W146 TFA

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W146 TFA 

W146 TFA 是 1-磷酸-鞘氨醇受体亚型 1 (S1PR1) 的选择性拮抗剂, EC50 值为 398 nM。

W146 TFA

W146 TFA Chemical Structure

CAS No. : 909725-62-8

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生物活性

W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.

IC50 & Target

EC50: 398 nM (S1PR1)[1].

体外研究
(In Vitro)

W146 is a S1PR1 antagonist with a Ki of ~70-80 nM[1].
W146 pretreatment significantly increases activated cleaved caspase-3 levels. The reduced EPCs apoptosis which induced by S1P is completely abolished after treatment with W146[2].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Apoptosis Analysis[2]

Cell Line: Endothelial progenitor cells (EPCs).
Concentration: 10 μM.
Incubation Time: 30 min before the addition of S1P.
Result: Increases activated cleaved caspase-3 levels.

体内研究
(In Vivo)

W146 (5 mg/kg, ip, prior to AMD3100 administration) pre-treatment shows approximately 8-fold increase of KSL-HSPC mobilization, measured by the CFU-G/M colony forming assays, compared to that in mice treated with AMD3100 alone[3]
The W146-mediated augmentation of KSL-HSPC mobilization is specific, because pretreatment of mice with W140 is unable to produce any effect on AMD3100-stimulated KSL-HSPC mobilization. Injections of W146, W140, JTE013, or Cay10444 do not alter the basal WBC count in mice[3].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Mice (4-6-week-old)[3]
.
Dosage: 5 mg/kg.
Administration: IP, 1 hour prior to AMD3100 (ADM) administration.
Result: Significantly increased in KSL-HSPC mobilization compared to that in mice pretreated with dextran followed by AMD3100 administration.

分子量

456.39

Formula

C18H28F3N2O6P

CAS 号

909725-62-8

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.

参考文献
  • [1]. M Germana Sanna, et al. Enhancement of capillary leakage and restoration of lymphocyte egress by a chiral S1P1 antagonist in vivo. Nat Chem Biol. 2006 Aug;2(8):434-41. Epub 2006 Jul 9.

    [2]. Jingjing Liu, et al. 3-amino-4-(3-hexylphenylamino)-4-oxobutyl phosphonic acid (W146), a Selective Antagonist of Sphingosine-1-phospahte Receptor Subtype 1, Enhances AMD3100-stimulated Mobilization of Hematopoietic Stem Progenitor Cells in Animals. J Biochem Pharmacol Res. 2013 Dec; 1(4): 197–203.

    [3]. Hang Wang, et al. Sphingosine-1-phosphate promotes the proliferation and attenuates apoptosis of Endothelial progenitor cells via S1PR1/S1PR3/PI3K/Akt pathway. Cell Biol Int. 2018 May 23.

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