PF-543

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

PF-543 是一种新型鞘氨醇竞争性 SphK1 抑制剂，可抑制 SphK1，IC50 和 Ki 分别为 2.0 nM 和 3.6 nM。

PF-543, a novel sphingosine-competitive inhibitor of SphK1, inhibits SphK1 with IC50 and Ki of 2.0 nM and 3.6 nM.

Western Blot Analysis Cell Line:Human pulmonary arterial smooth muscle (PASM) cells Concentration:10 nM, 100 nM, 1000 nM Incubation Time:24 ?hours Result:Abolished SK1 expression at nM concentrations.Apoptosis Analysis Cell Line:Human pulmonary arterial smooth muscle (PASM) cells Concentration:0.1 μM, 1 μM, 10 μM Incubation Time:24 ?hours Result:Induced caspase-3/7 activity in cultured human pulmonary smooth muscle cells.

Animal Model:Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension Dosage:1 mg/kg Administration:Intraperitoneal injection; every second day; for 21 days Result:Reduced right ventricular hypertrophy. The protection involves a reduction in the expression of p53 (that promotes cardiomyocyte death) and an increase in the expression of anti-oxidant nuclear factor Nrf-2.

Sphingosine Kinase 1 Inhibitor II

Others

Other Targets

SphK1| SphK1

Cancer

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1415562-82-1

465.6

C27H31NO4S

>98% (HPLC)

In Vitro:?DMSO : 100 mg/mL (214.78 mM)

C(O)[C@@H]1N(CCC1)Cc1ccc(cc1)COc1cc(cc(c1)C)CS(=O)(=O)c1ccccc1

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(-20℃)

With Ice Pack

≥ 2 years