For research use only. Not for therapeutic Use.
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].
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].
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].
| Catalog Number | I010790 |
| CAS Number | 909725-61-7 |
| Synonyms | [(3R)-3-amino-4-(3-hexylanilino)-4-oxobutyl]phosphonic acid |
| Molecular Formula | C16H27N2O4P |
| Purity | ≥95% |
| InChI | InChI=1S/C16H27N2O4P/c1-2-3-4-5-7-13-8-6-9-14(12-13)18-16(19)15(17)10-11-23(20,21)22/h6,8-9,12,15H,2-5,7,10-11,17H2,1H3,(H,18,19)(H2,20,21,22)/t15-/m1/s1 |
| InChIKey | FWJRVGZWNDOOFH-OAHLLOKOSA-N |
| SMILES | CCCCCCC1=CC(=CC=C1)NC(=O)C(CCP(=O)(O)O)N |
| Reference | [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. |
