1. GPCR/G Protein
  2. LPL Receptor
  3. FTY720 (S)-Phosphate

FTY720 (S)-Phosphate  (Synonyms: (S)-FTY720P; (S)-FTY720 phosphate)

目录号: HY-15382 纯度: 99.73% ee.: 99.76%
COA 产品使用指南

FTY720 (S)-Phosphate 是一种 S1P 受体 1 (S1PR1) 激动剂,可以用于急性肺损伤等急性炎症的研究。

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FTY720 (S)-Phosphate Chemical Structure

FTY720 (S)-Phosphate Chemical Structure

CAS No. : 402616-26-6

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Customer Review

Other Forms of FTY720 (S)-Phosphate:

MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

FTY720 (S)-Phosphate is an agonist of S1P receptor 1 (S1PR1), used in the research of acute inflammatory diseases such as acute lung injury.

IC50 & Target

S1PR1[1]

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
CHO EC50
> 10000 nM
Compound: (S)-5
Agonism of human S1P-2 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
Agonism of human S1P-2 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
[PMID: 16078855]
CHO EC50
0.28 nM
Compound: 2
Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 mins
Induction of internalization of C-terminal GFP-fused human S1P1 receptor expressed in CHO cell membranes after 50 mins
[PMID: 26924461]
CHO EC50
0.3 nM
Compound: (S)-5
Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
Agonism of human S1P-1 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
[PMID: 16078855]
CHO EC50
0.3 nM
Compound: (S)-5
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
Agonism of human S1P-5 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
[PMID: 16078855]
CHO EC50
0.6 nM
Compound: (S)-5
Agonism of human S1P-4 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
Agonism of human S1P-4 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
[PMID: 16078855]
CHO IC50
2.1 nM
Compound: (S)-FTY720-P, (S)-FTY720-Phosphate
Agonist activity at human S1P1 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
Agonist activity at human S1P1 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
[PMID: 22119341]
CHO IC50
2.2 nM
Compound: (S)-FTY720-P, (S)-FTY720-Phosphate
Agonist activity at human S1P4 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
Agonist activity at human S1P4 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
[PMID: 22119341]
CHO IC50
23 nM
Compound: (S)-FTY720-P, (S)-FTY720-Phosphate
Agonist activity at human S1P3 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
Agonist activity at human S1P3 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
[PMID: 22119341]
CHO EC50
3.1 nM
Compound: (S)-5
Agonism of human S1P-3 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
Agonism of human S1P-3 receptor expressed in CHO cells, 90-120 min in pH 7.4 using [35S]GTP-gamma-S as radioligand
[PMID: 16078855]
CHO IC50
5.9 nM
Compound: (S)-FTY720-P, (S)-FTY720-Phosphate
Agonist activity at human S1P2 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
Agonist activity at human S1P2 expressed in CHO cells after 60 mins by [35S]GTPgammaS binding assay
[PMID: 22119341]
CHO-K1 EC50
0.027 μM
Compound: 2a, FTY720-P
Agonist activity at human S1P3 receptor expressed in CHO-K1 cells co-expressing Gq/i5 G-protein assessed as calcium mobilization by FLIPR assay
Agonist activity at human S1P3 receptor expressed in CHO-K1 cells co-expressing Gq/i5 G-protein assessed as calcium mobilization by FLIPR assay
[PMID: 22104144]
CHO-K1 EC50
0.29 nM
Compound: 2, FTY720-P
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Agonist activity at rat S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
[PMID: 24900318]
CHO-K1 EC50
0.37 nM
Compound: 2, FTY720-P
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Agonist activity at human S1P1 receptor expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
[PMID: 24900318]
CHO-K1 EC50
1.3 nM
Compound: 2, FTY720-P
Agonist activity at rat S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Agonist activity at rat S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
[PMID: 24900318]
CHO-K1 EC50
2 nM
Compound: 1-P
Agonist activity at human S1P3 receptor expressed in CHOK1 cell membranes by [35S]GTPgammaS binding assay
Agonist activity at human S1P3 receptor expressed in CHOK1 cell membranes by [35S]GTPgammaS binding assay
[PMID: 24909680]
CHO-K1 EC50
3.3 nM
Compound: 2, FTY720-P
Agonist activity at human S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
Agonist activity at human S1P3R expressed in CHO-K1 cells by [35S]GTPgammaS binding assay
[PMID: 24900318]
CHO-K1 EC50
7 nM
Compound: 1-P
Agonist activity at human S1P1 receptor expressed in CHOK1 cell membranes by [35S]GTPgammaS binding assay
Agonist activity at human S1P1 receptor expressed in CHOK1 cell membranes by [35S]GTPgammaS binding assay
[PMID: 24909680]
U2OS EC50
0.4 nM
Compound: FTY720P
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
94 nM
Compound: FTY720P
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)

FTY720 (S)-Phosphate 是 S1PR1 的激动剂。FTY720 (S)-Phosphate (Tys,1 μM) 维持 S1PR1 蛋白表达,通过 S1PR1 增强人肺动脉内皮细胞屏障,但对诱导 S1PR1 泛素化没有影响。FTY720 (S)-Phosphate (0.01-50 μM) 还可减少 β-arrestin 向 S1PR1 的募集[1]

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

体内研究
(In Vivo)

FTY720 (S)-Phosphate (0.5 mg/kg,i.p.) 保留小鼠肺中的 S1PR1 表达,对博来霉素诱导的急性肺损伤 (ALI) 具有保护作用,并减弱博来霉素损伤小鼠的肺组织白细胞浸润[1]

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

分子量

387.45

Formula

C19H34NO5P

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years

*该产品在溶液状态不稳定,建议您现用现配,即刻使用。

溶解性数据
细胞实验: 

DMSO 中的溶解度 : 1 mg/mL (2.58 mM; 超声助溶 (<80°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5810 mL 12.9049 mL 25.8098 mL
5 mM --- --- ---
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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

  • 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:

以下溶解方案源自文献,仅供参考,建议您先取少量样品进行尝试。

  • 方案 一

    FTY720 (S)-Phosphate is dissolved in sterile water[2].

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: 99.73% ee.: 99.76%

参考文献
Animal Administration
[1]

Mice[1] Male C57BL/6 (20-25 g) mice 8-10 weeks old receive a single intratracheal dose of bleomycin at 0.6 U/kg (or sterile saline) on Day 0 followed immediately by intraperitoneal injection of FTY720 (S)-Phosphate (0.5 mg/kg), FTY720 (0.5 mg/kg), or saline. Additional doses of FTY720 (S)-Phosphate or FTY720 are injected on Days 3 and 6. Bronchoalveolar lavage (BAL) fluid and lungs are then collected on Day 7. BAL fluid is used to detect BAL protein levels, WBC count, and WBC differential count. Lungs are perfused with saline to remove blood for Western blot, tissue albumin, and histopathology evaluation. Peripheral blood is obtained on Day 7 for examination of total cell counts and lymphocytes. Experiments are repeated 3 times. 6-10 mice are used per experimental group[1].

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

参考文献

FTY720 (S)-Phosphate 相关分类

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;该产品在溶液状态不稳定,建议您现用现配,即刻使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5810 mL 12.9049 mL 25.8098 mL 64.5245 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:
FTY720 (S)-Phosphate
目录号:
HY-15382
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