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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 Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $44 | In Stock | |
5 mg | $76 | In Stock |
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] |
Alias | Sphingosine Kinase 1 Inhibitor II Citrate, PF543 Citrate |
Molecular Weight | 657.73 |
Formula | C33H39NO11S |
Cas No. | 1415562-83-2 |
Smiles | C(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 | Powder: -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
DMSO
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