Home GPCR & G Protein S1P Receptor inhibitor PF 429242 For research use only.

PF 429242

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).

PF 429242 Chemical Structure

PF 429242 Chemical Structure

CAS No. 947303-87-9

Purity & Quality Control

PF 429242 Related Products

Signaling Pathway

S1P Receptor Signaling Pathways

S1P Receptor Signaling Pathway

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 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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models CD-1 mice
Dosages 10 and 30 mg/kg/dose
Administration i.p.

Chemical Information & Solubility

Molecular Weight 409.56 Formula

C25H35N3O2
CAS No. 947303-87-9 SDF --
Smiles CCN(CC)CC1=CC=C(C=C1)C(=O)N(CCC2=CC=CC=C2OC)C3CCNC3
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 82 mg/mL ( (200.21 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 82 mg/mL

Ethanol : 82 mg/mL


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In vivo
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Tech Support

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

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