Free shipping on all orders over $ 500

Ervogastat

Cat. No. M21575
Ervogastat Structure
Synonym:

PF-06865571

Size Price Availability Quantity
5mg USD 400  USD400 In stock
10mg USD 600  USD600 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

Ervogastat is a DGAT2 inhibitor that can be used in studies related to non-alcoholic steatohepatitis (NASH).

Chemical Information
Molecular Weight 407.42
Formula C21H21N5O4
CAS Number 2186700-33-2
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Raman Sharma, et al. Chem Res Toxicol. Mitigating a Bioactivation Liability with an Azetidine-Based Inhibitor of Diacylglycerol Acyltransferase 2 (DGAT2) En Route to the Discovery of the Clinical Candidate Ervogastat

[2] Neeta B Amin, et al. Clin Ther. Inhibition of Diacylglycerol Acyltransferase 2 Versus Diacylglycerol Acyltransferase 1: Potential Therapeutic Implications of Pharmacology

[3] Kentaro Futatsugi, et al. J Med Chem. Discovery of Ervogastat (PF-06865571): A Potent and Selective Inhibitor of Diacylglycerol Acyltransferase 2 for the Treatment of Non-alcoholic Steatohepatitis

[4] Natasha R Catlin, et al. Toxicol Sci. The Postnatal Resolution of Developmental Toxicity Induced by Pharmacological Diacylglycerol Acyltransferase 2 (DGAT2) Inhibition During Gestation in Rats

[5] Neeta B Amin, et al. BMJ Open. Efficacy and safety of an orally administered DGAT2 inhibitor alone or coadministered with a liver-targeted ACC inhibitor in adults with non-alcoholic steatohepatitis (NASH): rationale and design of the phase II, dose-ranging, dose-finding, randomised, placebo-controlled MIRNA (Metabolic Interventions to Resolve NASH with fibrosis) study

Related DGAT Products
PF-07202954

PF-07202954 is an orally active, weakly basic DGAT2 inhibitor with an IC50 of 10 nM for human DGAT2.PF-07202954 reduces hepatic triglycerides in an obese rat model.

ION224

ION224 is an antisense compound that targets DGAT-2 for studies related to non-alcoholic steatohepatitis (NASH).

PF-07055341

PF-07055341 is a DGAT1/2 inhibitor that can be used in studies related to non-alcoholic steatohepatitis (NASH).

Pradigastat

Pradigastat (LCQ-908) is a potent, selective and orally active diacylglycerol acyltransferase 1 (DGAT1) inhibitor. Pradigastat has anti-obesity and anti-diabetic effects.

DGAT-1 inhibitor 2

DGAT-1 inhibitor 2 is an effective inhibitor of DGAT-1;antiobesity agents.

  Catalog
Abmole Inhibitor Catalog




Keywords: Ervogastat, PF-06865571 supplier, DGAT, inhibitors, activators


Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.