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PF-543 Citrate

🥰Excellent
Catalog No. T12436Cas No. 1415562-83-2
Alias Sphingosine Kinase 1 Inhibitor II Citrate, PF543 Citrate

PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a selective and potent inhibitor of sphingosine kinase 1 (SPHK1) and is an efficient inhibitor of 1-phosphate sphingosine (S1P) formation. It possesses anticancer, antifibrotic, and anti-inflammatory activities and can be used in research on colorectal cancer.

PF-543 Citrate

PF-543 Citrate

🥰Excellent
Purity: 99.33%
Catalog No. T12436Alias Sphingosine Kinase 1 Inhibitor II Citrate, PF543 CitrateCas No. 1415562-83-2
PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a selective and potent inhibitor of sphingosine kinase 1 (SPHK1) and is an efficient inhibitor of 1-phosphate sphingosine (S1P) formation. It possesses anticancer, antifibrotic, and anti-inflammatory activities and can be used in research on colorectal cancer.
Pack SizePriceAvailabilityQuantity
2 mg$44 In Stock
5 mg$76 In Stock
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Purity:99.33%
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Product Introduction

Bioactivity
Description
PF-543 Citrate (Sphingosine Kinase 1 Inhibitor II Citrate) is a selective and potent inhibitor of sphingosine kinase 1 (SPHK1) and is an efficient inhibitor of 1-phosphate sphingosine (S1P) formation. It possesses anticancer, antifibrotic, and anti-inflammatory activities and can be used in research on colorectal cancer.
Targets&IC50
SPHK1:2 nM, S1P:26.7 nM, SPHK1:3.6 nM (Ki)
In vitro
PF-543 Citrate is a selective sphingosine competitive SPHK1 inhibitor with an IC50 of 2 nM and a Ki of 3.6 nM.
PF-543 Citrate is also a potent inhibitor of sphingosine 1-phosphate (S1P) formation in whole blood with an IC50 of 26.7 nM.
PF-543 Citrate inhibits the formation of C17-S1P in 1483 cells with IC50 of 1.0 nM. [1]
In vivo
Administration of PF-543 Citrate (1 mg/kg intrperitoneal injection every other day for 21 days) in a mouse hypoxic model of pulmonary hypertension had no effect on vascular remodeling but reduced right ventricular hypertrophy.
PF-543 Citrate (10 mg/kg or 30 mg/kg intraperitoneally, 24h), T1/2 in mouse blood samples was 1.2 h. Administration of 10 mg/kg PF-543 Citrate to mice for 24 hours induced a decrease in SK1 expression in pulmonary vessels. [2]
The inhibition of SPHK1 and S1PR2 activity by PF-543 Citrate significantly hindered pancreatic fibrosis in CP mice. [4]
AliasSphingosine Kinase 1 Inhibitor II Citrate, PF543 Citrate
Chemical Properties
Molecular Weight657.73
FormulaC33H39NO11S
Cas No.1415562-83-2
SmilesC(CC(O)=O)(CC(O)=O)(C(O)=O)O.C(N1[C@@H](CO)CCC1)C2=CC=C(COC3=CC(CS(=O)(=O)C4=CC=CC=C4)=CC(C)=C3)C=C2
Relative Density.no data available
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
H2O: 40 mg/mL (60.82 mM), Sonication is recommended.
DMSO: 80 mg/mL (121.63 mM), Sonication is recommended.
Solution Preparation Table
H2O/DMSO
1mg5mg10mg50mg
1 mM1.5204 mL7.6019 mL15.2038 mL76.0190 mL
5 mM0.3041 mL1.5204 mL3.0408 mL15.2038 mL
10 mM0.1520 mL0.7602 mL1.5204 mL7.6019 mL
20 mM0.0760 mL0.3801 mL0.7602 mL3.8010 mL
50 mM0.0304 mL0.1520 mL0.3041 mL1.5204 mL
DMSO
1mg5mg10mg50mg
100 mM0.0152 mL0.0760 mL0.1520 mL0.7602 mL

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Preparation method for in vivo formula: Take 50 μL DMSOTargetMol | reagent main solution, add 300 μLPEG300TargetMol | reagent mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2OTargetMol | reagent mix well and clarify
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