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PF-543 Citrate

Cat. No. M9455
PF-543 Citrate Structure
Size Price Availability
10mg USD 135  USD150 Out of stock
50mg USD 387  USD430 Out of stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

PF-543 Citrate is a novel selective SK-1 inhibitor which inhibited SK-1 activity in a competitive manner with sphingosine. PF-543 inhibits SphK1 with a K(i) of 3.6 nM, is sphingosine-competitive and is more than 100-fold selective for SphK1 over the SphK2 isoform. PF-543 was effective as a potent inhibitor of S1P formation in whole blood, indicating that the SphK1 isoform of sphingosine kinase is the major source of S1P in human blood. PF-543 Citrate induces apoptosis, necrosis, and autophagy.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 657.73
Formula C33H39NO11S
CAS Number 1415562-83-2
Purity >98%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

Induction of autophagy by sphingosine kinase 1 inhibitor PF-543 in head and neck squamous cell carcinoma cells.
Hamada M, et al. Cell Death Discov. 2017 Aug 14;3:17047. PMID: 29109864.

Effect of the sphingosine kinase 1 selective inhibitor, PF-543 on arterial and cardiac remodelling in a hypoxic model of pulmonary arterial hypertension.
MacRitchie N, et al. Cell Signal. 2016 Aug;28(8):946-55. PMID: 27063355.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: PF-543 Citrate supplier, S1P Receptor, inhibitors

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