W146 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。
| 生物活性 | W146 is a selective antagonist of sphingosine-1-phosphate receptor 1 (S1PR1) with an EC50value of 398 nM. |
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体外研究
(In Vitro) | W146 is a S1PR1 antagonist with a Kiof ~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. |
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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].
| 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. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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