[CAS NO. 1415562-82-1] PF-543

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PRODUCTS SPECIFICATIONS [1415562-82-1]

Catalog

HY-15425

Brand

MCE

CAS

1415562-82-1

DESCRIPTION [1415562-82-1]

Overview

MDL	-
Molecular Weight	465.60
Molecular Formula	C27H31NO4S
SMILES	CC1=CC(OCC2=CC=C(CN3[C@@H](CO)CCC3)C=C2)=CC(CS(C4=CC=CC=C4)(=O)=O)=C1

For research use only. We do not sell to patients.

7 Publications Citing Use of MCE

Summary

PF-543 (Sphingosine Kinase 1 Inhibitor II) is a potent, selective, reversible and sphingosine-competitive SPHK1 inhibitor with an IC ₅₀ of 2 nM and a K _i of 3.6 nM. PF-543 is >100-fold selectivity for SPHK1 over SPHK2. PF-543 is an effective potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC ₅₀ of 26.7 nM. PF-543 induces apoptosis , necrosis, and autophagy ^[1] ^[2] ^[3] .

IC50 & Target

IC50: 2 nM (SPHK1); 26.7 nM (Sphingosine 1-phosphate (S1P)) ^[1]
Ki: 3.6 nM (SPHK1) ^[1]

In Vitro

PF-543 (10-1000 nM; 24 hours; PASM cells) treatment abolishes SK1 expression at nM concentrations ^[2] .
PF-543 (0.1-10 μM; 24 hours; PASM cells) treatment induces caspase-3/7 activity ^[2] .
PF-543 inhibits C ₁₇ -S1P formation in 1483 cells with an IC ₅₀ of 1.0 nM ^[1] .
SphK1 inhibition by PF-543 causes a dose-dependent depletion of the intracellular level of S1P with EC ₅₀ 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 ^[1] .

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis ^[2]

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 ^[2]

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.

In Vivo

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 ^[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 ^[2] .

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Female C57BL/6 J mice (7-12 week-old) with hypoxic-induced pulmonary arterial hypertension ^[2]
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.

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

-20°C, protect from light, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL ( 214.78 mM ; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1478 mL	10.7388 mL	21.4777 mL
5 mM	0.4296 mL	2.1478 mL	4.2955 mL
10 mM	0.2148 mL	1.0739 mL	2.1478 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in Saline)

Solubility: 5 mg/mL (10.74 mM); Suspended solution; Need ultrasonic
2.

Add each solvent one by one: 10% DMSO >> 90% Corn Oil

Solubility: ≥ 5 mg/mL (10.74 mM); Clear solution

* All of the co-solvents are available by MedChemExpress (MCE).