1. GPCR/G Protein
  2. LPL Receptor

PF429242 dihydrochloride 

Cat. No.: HY-13447A Purity: 98.76%
Handling Instructions

PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM.

For research use only. We do not sell to patients.
PF429242 dihydrochloride Chemical Structure

PF429242 dihydrochloride Chemical Structure

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 106 In-stock
5 mg USD 96 In-stock
10 mg USD 168 In-stock
25 mg USD 336 In-stock
50 mg USD 600 In-stock
100 mg USD 1056 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PF429242 dihydrochloride is a reversible and competitive S1P inhibitor with an IC50 of 175 nM.

IC50 & Target

IC50: 175 nM (S1P)[1]

In Vitro

10 μM PF-429242 inhibits endogenous SREBP processing in Chinese hamster ovary cells. PF-429242 also down-regulates the signal from an SRE-luciferase reporter gene in human embryonic kidney 293 cells and the expression of endogenous SREBP target genes in cultured HepG2 cells. In HepG2 cells, PF-429242 inhibits cholesterol synthesis, with an IC50 of 0.5 μM[1]. The addition of PF-429242 (30 μM) shows statistically significant suppression of infectious viral titers and viral RNA copies in the cell culture fluids. PF-429242 treatment also shows suppressive effects on DENV2 yields in the cultured fluids of human-derived HEK-293, Hep G2, and non-human-primate derived LLC-MK2 cells[2]. PF-429242 efficiently prevents the processing of GPC from the prototypic arenavirus lymphocytic choriomeningitis virus (LCMV) and LASV, which correlates with the compound's potent antiviral activity against LCMV and LASV in cultured cells[3].

In Vivo

In mice treated with PF-429242 for 24 h, the expression of hepatic SREBP target genes is suppressed, and the hepatic rates of cholesterol and fatty acid synthesis are reduced[1].

References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.0726 mL 10.3629 mL 20.7258 mL
5 mM 0.4145 mL 2.0726 mL 4.1452 mL
10 mM 0.2073 mL 1.0363 mL 2.0726 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

PF-429242 is prepared in saline.

Mice: To test the in vivo efficacy of PF-429242 in regulating SREBP target genes, male CD1 mice are dosed i.p. with 10 or 30 mg/kg PF-429242 or saline once every 6 over a 24-h period. Mice are euthanized 6 h after the final dose, and liver tissue is collected, frozen rapidly in liquid nitrogen, and stored at -80°C. For RNA isolation, 50 to 100 mg of frozen liver tissue from each sample is homogenized in 1 ml of TRIzol reagent. Total RNA is extracted following the manufacturer's instructions, and the resulting total RNA from each sample underwent DNA-free treatment[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

482.49

Formula

C₂₅H₃₇Cl₂N₃O₂

SMILES

O=C(N(CCC1=CC=CC=C1OC)[[email protected]]2CNCC2)C3=CC=C(CN(CC)CC)C=C3.[H]Cl.[H]Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: ≥ 83.3 mg/mL

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
PF429242 dihydrochloride
Cat. No.:
HY-13447A
Quantity: