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。

SAR-20347 is an inhibitor of TYK2, JAK1, JAK2 and JAK3 with IC 50 s of 0.6, 23, 26 and 41 nM, respectively.

Solid

JAK1 23 nM (IC50) JAK2 26 nM (IC50

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. has not independently confirmed the accuracy of these methods. They are for reference only.

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. has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

Powder -20°C 3 years；4°C 2 years

[1]. Works MG, et al. Inhibition of TYK2 and JAK1 ameliorates imiquimod-induced psoriasis-like dermatitis by inhibiting IL-22 and the IL-23/IL-17 axis. J Immunol. 2014 Oct 1;193(7):3278-87.

In Vitro: DMSO : 100 mg/mL (224.80 mM; Need ultrasonic and warming)配制储备液