(R)-FTY 720P

目录号: HY-114061: FAQs
Data Sheet 产品使用指南

摩尔计算器

(R)-FTY 720P 是 FTY 720P 的 R 异构体。(R)-FTY 720P 对 S1P_1,3,4,5 的结合亲和力比 (S)-异构体 (HY-15382) 弱。

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(R)-FTY 720P Chemical Structure

CAS No. : 402616-23-3

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规格	价格	是否有货
1 mg	￥2880	3 - 4 周
5 mg	现货	3 - 4 周
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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

(R)-FTY 720P is the R-isomer of FTY 720P. (R)-FTY 720P has less potent binding affinities to S1P_1,3,4,5 than (S)-Isomer (HY-15382)^[1].

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
CHO	EC₅₀	> 10000 nM Compound: (rac)-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	0.005 nM Compound: 1-P; FTY-P	Agonist activity at human S1P1 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by HTRF analysis Agonist activity at human S1P1 receptor expressed in CHO cells assessed as cAMP accumulation after 30 mins by HTRF analysis	[PMID: 26985316]
CHO	EC₅₀	0.0056 nM Compound: 1-P; FTY-P	Agonist activity at human S1P1 receptor expressed in CHO cells assessed as ERK phosphorylation after 7 mins by alphaLISA Agonist activity at human S1P1 receptor expressed in CHO cells assessed as ERK phosphorylation after 7 mins by alphaLISA	[PMID: 26985316]
CHO	IC₅₀	0.014 nM Compound: 1-P; FTY-P	Displacement of 33-P-S1P from from human S1P receptor expressed in CHO cell membranes after 50 mins by scintillation counting Displacement of 33-P-S1P from from human S1P receptor expressed in CHO cell membranes after 50 mins by scintillation counting	[PMID: 26985316]
CHO	EC₅₀	0.07 nM Compound: 1-P; FTY-P	Agonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assay Agonist activity at human S1P1 receptor expressed in CHO cells co-expressing GFP assessed as cellular internalization after 45 mins by Hoechst assay	[PMID: 26985316]
CHO	EC₅₀	0.3 nM Compound: 2	Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay Activity at human S1P1 receptor expressed in CHO cells by [35S]GTPgammaS binding assay	[PMID: 15615513]
CHO	EC₅₀	1.2 nM Compound: (rac)-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	1.4 nM Compound: (rac)-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	EC₅₀	11 nM Compound: FTY720-phosphate	Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cells assessed as inhibition of forskolin-induced cAMP accumulation by GTPgammaS binding assay	[PMID: 26509640]
CHO	EC₅₀	14 nM Compound: 3, FTY-720P	Agonist activity at S1P1 receptor (unknown origin) expressed in CHO cells preincubated for 2 hrs followed by D2-labeled IP1 and Ab-Cryp addition measured after 1 hr by fluorescence assay Agonist activity at S1P1 receptor (unknown origin) expressed in CHO cells preincubated for 2 hrs followed by D2-labeled IP1 and Ab-Cryp addition measured after 1 hr by fluorescence assay	10.1039/C3MD00079F
CHO	EC₅₀	2.4 nM Compound: (rac)-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	EC₅₀	3.4 nM Compound: FTY720-phosphate	Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay Agonist activity at S1P5 receptor (unknown origin) expressed in CHO cell membranes after 30 mins by GTPgammaS binding assay	[PMID: 26509640]
CHO	EC₅₀	35.1 nM Compound: 3, FTY720-P	Agonist activity at human S1P3 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay Agonist activity at human S1P3 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay	[PMID: 25072873]
CHO	EC₅₀	4.9 nM Compound: (rac)-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	44 nM Compound: 3, FTY-720P	Agonist activity at S1P3 receptor (unknown origin) expressed in CHO cells preincubated for 2 hrs followed by D2-labeled IP1 and Ab-Cryp addition measured after 1 hr by fluorescence assay Agonist activity at S1P3 receptor (unknown origin) expressed in CHO cells preincubated for 2 hrs followed by D2-labeled IP1 and Ab-Cryp addition measured after 1 hr by fluorescence assay	10.1039/C3MD00079F
CHO	EC₅₀	9.1 nM Compound: 3, FTY720-P	Agonist activity at human S1P1 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay Agonist activity at human S1P1 receptor expressed in CHO cells preincubated for 2 hrs before IP1 addition by IP1-HTRF assay	[PMID: 25072873]
HEK-293T	EC₅₀	0.1 nM Compound: FTY720-P	Activity at human S1P3 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay Activity at human S1P3 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	[PMID: 17113298]
HEK-293T	EC₅₀	1.3 nM Compound: FTY720-P	Activity at human S1P1 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay Activity at human S1P1 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	[PMID: 17113298]
HEK-293T	EC₅₀	4 nM Compound: FTY720-P	Activity at human S1P4 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay Activity at human S1P4 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	[PMID: 17113298]
HEK-293T	EC₅₀	4 nM Compound: FTY720-P	Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay Activity at human S1P5 receptor expressed in HEK293T cells by [35S]GTP-gamma-S binding assay	[PMID: 17113298]

体内研究
(In Vivo)

(R)-FTY 720P (静脉推注给药) 对麻醉大鼠的心率在剂量达到 0.3mg/kg 时没有明显影响^[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

402616-23-3

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

产品使用指南 (1538 KB)

参考文献

[1]. Kiuchi M, et al. Asymmetric synthesis and biological evaluation of the enantiomeric isomers of the immunosuppressive FTY720-phosphate. Bioorg Med Chem. 2005 Jan 17;13(2):425-32. [Content Brief]

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The dilution calculator equation

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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	×		=		×
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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:

(R)-FTY 720P402616-23-3LPL ReceptorLysophospholipid ReceptorR-isomerFTY 720PInhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

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(R)-FTY 720P

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