生物活性 | |||
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描述 | JTE-013 is recognized as a potent and selective antagonist of S1P2. It effectively blocks the binding of radiolabeled S1P to S1P2 receptors in both humans and rats, with IC50 values of 17 nM and 22 nM, respectively. When applied at concentrations ranging from 50 to 200 μM for 1 to 3 days, JTE-013 leads to a reduction in cell viability[1]. At dosages between 10 and 1000 nM over 30 minutes, JTE-013 counteracts the Akt inhibition induced by S1P and impedes the activation of ERK by S1P. JTE-013 shows a modest 4.2% inhibition of S1P3 and does not act as an antagonist to S1P1 at concentrations up to 10 μM. In SK-N-AS cells, exposure to 50, 100, 150, and 200 μM of JTE-013 for 1-3 days results in decreased cell viability, while 10, 100, and 1000 nM concentrations over 30 minutes reverse S1P-induced Akt inhibition and inhibit S1P-induced ERK activation[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.45mL 0.49mL 0.24mL |
12.25mL 2.45mL 1.22mL |
24.49mL 4.90mL 2.45mL |