中文名:辛波莫德(BAF312)
英文名:Siponimod (BAF312)
纯度:Moligand™,≥98%
货号:S413720
Cas号:1230487-00-9
存储温度:-20°C储存,充氩
运输条件:超低温运输
产品介绍:
Information
Siponimod (BAF312) BAF312 (Siponimod) is a next-generation S1P receptor agonist, selective for S1P1 and S1P5 receptors with EC50 of 0.39 nM and 0.98 nM, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. Phase 3.
Targets
S1P1 receptor ; S1P5 receptor 0.39 nM(EC50); 0.98 nM(EC50)
In vitro
BAF312 (Siponimod) is a potent and selective S1P receptor agonist, with EC50 of 0.39 nM and 0.98 nM for S1P1 and S1P5receptors, exhibits >1000-fold selectivity over S1P2, S1P3 and S1P4 receptors. BAF312 (1 h at 1 μM) promotes prominent internalization of S1P1 receptors by 91%.
In vivo
BAF312 effectively suppresses encephalomyelitis (EAE) in rats by internalizing S1P1 receptors, rendering them insensitive to the egress signal from lymph nodes. BAF312 significantly reduces clinical scores when dosed prophylactically or therapeutically in mice at 0.3 mg/kg.
Cell Research(from reference)
Cell lines:CHO
Concentrations:~1 μM
Incubation Time:1 h
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关键字: 3-Azetidinecarboxylic acid, 1-[[4-[(1E)-1-[[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]imino]ethyl]-2-ethylphenyl]methyl]- ; (Z)-4-Cyano-5-((3,5-dichloropyridin-4-yl)thio)-N-(4-(methylsulfonyl)phenyl)thiophene-2-carbimidic acid ; BAF-312(SiponiMod)
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