2. GPCR/G Protein
  3. LPL Receptor
  4. Siponimod hemifumarate

Siponimod hemifumarate  (Synonyms: BAF-312 hemifumarate)

目录号: HY-12355A
产品使用指南

摩尔计算器

Siponimod (BAF-312) hemifumarate 是一种有效，选择性的鞘氨醇 -1- 磷酸 (S1P) 受体调节剂。Siponimod hemifumarate 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 hemifumarate 可用于多发性硬化症 (MS) 的研究。

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Siponimod hemifumarate Chemical Structure

Siponimod hemifumarate Chemical Structure

CAS No. : 1234627-85-0

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Siponimod hemifumarate 的其他形式现货产品:

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Other Forms of Siponimod hemifumarate:

Siponimod hemifumarate 相关抗体

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Siponimod (BAF-312) hemifumarate is a potent and selective sphingosine-1-phosphate (S1P) receptor modulator. Siponimod hemifumarate is selective for S1P1 and S1P5 receptors over S1P2, S1P3, and S1P4 (EC50s of 0.39, 0.98, >10000, >1000, and 750 nM, respectively). Siponimod hemifumarate can be used for multiple sclerosis (MS) research[1][2].

IC50 & Target

S1PR1

0.39 nM (EC50)

S1PR5

0.98 nM (EC50)

S1PR4

750 nM (EC50)

S1PR3

>1000 nM (EC50)

S1PR2

>10000 nM (EC50)

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.0004 μM
Compound: 32, BAF312, Siponimod
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
Agonist activity at human S1P1 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
[PMID: 24900670]
CHO EC50
0.98 nM
Compound: 3, BAF312
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human S1P5 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 24125884]
CHO EC50
5 μM
Compound: 32, BAF312, Siponimod
Agonist activity at human S1P3 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
Agonist activity at human S1P3 receptor transfected in CHO cells incubated for 10 to 15 mins prior to GTPgamma35S addition measured after 120 mins by GTPgamma35S binding assay
[PMID: 24900670]
CHO EC50
750 nM
Compound: 3, BAF312
Agonist activity at human S1P4 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
Agonist activity at human S1P4 receptor expressed in CHO cells by [35S]GTPgammaS binding assay
[PMID: 24125884]
Clinical Trial
分子量

574.63

Formula

C29H35F3N2O3.1/2C4H4O4
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Siponimod hemifumarate 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Siponimod hemifumarate1234627-85-0BAF-312 hemifumarateLPL ReceptorLysophospholipid Receptormultiple sclerosisneurodegenerationinflammationsiponimodprogressiveS1P receptorS1P1 agonistlymphocytesInhibitorinhibitorinhibit

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