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Description: SAR-20347 is a novel and potent small molecule inhibitor with specificity for JAK1 and tyrosine kinase 2 (TYK2) over other JAK family members. In cellular assays, SAR-20347 dose dependently (1 nM-10 μM) inhibited JAK1- and/or TYK2-dependent signaling from the IL-12/IL-23, IL-22, and IFN-α receptors. In vivo, TYK2 mutant mice or treatment of wild-type mice with SAR-20347 significantly reduced IL-12-induced IFN-γ production and IL-22-dependent serum amyloid A to similar extents, indicating that, in these models, SAR-20347 is probably acting through inhibition of TYK2. In an imiquimod-induced psoriasis model, the administration of SAR-20347 led to a striking decrease in disease pathology, including reduced activation of keratinocytes and proinflammatory cytokine levels compared with both TYK2 mutant mice and wild-type controls. Taken together, these data indicate that targeting both JAK1- and TYK2-mediated cytokine signaling is more effective than TYK2 inhibition alone in reducing psoriasis pathogenesis.
References: J Immunol. 2014 Oct 1;193(7):3278-87.
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
Purity ≥98%
COA
MSDS
SAR20347 alters in vitro development of mouse T helper subsets. J Immunol. 2014 Oct 1;193(7):3278-87.
SAR-20347 inhibits TYK2- and JAK1-mediated IL-12 and IFN-α signaling. J Immunol. 2014 Oct 1;193(7):3278-87.
SAR-20347 reduces imiquimod-induced inflammation and keratinocyte cell numbers. J Immunol. 2014 Oct 1;193(7):3278-87.
SAR-20347 reduces imiquimod-induced inflammation and antimicrobial peptide production. J Immunol. 2014 Oct 1;193(7):3278-87.
SAR-20347 treatment and TYK2 mutant mice show reduced IL-17 and Vγ3. J Immunol. 2014 Oct 1;193(7):3278-87.
Proposed mechanism of action of SAR-20347 in ameliorating psoriasis-like symptoms. J Immunol. 2014 Oct 1;193(7):3278-87.