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

目錄號(hào): HY-15382 純度: 99.73% ee.: 99.76%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南技術(shù)支持

FTY720 (S)-Phosphate 是一種 S1P 受體 1 (S1PR1) 激動(dòng)劑，可以用于急性肺損傷等急性炎癥的研究。

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FTY720 (S)-Phosphate Chemical Structure

CAS No. : 402616-26-6

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Customer Review

Other Forms of FTY720 (S)-Phosphate:

Fingolimod phosphate In-stock
(S)-FTY720-phosphonate In-stock

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

•Front Immunol. 2017 Oct 19;8:1345. [Abstract]

FTY720 (S)-Phosphate 相關(guān)產(chǎn)品

•相關(guān)化合物庫(kù):

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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]

細(xì)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]

體外研究
(In Vitro)

FTY720 (S)-Phosphate 是 S1PR1 的激動(dòng)劑。FTY720 (S)-Phosphate (Tys，1 μM) 維持 S1PR1 蛋白表達(dá)，通過(guò) S1PR1 增強(qiáng)人肺動(dòng)脈內(nèi)皮細(xì)胞屏障，但對(duì)誘導(dǎo) S1PR1 泛素化沒(méi)有影響。FTY720 (S)-Phosphate (0.01-50 μM) 還可減少 β-arrestin 向 S1PR1 的募集^[1]。

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

體內(nèi)研究
(In Vivo)

FTY720 (S)-Phosphate (0.5 mg/kg，i.p.) 保留小鼠肺中的 S1PR1 表達(dá)，對(duì)博來(lái)霉素誘導(dǎo)的急性肺損傷 (ALI) 具有保護(hù)作用，并減弱博來(lái)霉素?fù)p傷小鼠的肺組織白細(xì)胞浸潤(rùn)^[1]。

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

分子量

387.45

Formula

C₁₉H₃₄NO₅P

CAS 號(hào)

402616-26-6

性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

Powder	-20°C	3 years

*該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 1 mg/mL (2.58 mM; 超聲助溶 (<80°C); 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)量	1 mg	5 mg	10 mg

1 mM	2.5810 mL	12.9049 mL	25.8098 mL
5 mM	---	---	---
10 mM	---	---	---

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；該產(chǎn)品在溶液狀態(tài)不穩(wěn)定，建議您現(xiàn)用現(xiàn)配，即刻使用。

摩爾計(jì)算器
稀釋計(jì)算器

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

以下溶解方案源自文獻(xiàn)，僅供參考，建議您先取少量樣品進(jìn)行嘗試。

方案一

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

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

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過(guò)程有損耗，建議您多配一只動(dòng)物的量

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

純度 & 產(chǎn)品資料

純度: 99.73% ee.: 99.76%

選擇批次：

Data Sheet (610 KB) SDS (252 KB)

COA (285 KB) HNMR (204 KB) RP-HPLC (260 KB) NP-HPLC (455 KB) LCMS (95 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[1]. Wang L, et al. FTY720 (s)-phosphonate preserves sphingosine 1-phosphate receptor 1 expression and exhibits superior barrier protection to FTY720 in acute lung injury. Crit Care Med. 2014 Mar;42(3):e189-99. [Content Brief]

[2]. Lingling Jia, et al. Clostridium butyricum?CGMCC0313.1 Protects against Autoimmune Diabetes by Modulating Intestinal Immune Homeostasis and Inducing Pancreatic Regulatory T Cells. Front Immunol.?2017 Oct 19;8:1345. [Content Brief]

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.
參考文獻(xiàn)	[1]. Wang L, et al. FTY720 (s)-phosphonate preserves sphingosine 1-phosphate receptor 1 expression and exhibits superior barrier protection to FTY720 in acute lung injury. Crit Care Med. 2014 Mar;42(3):e189-99. [Content Brief] [2]. Lingling Jia, et al. Clostridium butyricum?CGMCC0313.1 Protects against Autoimmune Diabetes by Modulating Intestinal Immune Homeostasis and Inducing Pancreatic Regulatory T Cells. Front Immunol.?2017 Oct 19;8:1345. [Content Brief]

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.

參考文獻(xiàn)

[1]. Wang L, et al. FTY720 (s)-phosphonate preserves sphingosine 1-phosphate receptor 1 expression and exhibits superior barrier protection to FTY720 in acute lung injury. Crit Care Med. 2014 Mar;42(3):e189-99. [Content Brief]

[2]. Lingling Jia, et al. Clostridium butyricum?CGMCC0313.1 Protects against Autoimmune Diabetes by Modulating Intestinal Immune Homeostasis and Inducing Pancreatic Regulatory T Cells. Front Immunol.?2017 Oct 19;8:1345. [Content Brief]

FTY720 (S)-Phosphate 相關(guān)分類

Inflammation/Immunology

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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.

Keywords:

FTY720 (S)-Phosphate402616-26-6(S)-FTY720P(S)-FTY720LPL ReceptorLysophospholipid ReceptorInhibitorinhibitorinhibit

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

Customer Review

Other Forms of FTY720 (S)-Phosphate:

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)