Siponimod
Cat. No.：YN320577
CAS No. ：1230487-00-9
| 产品名称: | Siponimod |
| CAS No.: | 1230487-00-9 |
| Chemical Name: | 1-[[4-[(1E)-1-[[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]imino]ethyl]-2-ethylphenyl]methyl]-3-azetidinecarboxylic acid |
| Synonyms: | BAF-312 |
| 分子量: | 516.60 |
| 分子式: | C₂₉H₃₅F₃N₂O₃ |
| SMILES: | O=C(C1CN(CC2=CC=C(/C(C)=N/OCC3=CC=C(C4CCCCC4)C(C(F)(F)F)=C3)C=C2CC)C1)O |
| 存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
| 运输: | Room temperature in continental US; may vary elsewhere. |
| 产品描述: | Siponimod (BAF-312)是有效，选择性的鞘氨醇-1-磷酸 (S1P)受体调节剂。 它对S1P1和S1P5受体的选择性高于S1P2，S1P3和S1P4 (EC50分别为0.39，0.98，10,000，1,000和750 nM)。 |
| IC50和靶点: | [{name:"S1PR1:0.39 nM (EC50)"},{name: "S1PR5:0.98 nM (EC50)"},{name: "S1PR4:750 nM (EC50)"},{name: "S1PR3:>1000 nM (EC50)"},{name: "S1PR2:>10000 nM (EC50)"}] |
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Gergely, P., Nuesslein-Hildesheim, B., Guerini, D., et al.The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rateBr. J. Pharmacol.167(5),1035-1047(2012)
Pan, S., Gray, N.S., Gai, W., et al.Discovery of BAF312 (siponimod), a potent and selective S1P receptor modulatorACS Med. Chem. Lett.4(3),333-337(2013)
O'Sullivan, C., Schubart, A., Mir, A.K., et al.The dual S1PR1/S1PR5 drug BAF312 (siponimod) attenuates demyelination in organotypic slice culturesJ. Neuroinflammation13,31(2016)
Poirier, B., Briand, V., Kadereit, D., et al.A G protein-biased S1P1 agonist, SAR247799, protects endothelial cells without affecting lymphocyte numbersSci. Signal.13(634),eaax8050(2020)
