Siponimod hemifumarate (Synonyms: BAF-312 hemifumarate)

目录号: HY-12355A: Data Sheet 产品使用指南技术支持

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

CAS No. : 1234627-85-0

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Siponimod hemifumarate 的其他形式现货产品:

Siponimod

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Siponimod In-stock
Siponimod-d₁₁ 询价

MCE 顾客使用本产品发表的 9 篇科研文献

Siponimod hemifumarate 相关产品

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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

NCT Number	Sponsor	Condition	Start Date	Phase
NCT01565902	Novartis Pharmaceuticals\|Novartis	Hepatic Impairment	October 2012	Phase 1
NCT04540861	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis
NCT03623243	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis\|Relapsing Multiple Sclerosis\|Advancing Multiple Sclerosis	February 14, 2019	Phase 3
NCT01665144	Novartis Pharmaceuticals\|Novartis	Secondary Progressive Multiple Sclerosis	December 20, 2012	Phase 3
NCT01185821	Novartis Pharmaceuticals\|Novartis	Relapsing Remitting Multiple Sclerosis	August 30, 2010	Phase 2
NCT02029274	Novartis Pharmaceuticals\|Novartis	Active Dermatomyositis	August 25, 2013	Phase 2
NCT01904214	Novartis Pharmaceuticals\|Novartis	Renal Impairment	July 2013	Phase 1
NCT01801917	Novartis Pharmaceuticals\|Novartis	Polymyositis	April 24, 2013	Phase 2
NCT04895202	Novartis Pharmaceuticals\|Novartis	Secondary Progressive Multiple Sclerosis With Inflammatory Disease Activity	November 19, 2021
NCT00422175	Novartis	Healthy	October 2006	Phase 1
NCT04933552	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis	December 15, 2021
NCT03338998	Novartis Pharmaceuticals\|Novartis	Hemorrhagic Stroke\|Intracerebral Hemorrhage (ICH)	December 24, 2017	Phase 2
NCT00879658	Novartis Pharmaceuticals\|Novartis	Relapsing-remitting Multiple Sclerosis	March 30, 2009	Phase 2
NCT04926818	Novartis Pharmaceuticals\|Novartis	Multiple Sclerosis (MS)	October 5, 2021	Phase 3
NCT05376579	Novartis Pharmaceuticals\|Novartis	Active Secondary Progressive Multiple Sclerosis	June 17, 2022
NCT01148810	Novartis Pharmaceuticals\|Novartis	Polymyositis\|Dermatomyositis	June 15, 2010	Phase 2
NCT05688436	Biogen	Multiple Sclerosis	September 24, 2021
NCT04792567	Novartis Pharmaceuticals\|Novartis	Secondary Progressive Multiple Sclerosis	April 19, 2021	Phase 4

分子量

574.63

Formula

C₂₉H₃₅F₃N₂O₃.1/2C₄H₄O₄

CAS 号

1234627-85-0

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

Data Sheet (532 KB) 产品使用指南 (1538 KB)

参考文献

[1]. 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. [Content Brief]

[2]. McGinley M, et al. Prospects of siponimod in secondary progressive multiple sclerosis. Ther Adv Neurol Disord. 2018 Jul 17;11:1756286418788013. [Content Brief]

[3]. Behrangi N, et al. Mechanism of Siponimod: Anti-Inflammatory and Neuroprotective Mode of Action. Cells. 2019 Jan 7;8(1):24. [Content Brief]

Siponimod hemifumarate 相关分类

Neurological Disease Inflammation/Immunology

摩尔计算器
稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量		浓度		体积		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)	×	体积 _(start)	=	浓度 _(final)	×	体积 _(final)
	×		=		×
C1		V1		C2		V2

Keywords:

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

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Siponimod hemifumarate (Synonyms: BAF-312 hemifumarate)

Customer Review

Other Forms of Siponimod hemifumarate:

MCE 顾客使用本产品发表的 9 篇科研文献

Siponimod hemifumarate 相关产品

•同靶点产品:

查看 LPL Receptor 亚型特异性产品:

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Siponimod hemifumarate (Synonyms: BAF-312 hemifumarate)

Customer Review

Other Forms of Siponimod hemifumarate:

Siponimod hemifumarate 相关抗体

MCE 顾客使用本产品发表的 9 篇科研文献

Siponimod hemifumarate 相关产品

•同靶点产品:

查看 LPL Receptor 亚型特异性产品:

生物活性

纯度 & 产品资料

参考文献

Siponimod hemifumarate 相关分类

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