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| 商品编号 | 规格 | 价格 | 会员价 | 是否有货 | 数量 |
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| PL06783-5mg | 5mg | ¥542.00 | 请登录 |
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| PL06783-10mg | 10mg | ¥817.00 | 请登录 |
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| PL06783-50mg | 50mg | ¥2365.00 | 请登录 |
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| PL06783-100mg | 100mg | ¥3285.00 | 请登录 |
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| PL06783-500mg | 500mg | ¥7225.00 | 请登录 |
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| PL06783-1g | 1g | 询价 | 询价 |
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| PL06783-10mM*1mLinDMSO | 10mM*1mLinDMSO | ¥1461.00 | 请登录 |
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| PL06783-1 mL x 10 mM (in DMSO) | ¥617.00 | 请登录 |
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| 中文名称 |
Siponimod
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|---|---|
| 英文名称 |
Siponimod
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| 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]
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| Cas No. |
1230487-00-9
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| 分子式 |
C29H35F3N2O3
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| 分子量 |
516.60
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| 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)
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| 详情描述 |
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。
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| 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。
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|---|---|
| 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.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
S1PR1 0.39 nM (EC50) S1PR5 0.98 nM (EC
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| 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.
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| 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
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 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)
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| ClinicalTrial |
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| 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.
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| 溶解度数据 |
In Vitro: DMSO : ≥ 30 mg/mL (58.07 mM)配制储备液
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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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