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SAR-20347

CAS No. : 1450881-55-6

MCE 站：SAR-20347

产品活性：SAR-20347 是 TYK2，JAK1，JAK2 和 JAK3 的抑制剂，其 IC₅₀ 值分别为 0.6, 23, 26 和 41 nM。

研究领域：Epigenetics  |  Stem Cell/Wnt  |  JAK/STAT Signaling

作用靶点：JAK

In Vitro: When NK-92 cells are stimulated with IL-12, SAR-20347 potently inhibits IL-12-mediated STAT4 phosphorylation, a TYK2-dependent event, with an IC₅₀ of 126 nM. SAR-20347 demonstrates a selectivity of TYK2>JAK1>JAK2>JAK3. Cells without IL-12 in the culture media have no measureable IFN-γ, while cells incubated with IL-12 and SAR-20347 demonstrate dose-dependent inhibition of IFN-γ production. SAR-20347 dose-dependently inhibits the production of secreted embryonic alkaline phosphatase (SEAP) with greatest inhibition occurring with 5 μM of SAR-20347 in these experiments.

In Vivo: 60 mg/kg SAR-20347 inhibits the production of IFN-γ in the serum by 91% compare to vehicle-treated animals, demonstrating that SAR-20347 can inhibit TYK2 signaling in vivo. SAR-20347 treatment significantly reduces IL-17 production as measured by average signal intensity, consistent with the gene expression analysis.

相关产品：Bioactive Compound Library Plus  |  Epigenetics Compound Library  |  Immunology/Inflammation Compound Library  |  JAK/STAT Compound Library  |  Kinase Inhibitor Library  |  Stem Cell Signaling Compound Library  |  Anti-Cancer Compound Library  |  Anti-Aging Compound Library  |  Differentiation Inducing Compound Library  |  Reprogramming Compound Library  |  Anti-Breast Cancer Compound Library  |  Anti-Pancreatic Cancer Compound Library  |  Anti-Blood Cancer Compound Library  |  AG490  |  Upadacitinib  |  AT9283  |  Gandotinib  |  Lestaurtinib  |  Cucurbitacin I  |  Oclacitinib maleate  |  JANEX-1  |  XL019  |  Atractylenolide I  |  FLLL32  |  LFM-A13  |  Brevilin A  |  ZM39923 hydrochloride  |  Ginsenoside Rk1  |  WHI-P154  |  Curculigoside  |  FM-381  |  RO8191  |  Reticuline  |  TCS 21311  |  WHI-P97  |  Coumermycin A1  |  Delphinidin chloride  |  Ilginatinib maleate  |  Protosappanin A  |  Dehydrocrenatidine  |  FM-479  |  NSC 33994

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