Siponimod|1230487-00-9|(辛波莫德; BAF-312)-陌孚医药/Medlife

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Siponimod (Synonyms: 辛波莫德; BAF-312)

目录号: PL02609 纯度: ≥98%

CAS No. :1230487-00-9

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中文名称	Siponimod
英文名称	Siponimod
英文别名	BAF-312(SiponiMod);1-(4-[1-[(E)-4-Cyclohexyl-3-trifluoromethyl-benzyloxyimino]-ethyl]-2-ethyl-benzyl)-azetidine-3-carboxylic acid;BAF 312;Siponimod;BAF312 (Siponimod);BAF312;RR6P8L282I;Siponimod [INN];3-Azetidinecarboxylic acid, 1-((4-((1E)-1-(((4-cyclohexyl-3-(trifluoromethyl)phenyl)methoxy)imino)ethyl)-2-ethylphenyl)methyl)-;1-[[4-[(E)-N-[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]-C-methylcarbonimidoyl]-2-ethylphenyl]methyl]azetidine-3-carboxylic acid;Siponimod [WHO-DD];3-Azetidinecarboxylic acid, 1-[[4-[(1E)-1-[[[4-cyclohexyl-3-(trifluoromethyl)phenyl]methoxy]imino]ethyl]
Cas No.	1230487-00-9
分子式	C₂₉H₃₅F₃N₂O₃
分子量	516.60
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Siponimod (BAF-312) 是一种口服有效、选择性的鞘脂 S1P 受体调节剂。Siponimod 对 S1P₁ 和 S1P₅ 受体的选择性高于 S1P₂、S1P₃ 和 S1P₄，EC₅₀ 分别为 0.39，0.98，>10000，>1000 和 750 nM。Siponimod 可用于多发性硬化症 (MS) 的研究。

生物活性

Siponimod (BAF-312) is an orally active and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod is selective for S1P 1 and S1P 5 over S1P 2 , S1P 3 , and S1P 4 , with EC 50 s of 0.4, 0.98, >10000, >1000, and 750 nM, respectively. Siponimod can be used for multiple sclerosis (MS) research.

性状

Solid

IC50 & Target[1][2]

S1PR1 0.39 nM (EC50) S1PR5 0.98 nM (EC

体外研究(In Vitro)

Siponimod (compound 32) exhibits selectivity to S1P1 and S1P5, and spares activity on the S1P2, S1P3 and S1P4 receptors.
Siponimod (1 mM; 0-1 h) promotes internalization of S1P1 receptors, results 94% S1P1 receptors localized intracellularly at 1 h.
Siponimod (0.001 nM-1 μM; 1 h) activates the GIRK channel in atrial myocytes, with an EC50 value of 15.8 nM in CHO cell line CCL-61.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Siponimod (1 g/kg; i.v.; single dose) shows low to moderate in monkey, but high in rat in metabolism studies with liver microsomes. The absolute bioavailability is 50 and 71% in the rat and monkey, respectively, indicating no major presystemic first pass metabolism.
Siponimod (0.3, 3 mg/kg; p.o.; once daily; 23 d) suppresses experimental autoimmune encephalomyelitis (EAE) in rats by internalizing S1P1 receptors.
Parmacokinetics of Siponimod in rats and monkey

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Gergely P, et al. The selective sphingosine 1-phosphate receptor modulator BAF312 redirects lymphocyte distribution and has species-specific effects on heart rate. Br J Pharmacol. 2012 Nov;167(5):1035-47.
[2]. Pan S, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013 Jan 4;4(3):333-7.

溶解度数据	In Vitro: DMSO : ≥ 30 mg/mL (58.07 mM)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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