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质量水平
方案
≥98% (HPLC)
表单
powder
颜色
white to beige
溶解性
DMSO: 2 mg/mL, clear
储存温度
−20°C
SMILES字符串
Fc1c(c(ccc1)Cl)c2nc(c([o]2)Nc3ccc(cc3)C(=O)N4CCOCC4)C(=O)N
InChI
1S/C21H18ClFN4O4/c22-14-2-1-3-15(23)16(14)19-26-17(18(24)28)20(31-19)25-13-6-4-12(5-7-13)21(29)27-8-10-30-11-9-27/h1-7,25H,8-11H2,(H2,24,28)
InChI key
HEDPDFHTQKEORT-UHFFFAOYSA-N
生化/生理作用
Orally active, ATP-competitive, TYK2- and JAK1-selective tyrosine kinase inhibitor in vitro and in vivo.
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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
历史批次信息供参考:
Xia Kang et al.
Cell communication and signaling : CCS, 16(1), 42-42 (2018-07-22)
Chronic muscle injury is characteristics of fatty infiltration and fibrosis. Recently, fibro/adipogenic progenitors (FAPs) were found to be indispensable for muscular regeneration while were also responsible for fibrosis and fatty infiltration in muscle injury. Many myokines have been proven to
Ming-Ming Hu et al.
Cell research, 29(3), 193-205 (2019-01-18)
The mechanisms on metabolic regulation of immune responses are still elusive. We show here that viral infection induces immediate-early NF-κB activation independent of viral nucleic acid-triggered signaling, which triggers a rapid transcriptional induction of bile acid (BA) transporter and rate-limiting
Melissa G Works et al.
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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