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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 Chemical Structure
CAS No. : 909725-62-8
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是否有货 |
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100 mg |
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250 mg |
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500 mg |
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* Please select Quantity before adding items.
生物活性 |
W146 TFA is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50 value of 398 nM.
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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. |
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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. |
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运输条件 |
Room temperature in continental US; may vary elsewhere.
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis.
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参考文献 |
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[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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