1. Metabolic Enzyme/Protease GPCR/G Protein
  2. Endogenous Metabolite LPL Receptor
  3. Sphingosine-1-phosphate

Sphingosine-1-phosphate  (Synonyms: S1P)

目录号: HY-108496 纯度: ≥99.0%
COA 产品使用指南 技术支持

Sphingosine-1-phosphate (S1P) 是 S1P1-5 受体 (S1P1-5 receptors) 的激动剂和 GPR3、GPR6、GPR12 的配体。Sphingosine-1-phosphate 是细胞内的第二信使,动员 Ca2+ 作为 G 蛋白偶联受体的细胞外配体。Sphingosine-1-phosphate 是由鞘磷脂 (HY-113498) 或其他膜磷脂生成的重要脂质介质。Sphingosine-1-phosphate 可以促进 DNA 合成,细胞的增殖和迁移。

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Sphingosine-1-phosphate Chemical Structure

Sphingosine-1-phosphate Chemical Structure

CAS No. : 26993-30-6

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Other Forms of Sphingosine-1-phosphate:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Sphingosine-1-phosphate (S1P) is an agonist of S1P1-5 receptors and a ligand of GPR3, GPR6 and GPR12. Sphingosine-1-phosphate is an intracellular second messenger and mobilizes Ca2+ as an extracellular ligand for G protein-coupled receptors[1]. Sphingosine-1-phosphate is an important lipid mediator generated from Sphingomyelin (HY-113498) or other membrane phospholipids[2]. Sphingosine-1-phosphate stimulates the DNA synthesis, cell proliferation and migration[4].

IC50 & Target

Human Endogenous Metabolite

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
0.2 nM
Compound: S1P
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
Displacement of [33P]S1P from human recombinant S1P5 receptor expressed in CHO cells by scintillation counting
[PMID: 20446681]
CHO EC50
0.55 nM
Compound: sphingosine-P
Activity at human recombinant S1P1 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
Activity at human recombinant S1P1 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
[PMID: 17070046]
CHO EC50
0.91 nM
Compound: sphingosine-P
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
Activity at human recombinant S1P5 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
[PMID: 17070046]
CHO EC50
1.6 nM
Compound: sphingosine-P
Activity at human recombinant S1P3 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
Activity at human recombinant S1P3 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
[PMID: 17070046]
CHO EC50
121 nM
Compound: S1P
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
Agonist activity at human recombinant S1P5 receptor expressed in CHO cells by GTPgammaS binding assay
[PMID: 20446681]
CHO EC50
164 nM
Compound: S1P
Agonist activity at human recombinant S1P4 receptor expressed in CHO cells by GTPgammaS binding assay
Agonist activity at human recombinant S1P4 receptor expressed in CHO cells by GTPgammaS binding assay
[PMID: 20446681]
CHO IC50
2.9 nM
Compound: S1P
Displacement of [33P]S1P from human recombinant S1P4 receptor expressed in CHO cells by scintillation counting
Displacement of [33P]S1P from human recombinant S1P4 receptor expressed in CHO cells by scintillation counting
[PMID: 20446681]
CHO EC50
7.9 nM
Compound: sphingosine-P
Activity at human recombinant S1P4 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
Activity at human recombinant S1P4 receptor expressed in CHO cells assessed as increase in calcium release by FLIPR assay
[PMID: 17070046]
HEK293 EC50
0.1 nM
Compound: S1P
Displacement of [33P]S1P from human recombinant S1P1 receptor expressed in HEK cells by scintillation counting
Displacement of [33P]S1P from human recombinant S1P1 receptor expressed in HEK cells by scintillation counting
[PMID: 20446681]
HEK293 EC50
0.2 nM
Compound: S1P
Displacement of [33P]S1P from human recombinant S1P3 receptor expressed in HEK cells by scintillation counting
Displacement of [33P]S1P from human recombinant S1P3 receptor expressed in HEK cells by scintillation counting
[PMID: 20446681]
HEK293 EC50
0.7 nM
Compound: S1P
Displacement of [33P]S1P from human recombinant S1P2 receptor expressed in HEK cells by scintillation counting
Displacement of [33P]S1P from human recombinant S1P2 receptor expressed in HEK cells by scintillation counting
[PMID: 20446681]
HEK293 EC50
0.7 nM
Compound: S1P
Agonist activity at human recombinant S1P3 receptor expressed in HEK cells by GTPgammaS binding assay
Agonist activity at human recombinant S1P3 receptor expressed in HEK cells by GTPgammaS binding assay
[PMID: 20446681]
HEK293 EC50
25.3 nM
Compound: S1P
Agonist activity at human recombinant S1P1 receptor expressed in HEK cells by GTPgammaS binding assay
Agonist activity at human recombinant S1P1 receptor expressed in HEK cells by GTPgammaS binding assay
[PMID: 20446681]
HEK293 EC50
43.9 nM
Compound: S1P
Agonist activity at human recombinant S1P2 receptor expressed in HEK cells by GTPgammaS binding assay
Agonist activity at human recombinant S1P2 receptor expressed in HEK cells by GTPgammaS binding assay
[PMID: 20446681]
HEK-293T IC50
0.78 nM
Compound: S1P
Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor expressed in HEK293T cells after 60 mins by scintillation counting
Displacement of [33P]sphingosine-1-phosphate from human S1P1 receptor expressed in HEK293T cells after 60 mins by scintillation counting
[PMID: 20304639]
HEK-293T EC50
0.9 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
[PMID: 14505636]
HEK-293T IC50
0.92 nM
Compound: S1P
Displacement of [33P]sphingosine-1-phosphate from human S1P3 receptor expressed in HEK293T cells after 60 mins by scintillation counting
Displacement of [33P]sphingosine-1-phosphate from human S1P3 receptor expressed in HEK293T cells after 60 mins by scintillation counting
[PMID: 20304639]
HEK-293T IC50
1.04 nM
Compound: S1P
Displacement of [33P]sphingosine-1-phosphate from human S1P4 receptor expressed in HEK293T cells after 60 mins by scintillation counting
Displacement of [33P]sphingosine-1-phosphate from human S1P4 receptor expressed in HEK293T cells after 60 mins by scintillation counting
[PMID: 20304639]
HEK-293T EC50
1.1 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
[PMID: 14505636]
HEK-293T EC50
1.2 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
[PMID: 15341948]
HEK-293T EC50
1.3 nM
Compound: S1P
Agonist activity at human S1P2R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
Agonist activity at human S1P2R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
[PMID: 24900589]
HEK-293T EC50
1.7 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
[PMID: 15341948]
HEK-293T EC50
1.8 nM
Compound: S1P
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
Agonist activity at human S1P5R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
[PMID: 24900589]
HEK-293T EC50
13 nM
Compound: S1P
Agonist activity at human S1P4R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
Agonist activity at human S1P4R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
[PMID: 24900589]
HEK-293T IC50
2 nM
Compound: S1P
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
Displacement of [33P]sphingosine-1-phosphate from human S1P5 receptor expressed in HEK293T cells after 60 mins by scintillation counting
[PMID: 20304639]
HEK-293T EC50
2.2 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
[PMID: 15341948]
HEK-293T EC50
2.4 nM
Compound: S1P
Antagonist activity at human S1P3 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting
Antagonist activity at human S1P3 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting
[PMID: 20304639]
HEK-293T EC50
2.9 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
[PMID: 14505636]
HEK-293T EC50
20 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
[PMID: 15341948]
HEK-293T EC50
270 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 4 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 4 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
[PMID: 14505636]
HEK-293T EC50
3.94 nM
Compound: S1P
Agonist activity at human S1P3R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
Agonist activity at human S1P3R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
[PMID: 24900589]
HEK-293T EC50
37 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 4 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 4 expressed in HEK293T cells was determined using [gamma-35S]-GTP as radioligand
[PMID: 15341948]
HEK-293T EC50
4.25 nM
Compound: S1P
Agonist activity at human S1P1R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
Agonist activity at human S1P1R expressed in HEK293T cells assessed as [35S]GTPgammaS binding after 30 mins by scintillation counting
[PMID: 24900589]
HEK-293T EC50
4.5 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand. (Experiment 2)
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 1 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand. (Experiment 2)
[PMID: 14505636]
HEK-293T EC50
43.9 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 1)
[PMID: 14505636]
HEK-293T EC50
5.6 nM
Compound: S1P
Antagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting
Antagonist activity at human S1P1 receptor expressed in HEK293T cells assessed as inhibition of sphingosine-1-phosphate-induced gamma-[35S]GTP binding after 30 mins by scintillation counting
[PMID: 20304639]
HEK-293T EC50
8.3 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 2 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
[PMID: 14505636]
HEK-293T EC50
8.7 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 3 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
[PMID: 14505636]
HEK-293T EC50
9.2 nM
Compound: S1P
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
In vitro binding affinity towards human Sphingosine 1-phosphate receptor 5 expressed in HEK293T cells using [gamma-35S]-GTP as radioligand (Experiment 2)
[PMID: 14505636]
U2OS EC50
0.018 μM
Compound: 1, S1P
Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining
Agonist activity at human S1P1 receptor expressed in human U2OS cells co-expressing eGFP assessed as receptor internalization into cytoplasm using Hoechst dye staining
[PMID: 22104144]
U2OS EC50
2.8 nM
Compound: S1P
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
Agonist activity at human S1P1 receptor expressed in EDG1-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
[PMID: 26687487]
U2OS EC50
79 nM
Compound: S1P
Agonist activity at human S1P3 receptor expressed in EDG3-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
Agonist activity at human S1P3 receptor expressed in EDG3-bla U2OS cells incubated for 18 hrs prior to GenBlazer substrate addition by beta-arrestin recruitment assay
[PMID: 26687487]
体外研究
(In Vitro)

在血清饥饿条件下 (1% FCS)[1],S1P (1 μM) 在 HEK293 细胞中诱导显著的 Ca2+ 释放。
在功能性 Ca2+ 测定,Suramin (HY-B0879) 单独对通过 gpr3、gpr6 或 gpr12 释放细胞内 Ca2+ 没有任何影响。相反,S1P (1 μM) 在不同浓度的苏拉明 (HY-B0879) 存在下,在转染的 HEK293 细胞中诱导 gpr3、gpr6 和 gpr12 的 Ca2+ 释放[2]
在功能性 Ca2+ 测定中,S1P (3-3000 nM) 在 Suramin (300 μM) 存在下表现出纳摩尔 EC50 值对于 gpr3 (EC50=29 nM),gpr6 (EC50=15 nM) 和 gpr12 (EC50=24 nM),大鼠gpr3 (EC50=68 nM),分别作用于HEK293细胞[2]
S1P增加表达S1P1和Gqi5,当以 200 nM 的浓度使用时,它允许 Gi 蛋白刺激磷脂酶 C,以及表达 S1P2 和 S1P3 受体的 TAg-Jurkat 细胞 (EC 50s=8 和 11 nM)[3]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

379.47

Formula

C18H38NO5P

CAS 号
性状

固体

颜色

White to yellow

结构分类
初始来源
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
细胞实验: 

1 M NaOH 中的溶解度 : 33.33 mg/mL (87.83 mM; 超声助溶)

Methanol 中的溶解度 : 3.85 mg/mL (10.15 mM; ultrasonic and warming and adjust pH to 3 with 1M HCl and heat to 60°C)

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.6353 mL 13.1763 mL 26.3525 mL
5 mM 0.5271 mL 2.6353 mL 5.2705 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物实验:

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比; 如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶。

  • 方案 一

    请依序添加每种溶剂: 0.1% BSA in Saline

    Solubility: 0.5 mg/mL (1.32 mM); 悬浊液; 超声助溶 (<60°C)

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料

纯度: ≥99.0%

参考文献

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
Methanol / 1 M NaOH 1 mM 2.6353 mL 13.1763 mL 26.3525 mL 65.8814 mL
5 mM 0.5271 mL 2.6353 mL 5.2705 mL 13.1763 mL
10 mM 0.2635 mL 1.3176 mL 2.6353 mL 6.5881 mL
1 M NaOH 15 mM 0.1757 mL 0.8784 mL 1.7568 mL 4.3921 mL
20 mM 0.1318 mL 0.6588 mL 1.3176 mL 3.2941 mL
25 mM 0.1054 mL 0.5271 mL 1.0541 mL 2.6353 mL
30 mM 0.0878 mL 0.4392 mL 0.8784 mL 2.1960 mL
40 mM 0.0659 mL 0.3294 mL 0.6588 mL 1.6470 mL
50 mM 0.0527 mL 0.2635 mL 0.5271 mL 1.3176 mL
60 mM 0.0439 mL 0.2196 mL 0.4392 mL 1.0980 mL
80 mM 0.0329 mL 0.1647 mL 0.3294 mL 0.8235 mL
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.

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产品名称:
Sphingosine-1-phosphate
目录号:
HY-108496
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