DC Chemicals Limited
China
Product Name: W146 TFA
Price: $Inquiry/1g
Purity: 98.0%
Stocking Period: 1 Day
Contact: Tony Cao

909725-62-8

909725-62-8 structure

909725-62-8 structure

Name: W146 TFA
Chemical Name: {(3R)-3-Amino-4-[(3-hexylphenyl)amino]-4-oxobutyl}phosphonic acid
CAS Number: 909725-62-8
Molecular Formula: C₁₈H₂₈F₃N₂O₆P
Molecular Weight: 456.4
Catalog: Signaling Pathways Apoptosis Apoptosis
Create Date: 2018-03-07 06:24:26
Modify Date: 2024-01-11 09:25:03
W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.

Name	{(3R)-3-Amino-4-[(3-hexylphenyl)amino]-4-oxobutyl}phosphonic acid
Synonyms	{(3R)-3-Amino-4-[(3-hexylphenyl)amino]-4-oxobutyl}phosphonic acid Phosphonic acid, [(3R)-3-amino-4-[(3-hexylphenyl)amino]-4-oxobutyl]-

Description	W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
Related Catalog	Signaling Pathways >> Apoptosis >> Apoptosis Research Areas >> Cancer Signaling Pathways >> GPCR/G Protein >> LPL Receptor Research Areas >> Metabolic Disease
Target	EC50: 398 nM (S1PR1)[1].
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]. 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.
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]. 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.
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]. 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.

Molecular Formula	C₁₈H₂₈F₃N₂O₆P
Molecular Weight	456.4