PF 429242

Catalog No.S6418

PF 429242 Chemical Structure

Molecular Weight(MW): 409.56

PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM).

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Biological Activity

Description PF 429242 is known as a S1P inhibitor with an IC50 of 170 nM, showing no significant inhibition of trypsin, elastase, proteinase K, plasmin, kallikren, factor XIa, thrombin, or furin at concentrations up to 100 μM and only modest inhibition of urokinase (IC50 = 50 μM) and factor Xa (IC50 = 100 μM).
Targets
S1P [1]
(Cell-free assay)
170 nM
In vitro

In cultured human liver (Hep-G2) cells, PF-429242 prevents proteolytic processing and nuclear translocation of SREBP, reduces the expression of key genes involved in cholesterol synthesis and fatty acid synthesis, and inhibits both pathways in the absence of any cytotoxicity[1]. The addition of PF-429242 suppresses the viral propagation of all serotypes of DENV in several primate-derived cells[2].

In vivo

PK data for PF-429242 show that it had rapid clearance (CL = 75 ml/min/kg) and poor oral bioavailability (5%) in rats[1].

Protocol

Cell Research:

[2]

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  • Cell lines: HeLa cells
  • Concentrations: 3 to 300 µM
  • Incubation Time: 72 h
  • Method:

    HeLa cells are seeded in MEM supplemented with 2% FCS and 0.2 mM nonessential amino acids, which contained 3 to 300 µM of PF-429242. After 72 h post drug treatment, a CellTiter-Glo mixture is added to the cultured cells, and the intracellular ATP is measured for luminescence intensity with ARVO MX/Light 1420 Multilabel/Luminescence counter.


    (Only for Reference)
Animal Research:

[1]

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  • Animal Models: CD-1 mice
  • Formulation: --
  • Dosages: 10 and 30 mg/kg/dose
  • Administration: i.p.
    (Only for Reference)

References

Solubility (25°C)

In vitro DMSO 82 mg/mL (200.21 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 409.56
Formula

C25H35N3O2

CAS No. 947303-87-9
Storage powder
in solvent
Synonyms N/A

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID