Siponimod

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Chemical Structure| 1230487-00-9 同义名 : 辛波莫德(BAF312) ;BAF-312
CAS号 : 1230487-00-9
货号 : A588237
分子式 : C29H35F3N2O3
纯度 : 99%+
分子量 : 516.595
MDL号 : MFCD26142651
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(58.07 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 BAF312, also called Siponimod, is a selective, potent and brain-penetrant S1P receptor modulator used to treat multiple sclerosis, with EC50 values of 0.4nM and 5nM for S1P1 and S1P3 in GTPγS binding assay, respectively. Oral administration of 1mg/kg BAF312 markedly reduced peripheral lymphocyte count, a pharmacodynamic biomarker in autoimmune diseases for S1P1 activation, by 88% in Lewis rats at 8h post treatment, with a shorter duration of action than FTY720[1]. BAF312 also showed effect on S1P5 with EC50 of 0.98nM. Treatment with BAF312 at concentration of 1μM for 1h promote internalization of S1P1 receptors in CHO cells expressed myc-tagged human S1P1 receptors. Daily oral administration of BAF312 at dose of 0.3 or 3mg/kg for 24 days dose-dependently suppressed ongoing disease symptoms in rat EAE. BAF312 concentration-dependently activated the GIRK channel via S1P1 in atrial myocytes with EC50 value of 15.8nM[2].
作用机制 BAF312 is structurally based on FTY720.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.94mL

0.39mL

0.19mL

9.68mL

1.94mL

0.97mL

19.36mL

3.87mL

1.94mL
参考文献

[1]Pan S, Gray NS, et al. Discovery of BAF312 (Siponimod), a Potent and Selective S1P Receptor Modulator. ACS Med Chem Lett. 2013 Jan 4;4(3):333-7.

[2]Gergely P, Nuesslein-Hildesheim B, 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.

[3]Fryer RM, Muthukumarana A, et al. The clinically-tested S1P receptor agonists, FTY720 and BAF312, demonstrate subtype-specific bradycardia (S1P₁) and hypertension (S1P₃) in rat. PLoS One. 2012;7(12):e52985.

[4]Siponimod