PF-543 Citrate

SKU: orb1708881

Description

PF-543 Citrate is a potent and selective sphingosine kinase 1 (SPHK1) inhibitor that blocks S1P formation. It exhibits anticancer, antifibrotic, and anti-inflammatory properties, making it a valuable research tool for studying diseases like colorectal cancer in both cellular and animal models.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1415562-83-2
• MW: 657.73
• Purity: 99.33% (May vary between batches)
• Formula: C₃₃H₃₉NO₁₁S
• 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
• Target: Autophagy,S1P Receptor,LPL Receptor,Apoptosis
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (5.02 mM);H2O:40 mg/mL (60.82 mM);DMSO:80 mg/mL (121.63 mM)

Bioactivity

• Target IC50:
  SPHK1:3.6 nM (Ki)|SPHK1:2 nM|S1P:26.7 nM
• 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. The inhibition of SPHK1 and S1PR2 activity by PF-543 Citrate significantly hindered pancreatic fibrosis in CP mice.
• 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.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

S1PReceptor, S1P Receptor, SPHK1, Sphingosine Kinase 1 Inhibitor II Citrate, Sphingosine 1-phosphate, PF 543 Citrate, PF543 Citrate, PF-543 Citrate

Compound Identifiers

PubChem CID

71576669