A922500

Catalog No.S2674

A922500 Chemical Structure

Molecular Weight(MW): 428.48

A922500 is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.

Size Price Stock Quantity  
In DMSO USD 260 In stock
USD 150 In stock
USD 210 In stock
USD 670 In stock
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Biological Activity

Description A922500 is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.
Features A potent, selective, and orally bioavailable DGAT-1 inhibitor.
Targets
human DGAT-1 [1] mouse DGAT-1 [1] DGAT-2 [1]
7 nM 24 nM 53 μM
In vitro

A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. [1] A 922500 potently inhibits huDGAT-1 and mseDGAT-1. [2]

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. [1] 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. [2] A 922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations. [3]

Protocol

Animal Research:[1]
+ Expand
  • Animal Models: Thirteen-week-old male Golden Syrian hamsters with hyperlipidemia, Ten-week-old Male Zucker fatty rats
  • Formulation: Polyethylene glycol/hydroxypropyl-β-cyclodextrin (10% w/v)
  • Dosages: 0.03, 0.3, and 3 mg/kg
  • Administration: Oral gavage
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 86 mg/mL (200.7 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 15% Captisol 20 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 428.48
Formula

C26H24N2O4

CAS No. 959122-11-3
Storage powder
in solvent
Synonyms N/A

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Transferase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID