W146 TFA

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

Product information

CAS Number: 909725-62-8

Molecular Weight: 456.39

Formula: C18H28F3N2O6P

Chemical Name: [3R-amino-4-[(3-hexylphenyl)amino]-4-oxobutyl]-phosphonic acid, mono(trifluoroacetate)

Smiles: CCCCCCC1=CC(=CC=C1)NC(=O)[C@H](N)CCP(O)(O)=O.OC(=O)C(F)(F)F

InChiKey: JDWCNCPWPLHFEX-XFULWGLBSA-N

InChi: InChI=1S/C16H27N2O4P.C2HF3O2/c1-2-3-4-5-7-13-8-6-9-14(12-13)18-16(19)15(17)10-11-23(20,21)22;3-2(4,5)1(6)7/h6,8-9,12,15H,2-5,7,10-11,17H2,1H3,(H,18,19)(H2,20,21,22);(H,6,7)/t15-;/m1./s1

Technical Data

Appearance: Solid Power

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: To be determined

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined

HS Tariff Code: 382200

How to use

In Vitro:

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

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 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.

References:

1. 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.
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.

Products are for research use only. Not for human use.