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

Sphingosine-1-phosphate  (Synonyms: S1P)

目錄號(hào): HY-108496 純度: ≥99.0%
COA 產(chǎn)品使用指南 技術(shù)支持

Sphingosine-1-phosphate (S1P) 是 S1P1-5 受體 (S1P1-5 receptors) 的激動(dòng)劑和 GPR3、GPR6、GPR12 的配體。Sphingosine-1-phosphate 是細(xì)胞內(nèi)的第二信使,動(dòng)員 Ca2+ 作為 G 蛋白偶聯(lián)受體的細(xì)胞外配體。Sphingosine-1-phosphate 是由鞘磷脂 (HY-113498) 或其他膜磷脂生成的重要脂質(zhì)介質(zhì)。Sphingosine-1-phosphate 可以促進(jìn) DNA 合成,細(xì)胞的增殖和遷移。

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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:

查看 LPL Receptor 亞型特異性產(chǎn)品:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

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

 

細(xì)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]
體外研究
(In Vitro)

在血清饑餓條件下 (1% FCS)[1],S1P (1 μM) 在 HEK293 細(xì)胞中誘導(dǎo)顯著的 Ca2+ 釋放。
在功能性 Ca2+ 測(cè)定,Suramin (HY-B0879) 單獨(dú)對(duì)通過 gpr3、gpr6 或 gpr12 釋放細(xì)胞內(nèi) Ca2+ 沒有任何影響。相反,S1P (1 μM) 在不同濃度的蘇拉明 (HY-B0879) 存在下,在轉(zhuǎn)染的 HEK293 細(xì)胞中誘導(dǎo) gpr3、gpr6 和 gpr12 的 Ca2+ 釋放[2]
在功能性 Ca2+ 測(cè)定中,S1P (3-3000 nM) 在 Suramin (300 μM) 存在下表現(xiàn)出納摩爾 EC50 值對(duì)于 gpr3 (EC50=29 nM),gpr6 (EC50=15 nM) 和 gpr12 (EC50=24 nM),大鼠gpr3 (EC50=68 nM),分別作用于HEK293細(xì)胞[2]。
S1P增加表達(dá)S1P1和Gqi5,當(dāng)以 200 nM 的濃度使用時(shí),它允許 Gi 蛋白刺激磷脂酶 C,以及表達(dá) S1P2 和 S1P3 受體的 TAg-Jurkat 細(xì)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 號(hào)
性狀

固體

顏色

White to yellow

結(jié)構(gòu)分類
初始來源
運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)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)

溶解性數(shù)據(jù)
細(xì)胞實(shí)驗(yàn): 

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

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)

配制儲(chǔ)備液
濃度 溶劑體積 質(zhì)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
查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

  • 摩爾計(jì)算器

  • 稀釋計(jì)算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動(dòng)物實(shí)驗(yàn):

以下溶解方案,請(qǐng)直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請(qǐng)依序添加每種溶劑: 0.1% BSA in Saline

    Solubility: 0.5 mg/mL (1.32 mM); 懸濁液; 超聲助溶 (<60°C)

掃碼獲得
動(dòng)物溶解方案

動(dòng)物溶解方案計(jì)算器
請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息:

給藥劑量

mg/kg

動(dòng)物的平均體重

g

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

由于實(shí)驗(yàn)過程有損耗,建議您多配一只動(dòng)物的量
純度 & 產(chǎn)品資料

純度: ≥99.0%

參考文獻(xiàn)

完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用,-20°C儲(chǔ)存時(shí),請(qǐng)?jiān)?個(gè)月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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

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產(chǎn)品名稱:
Sphingosine-1-phosphate
目錄號(hào):
HY-108496
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