PF 429242

Catalog No.S6418 Batch:S641803

Technical Data

Formula

C₂₅H₃₅N₃O₂

Molecular Weight

409.56

CAS No.

947303-87-9

Solubility (25°C)*

In vitro

DMSO

82 mg/mL (200.21 mM)

Water

82 mg/mL (200.21 mM)

Ethanol

82 mg/mL (200.21 mM)

In vivo (Add solvents to the product individually and in order)

Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.1mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 82 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil	0.51mg/ml	Taking the 1 mL working solution as an example, add 50 μL of 10.2 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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 (from reference)

Cell Assay:^{^[2]}	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.
Animal Study:^{^[1]}	Animal Models CD-1 mice Dosages 10 and 30 mg/kg/dose Administration i.p.

Cell Assay:^{^[2]}

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.

Animal Study:^{^[1]}

Animal Models
CD-1 mice
Dosages
10 and 30 mg/kg/dose
Administration
i.p.

References

Selleck's PF 429242 has been cited by 2 publications

The Scap-SREBP1-S1P/S2P lipogenesis signal orchestrates the homeostasis and spatiotemporal activation of NF-κB [ Cell Rep, 2023, 42(6):112586]	PubMed: 37267109
RORγ Is a Targetable Master Regulator of Cholesterol Biosynthesis in a Cancer Subtype [ Nat Commun, 2019, 11;10(1):4621]	PubMed: 31604910

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.