Ervogastat

Ervogastat : Inhibitor of DGAT2

Structure

SERP Rating

In Cells

(2 ratings)

In Model Organisms

(2 ratings)

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Probe Ervogastat is in the process of SERP review.

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Information

DGAT2

Inhibitor

up to 100 nM

Probe Availability:

Selleck Chemicals

In Vitro Validations

Uniprot ID: Q96PD7

Target Class: Enzyme

Target SubClass: Acyltransferase

Potency: IC50

Potency Value: 17.2 nM

Potency Assay: Radiolabelled incorporation assay

PDB ID for probe-target interaction (3D structure): --

Target aliases:

Diacylglycerol O-acyltransferase 2, DGAT2, DGAT2_H ...

DOI Reference: 10.1021/acs.jmedchem.2c01200

In Cell Validations

In Vivo Data

Off-Target Selectivity Assesments

Potency assay (off target): Mouse MGAT1, human MGAT2, human MGAT3, or human DGAT1 potency IC50 > 50 μM Functional assay from Invitrogen panel, ATP = Km, in-house functional assay in antagonist/inhibitor mode and binding assay from CEREP panel using an agonist, antagonist and functional binding were used to assess selectivity @ 10 μM without any relevant hit. CYP IC50 (1A2, 3A4, 2C8, 2C9, 2C19, 2D6) (μM) >30, >30, >24, >30, 7.8, >30, >30, respectively

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SERP ratings and comments

SERP Ratings

In Cell Rating

In Model Organisms

SERP Comments:

PF-0686571 (Ervogastat) is a first-in-class DGAT2 inhibitor that has received Fast Track Designation by the FDA and is currently in Phase 2 for the treatment of NASH or improvement of liver fibrosis. This probe compound has demonstrated potent reversible inhibition against DGAT2 (<20 nM) and selectivity (<50 uM against DGAT1) and no appreciable off-target activity in a CEREP panel. Cellular potency in hepatocytes was found to be <10 nM and robust in vivo efficacy in rat with doses as low as 1 mg/kg. This is a well characterized probe that is suitable for use as a DGAT2 probe (in vitro and in vivo)

(last updated: 10 Oct 2023 )

SERP Ratings

In Cell Rating

In Model Organisms

(last updated: 10 Oct 2023 )