Free shipping on all orders over $ 500

A-922500

Cat. No. M2059
A-922500 Structure
Synonym:

DGAT-1 Inhibitor 4a; A922500

Size Price Availability Quantity
5mg USD 125  USD125 In stock
10mg USD 175  USD175 In stock
50mg USD 550  USD550 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control & Documentation
Biological Activity

A-922500 (DGAT-1 Inhibitor 4a) is a potent orally active inhibitor of DGAT-1 activity, inhibiting both human and mouse forms of the enzymes with IC50 values of 9 and 22 nM, respectively. DGAT-1 deficient mice demonstrate a phenotype that is protective against the development of diet-induced obesity (DIO) or insulin resistance, implicating the actions of this enzyme in the development of such metabolic disorders. A-922500 conferred significant weight loss within seven days without affecting food intake and significantly reduced plasma and liver triglycerides with chronic dosing when administered at 3 mg/kg to DIO mice. DGAT-1 inhibitor A-922500 (0.03, 0.3 and 3 mg/kg, p.o.), dose-dependently attenuated the maximal postprandial rise in serum triglyceride concentrations. A-922500 is devoid of activity at DGAT-2, ACAT1 or ACAT2.

Chemical Information
Molecular Weight 428.48
Formula C26H24N2O4
CAS Number 959122-11-3
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] King AJ, et al. J Pharmacol Exp Ther. Diacylglycerol acyltransferase 1 inhibition lowers serum triglycerides in the Zucker fatty rat and the hyperlipidemic hamster.

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).

Ervogastat

Ervogastat is a DGAT2 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.

  Catalog
Abmole Inhibitor Catalog




Keywords: A-922500, DGAT-1 Inhibitor 4a; A922500 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.