PF-543 HydrochlorideCAS号： 1706522-79-3分子式： C27H32ClNO4S分子量： 502.1描述纯度储存/保存方法可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
| 产品描述 | |
| 描述 |
PF-543 inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform.
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| 纯度 |
98%
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| 储存/保存方法 |
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
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| 基本信息 | |
| 可溶性/溶解性 |
DMSO:90 mg/mL (136.83mM)
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| 生物活性 | |
| 靶点 |
SphK1:2 nM (IC50), SphK1:3.6 nM (Ki), sphingosine 1-phosphate (S1P):26.7 nM (IC50)
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| In vitro(体外研究) |
SphK1 inhibition by PF-543 causes a dose-dependent depletion of the intracellular level of S1P with EC50 concentration of 8.4 nM and a concomitant elevation of the intracellular level of sphingosine in 1483 cells. The level of endogenous S1P in 1483 cells after a 1 h treatment with 200 nM PF-543 is decreased 10-fold, producing a proportional increase in the level of sphingosine.
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| In vivo(体内研究) |
PF543 was found to be a potent inhibitor (IC50 = 26.7 nM) capable of blocking >90% of C17-S1P formation in the blood.
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