SML2915
SAR-20347
≥98% (HPLC)
Synonym(s):
2-(2-Chloro-6-fluorophenyl)-5-(4-(morpholine-4-carbonyl)phenylamino)oxazole-4-carboxamide, 2-(2-Chloro-6-fluorophenyl)-5-[[4-(4-morpholinylcarbonyl)phenyl]amino]-4-oxazolecarboxamide, SAR 20347, SAR20347
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About This Item
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Quality Level
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Biochem/physiol Actions
SAR-20347 is an orally active, ATP-competitive, TYK2- and JAK1-selective tyrosine kinase inhibitor (IC50 = 13 nM/TYK2 & 59 nM/JAK1 vs. 0.88 μM/JAK2 & 1.44 μM/JAK3 with 10 μM ATP) that effectively inhibits cellular TYK2- (IL12-induced pSTAT4 IC50 = 107 nM/CD4+ cells, 126 nM/NK-92) and JAK1- (IL6-induced pSTAT3 IC50 = 345 nM/TF-1, 407 nM/CD14+ cells) mediated signaling with little affinity toward 72 other kinases. SAR-20347 suppresses IL22-induced serum amyloid A (by 44%; 50 mg/kg p.o. 30 min prior to 10 μg IL22 i.p.) and alleviates imiquimod-induced psoriasis-like dermatitis (30 min prior and 5 h post daily 62.5 mg 5% imiquimod cream) in mice in vivo.
Storage Class
11 - Combustible Solids
wgk_germany
WGK 3
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Journal of immunology (Baltimore, Md. : 1950), 193(7), 3278-3287 (2014-08-27)
Psoriasis is a chronic autoimmune disease affecting the skin and characterized by aberrant keratinocyte proliferation and function. Immune cells infiltrate the skin and release proinflammatory cytokines that play important roles in psoriasis. The Th17 network, including IL-23 and IL-22, has
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