Home / Pharmacology / Enzymes / Transferases / Diacylglycerol O-Acyltransferase / Diacylglycerol O-Acyltransferase Inhibitors / PF 06424439

PF 06424439

Cat. No. 6348 4 Citations 1 Review Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
Description: Potent and selective DGAT2 inhibitor
Chemical Name: [(3R)-1-[2-[1-(4-Chloro-1H-pyrazol-1-yl)cyclopropyl]-3H-imidazo[4,5-b]pyridin-5-yl]-3-piperidinyl]-1-pyrrolidinylmethanone methanesulfonate
Purity: ≥98% (HPLC)
Datasheet
Citations (4)
Reviews (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for PF 06424439

PF 06424439 is a potent and selective DGAT2 inhibitor (IC50 = 14 nM). Exhibits no significant activity at MGAT1-3 or DGAT1. Reduces triglyderide synthesis in human hepatocytes in vitro. Reduces plasma triglyceride and cholesterol levels in a rat dyslipidemia model. Orally bioavailable.

Licensing Information

Sold for research purposes under agreement from Pfizer Inc.

Technical Data for PF 06424439

M. Wt 536.05
Formula C22H26ClN7O.CH4O3S
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 1469284-79-4
PubChem ID 89854212
InChI Key ZSTFDNQQOJUJFL-XFULWGLBSA-N
Smiles ClC(C=N1)=CN1C2(CC2)C3=NC4=CC=C(N5C[C@H](C(N6CCCC6)=O)CCC5)N=C4N3.O=S(C)(O)=O

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for PF 06424439

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 53.6 100
DMSO 53.6 100

Preparing Stock Solutions for PF 06424439

The following data is based on the product molecular weight 536.05. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.87 mL 9.33 mL 18.65 mL
5 mM 0.37 mL 1.87 mL 3.73 mL
10 mM 0.19 mL 0.93 mL 1.87 mL
50 mM 0.04 mL 0.19 mL 0.37 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.
=
x
x
g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

=
÷

Dilution Calculator

Calculate the dilution required to prepare a stock solution.
x
=
x

Product Datasheets for PF 06424439

Certificate of Analysis / Product Datasheet
Select another batch:
Safety Datasheet

References for PF 06424439

References are publications that support the biological activity of the product.

Futatsugi et al (2015) Discovery and optimization of imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2). J.Med.Chem. 58 7173 PMID: 26349027

If you know of a relevant reference for PF 06424439, please let us know.

View Related Products by Target

View Related Products by Product Action

View all Diacylglycerol O-Acyltransferase Inhibitors

Keywords: PF 06424439, PF 06424439 supplier, PF06424439, diacylglyercol, O-Acyltransferases, DGAT2, inhibitors, inhibits, potent, selective, orally, bioavailable, dyslipidemia, Diacylglycerol, O-Acyltransferase, 6348, Tocris Bioscience

4 Citations for PF 06424439

Citations are publications that use Tocris products. Selected citations for PF 06424439 include:

Jian et al (2020) ABHD5 suppresses cancer cell anabolism through lipolysis-dependent activation of the AMPK/mTORC1 pathway. J Biol Chem 296 100104 PMID: 33219129

Kai et al (2021) BATF Regulates T Regulatory Cell Functional Specification and Fitness of Triglyceride Metabolism in Restraining Allergic Responses. J Immunol 206 2088-2100 PMID: 33879580

Naomi P et al (2023) An AI-guided screen identifies probucol as an enhancer of mitophagy through modulation of lipid droplets. PLoS Biol 21 e3001977 PMID: 36862640

Soeren S et al (2022) Reducing lipid bilayer stress by monounsaturated fatty acids protects renal proximal tubules in diabetes. Elife 11 PMID: 35550039

Do you know of a great paper that uses PF 06424439 from Tocris? Please let us know.

Reviews for PF 06424439

Average Rating: 5 (Based on 1 Review.)

5 Star
100%
4 Star
0%
3 Star
0%
2 Star
0%
1 Star
0%

Have you used PF 06424439?

Submit a review and receive an Amazon gift card.

$50/€35/£30/$50CAN/¥300 Yuan/¥5000 Yen for first to review with an image

$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image

$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image

Submit a Review

Filter by:


Works great!.
By Qing Li on 10/19/2022
Assay Type: In Vitro
Species: Mouse
Cell Line/Tissue: BMDM

I incubated BMDM with this inhibitor, it reduced the lipid level. Works great!

review image