PF 06424439
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%
Biological Activity
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.Technical Data
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.
Additional Information
Background References
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Discovery and optimization of imidazopyridine-based inhibitors of diacylglycerol acyltransferase 2 (DGAT2).
Futatsugi et al.
J.Med.Chem., 2015;58:7173
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Citations for PF 06424439
The citations listed below are publications that use Tocris products. Selected citations for PF 06424439 include:
4 Citations: Showing 1 - 4
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An AI-guided screen identifies probucol as an enhancer of mitophagy through modulation of lipid droplets.
Authors: Naomi P Et al.
PLoS Biol 2023;21:e3001977
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Reducing lipid bilayer stress by monounsaturated fatty acids protects renal proximal tubules in diabetes.
Authors: Soeren S Et al.
Elife 2022;11
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BATF Regulates T Regulatory Cell Functional Specification and Fitness of Triglyceride Metabolism in Restraining Allergic Responses.
Authors: Kai Et al.
J Immunol 2021;206:2088-2100
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ABHD5 suppresses cancer cell anabolism through lipolysis-dependent activation of the AMPK/mTORC1 pathway.
Authors: Jian Et al.
J Biol Chem 2020;296:100104
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