of autoimmune and inflammatory diseases.

Research Area

Cardiovascular Research, Epigenetics & Chromatin, Signal Transduction, Stem Cell & Developmental Biology

Images & Validation

Key Properties

CAS Number1450881-55-6
MW444.84
Purity99.77% (May vary between batches)
FormulaC21H18ClFN4O4
SMILESNC(=O)c1nc(oc1Nc1ccc(cc1)C(=O)N1CCOCC1)-c1c(F)cccc1Cl
TargetTyrosine Kinases,JAK
SolubilityDMSO:55 mg/mL (123.64 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.5 mM)

Bioactivity

Target IC50
JAK2:26nM|JAK1:23nM|TYK2:0.6 nM|JAK3:41 nM
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.
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).
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).
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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

SAR20347, SAR-20347, SAR 20347, TyrosineKinases, Tyrosine Kinases, TYK2, JAK, JAK1, Janus kinase, inhibit, JAK2, JAK3, Inhibitor

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Quality Guarantee

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Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Key Properties

No computed properties available.

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Protocol Information

SAR-20347 (orb1303059)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
¥ 910.00
1 ml x 10 mM (in DMSO)
¥ 1,560.00
5 mg
¥ 1,560.00
10 mg
¥ 2,080.00
25 mg
¥ 3,640.00
50 mg
¥ 5,460.00
100 mg
¥ 8,580.00
200 mg
¥ 11,830.00
DispatchUsually dispatched within 3-5 working days
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