PF-543 (hydrochloride) - CAS:1706522-79-3

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PF-543 (hydrochloride) (Synonyms:Sphingosine Kinase 1 Inhibitor II hydrochloride)

目录号 : KCM11942 CAS No. : 1706522-79-3 纯度 : ≥98%

Data Sheet 产品使用指南

PF-543 is a potent inhibitor of sphingosine kinase 1 (SPHK1; IC = 2 nM) that inhibits sphingosine-1-phosphate (S1P) binding to human recombinant SPHK1 (K = 3.6 nM). It is selective for SPHK1 over SPHK2 (IC = 356 nM) as well as a panel of protein and lipid kinases and S1P receptors at a concentration of 10 µM. PF-543 inhibits the formation of S1P in 1483 cells and human whole blood (ECs = 8.4 and 26.7 nM, respectively). In vivo, PF-543 prevents sickling, hemolysis, and inflammation in a transgenic mouse model of sickle cell disease.

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1mg		In-stock
5mg		In-stock
10mg		In-stock
25mg		In-stock

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生物活性

PF-543 (hydrochloride) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC₅₀ of 2 nM and a Ki of 3.6 nM. PF-543 hydrochloride is >100-fold selectivity for SPHK1 over SPHK2. PF-543 (hydrochloride) is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC₅₀ of 26.7 nM. PF-543 (hydrochloride) induces apoptosis, necrosis, and autophagy.

体外研究

PF-543 (10-1000 nM; 24 hours; PASM cells) treatment abolishes SK1 expression at nM concentrations.
PF-543 (0.1-10 μM; 24 hours; PASM cells) treatment induces caspase-3/7 activity.
PF-543 inhibits C₁₇-S1P formation in 1483 cells with an IC₅₀ of 1.0 nM.
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.

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.

体内研究

PF-543 (1 mg/kg; intraperitoneal injection; every second day; for 21 days; female C57BL/6 J mice) treatment has no effect on vascular remodelling but reduces right ventricular hypertrophy. The protection involves a reduction in the expression of p53 and an increase in the expression of anti-oxidant nuclear factor Nrf-2.
Mice are initially dosed (ip) with 10 mg/kg or 30 mg/kg of PF-543 for 24 h and the T_1/2 is 1.2 h in blood samples. Administration of 10 mg/kg PF-543 for 24 h to mice induces a decrease in SK1 expression in pulmonary vessels.

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.

分子式

C₂₇H₃₁NO₄S^.HCl

分子量

502.07

CAS号

1706522-79-3

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

纯度： ≥98%

Data Sheet

产品使用指南

MacRitchie N, et al. Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension. Cell Signal. 2016 Aug;28(8):946-55.

Schnute ME, et al. Modulation of cellular S1P levels with a novel, potent and specific inhibitor of sphingosine kinase-1. Biochem J. 2012 May 15;444(1):79-88.

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