W146 |
Katalog-Nr.GC16621 |
W146 ist ein selektiver Antagonist des Sphingosin-1-Phosphat-Rezeptors 1 (S1PR1) mit einem EC50-Wert von 398 nM.
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Cas No.: 909725-61-7
Sample solution is provided at 25 µL, 10mM.
W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
W146 is a S1PR1 antagonist with a Ki of ~70-80 nM[1]. Compared with the S1P treated group, the S1P attenuated TUNEL labeling index of EPCs is significantly increased by pretreatment with W146. Furthermore, pretreatment with W146 significantly increases activated cleaved caspase-3 levels. The reduced EPCs apoptosis which induced by S1P is completely abolished after treatment with W146[2].
Injections of W146, W140, JTE013, or Cay10444 do not alter the basal WBC count in mice. It is found that a significant increase in KSL-HSPC mobilization when mice are pretreated with W146, compared to that in mice pretreated with dextran followed by AMD3100 administration. Moreover, pre-treatment of W146 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. 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[3].
References:
[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]. 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.
[3]. 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.
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