A 922500

SKU: orb1300832

Description

A 922500

Research Area

Metabolism Research

Key Properties

• CAS Number: 959122-11-3
• MW: 428.48
• Purity: 97.66%
• Formula: C₂₆H₂₄N₂O₄
• SMILES: OC(=O)[C@@H]1CCC[C@H]1C(=O)c1ccc(cc1)-c1ccc(NC(=O)Nc2ccccc2)cc1
• Target: Transferase,Acyltransferase
• Solubility: DMSO:73 mg/mL (170.37 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.67 mM)

Bioactivity

• Target IC50:
  DGAT-1 (mouse):24 nM|DGAT-1 (human):7 nM
• In Vivo:
  Zucker fatty rats and diet-induced dyslipidemic hamsters are dosed orally with A 922500 (0.03, 0.3, and 3 mg/kg) for 14 days. Serum triglycerides ae significantly reduced by the 3 mg/kg dose of A 922500 in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%). These serum triglyceride changes are accompanied by significant reductions in free fatty acid levels by 32% in the Zucker fatty rat and 55% in the hyperlipidemic hamster. In addition, high-density lipoprotein-cholesterol is significantly increases (25%) in the Zucker fatty rat by A 922500 administered at 3 mg/kg. A 922500 confers weight loss and a reduction in liver triglycerides when dosed chronically in DIO mice and depletes serum triglycerides following a lipid challenge in a dose-dependent manner, thus, reproducing major phenotypical characteristics of DGAT-1(-/-) mice. A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations.
• In Vitro:
  A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. A 922500 potently inhibits huDGAT-1 and mseDGAT-1.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

DGAT-2, DGAT-1 Inhibitor 4a, Diglyceride acyltransferase, Diacylglycerol acyltransferase, A922500, A-922500, A 922500, Acyltransferase, acyl-CoA:cholesterol acyltransferase, Inhibitor, inhibit, mono- acylglycerol acyltransferase, mouse DGAT-1, human DGAT-1

Compound Identifiers

PubChem CID

24768261