PF 06424439

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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)
Citations (4)
Reviews (1)

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
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
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

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Product Datasheets for PF 06424439

Certificate of Analysis / Product Datasheet
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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.

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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:

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

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

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

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.)

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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!

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