SAR-20347

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

SAR-20347 (SAR20347) 是一种有效的选择性 JAK1 和 Tyk2 抑制剂，在 TR-FRET 测定中 IC50 分别为 59 和 13 nM。

SAR-20347 (SAR20347) is a potent, selective inhibitor of JAK1 and Tyk2 with IC50 of 59 and 13 nM in TR-FRET assays, shows selectivity against JAK2 and JAK3 (IC50>800 nM); potently inhibits IL-12-mediated STAT4 phosphorylation with IC50 of 126 nM, inhibits JAK1-mediated IL-6 pSTAT3 signaling with IC50 of 345 nM in TF-1 and 407 nM in CD4+ cells, poorly inhibits JAK2 mediated STAT5 phosphorylation with IC50 of >1 uM; ameliorates imiquimod-induced psoriasis-like dermatitis in vivo.

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.

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.

SAR20347

Angiogenesis

JAK

JAK1|JAK2|JAK3|TYK2

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1450881-55-6

444.847

C21H18ClFN4O4

>98% (HPLC)

DMSO: 100 mg/mL （ < 1 mg/ml refers to the product slightly soluble or insoluble )

O=C(C1=C(NC2=CC=C(C(N3CCOCC3)=O)C=C2)OC(C4=C(F)C=CC=C4Cl)=N1)N

2-(2-chloro-6-fluorophenyl)-5-((4-(morpholine-4-carbonyl)phenyl)amino)oxazole-4-carboxamide

(-20℃)

With Ice Pack

≥ 2 years