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My CartCAS：1230487-00-9
Storage：Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year
Purity：≥98%
Appearance：White to off-white Solid
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| CAS | 1230487-00-9 |
| Name | Siponimod |
| Molecular Formula | C29H35F3N2O3 |
| Molecular Weight | 516.6 |
| Solubility | Soluble in DMSO ≥5mg/mL |
| Purity | ≥98% |
| Appearance | White to off-white Solid |
| Storage | Powder:-20℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| MDL | MFCD26142651 |
| SMILES | O=C(C1CN(CC2=CC=C(/C(C)=N/OCC3=CC=C(C4CCCCC4)C(C(F)(F)F)=C3)C=C2CC)C1)O |
| Target Point | S1P Receptor（S1P1，S1P5） |
| Passage | GPCR & G Protein |
| Background | Siponimod is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. |
| Biological Activity | BAF312 (Siponimod)是一种二代S1P受体激动剂，选择性作用于S1P1和S1P5受体，EC50分别为0.39 nM和0.98 nM，比作用于S1P2， S1P3和S1P4受体选择性高1000倍以上。[1-3] |
| IC50 | S1P1 receptor: 0.39nM(EC50) [1] |
| In Vitro | BAF312(Siponimod)是有效的选择性S1P受体激动剂，对S1P1和S1P5受体的EC50 为 0.39 nM 和 0.98 nM，表现出高于S1P2，S1P3 和 S1P4受体1000多倍的选择性。[1] BAF312(1 μM下1小时)促进91%S1P1受体的显著内化。[2] |
| In Vivo | BAF312通过内化S1P1受体，使其对淋巴结的出口信号不敏感，从而有效抑制大鼠脑脊髓炎(EAE)。[1] BAF312以预防或治疗剂量0.3毫克/千克在小鼠体内显著降低临床评分。[3] |
| Cell Experiment | Animal Models: 脑脊髓炎(EAE)大鼠模型; Dosages: 0.03，0.3 和 3 毫克/千克; Administration: 口服灌胃[1] |
| Animal Experiment | 激动剂介导的S1P1受体在CHO细胞中的内化作用，通过流式细胞术Myc标记的hS1P1细胞与激动剂，PBS清洗后，在标准培养基中于37°C下培育1小时进行分析。等分试剂在冰上保存3小时，另一等分试样在37°C下在培养基(不含激动剂)中放置3(或12)小时。随后细胞与4微克/毫升单克隆鼠抗C-myc IgG1抗体或同型对照小鼠IgG1在4°C下培养60分钟，随后用1微克/毫升Alexa488标记的山羊抗小鼠二次结合物培育。细胞通过流式细胞术，每个样品使用10000活细胞进行测定。[1] |
| Kinase Experiment | 细胞均匀分布，并以26900 × g在4°C下离心30分钟。细胞膜重悬浮于20 mM HEPES(pH 7.4)，100 mM NaCl，10 mM MgCl2，1 mM EDTA 和 含0.1% 脱脂 BSA的2–3毫克蛋白质/毫升溶液中。GTPγ[35S]结合试验，通过细胞膜(75 毫克蛋白质/毫升)在50 mM HEPES，100 mM NaCl，10 mM MgCl2，20 微克/毫升皂苷和0.1%脱脂BSA(pH 7.4)，5 毫克/毫升小麦胚芽凝集素涂层的闪烁迫近分析珠子，以及10 μM GDP中培养进行10-15分钟。GTPγ[35S]结合反应通过加入200 pM GTPγ[35S]启动。在室温下进行120分钟后，将板以300 × g离心10分钟，并计数。[1] |
| Data Literature Source | [1] Gergely P，et al. Br J Pharmacol，2012，167(5)，1035-1047. [2] Pan S，et al. ACS Med，Chem，Lett，2013，4 (3)，333–337. [3] Lewis ND，et al. J Immunol，2013，190(7)，3533-3540. |
| Unit | Bottle |
| Specification | 2mg 5mg 10mg |
是有效，选择性的 鞘氨醇-1-磷酸 (S1P) 受体调节剂。
Remark：These protocols are for reference only. Solarbio does not independently validate these methods.
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