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A 922500

Catalog No. T6365   CAS 959122-11-3
Synonyms: A922500, DGAT-1 Inhibitor 4a

A 922500 (DGAT-1 Inhibitor 4a) 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.

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A 922500 Chemical Structure
A 922500, CAS 959122-11-3
Pack Size Availability Price/USD Quantity
1 mg In stock $ 45.00
2 mg In stock $ 63.00
5 mg In stock $ 97.00
10 mg In stock $ 143.00
25 mg In stock $ 269.00
50 mg In stock $ 453.00
100 mg In stock $ 667.00
1 mL * 10 mM (in DMSO) In stock $ 112.00
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Purity: 97.34%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description A 922500 (DGAT-1 Inhibitor 4a) 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.
Targets&IC50 mouse DGAT-1:24 nM, human DGAT-1:7 nM
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]
Synonyms A922500, DGAT-1 Inhibitor 4a
Molecular Weight 428.48
Formula C26H24N2O4
CAS No. 959122-11-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 21.4 mg/mL (50 mM)

TargetMolReferences and Literature

1. King AJ et al. J Pharmacol Exp Ther. 2009, 330(2), 526-531. 2. Zhao G, et al. J Med Chem. 2008, 51(3), 380-383. 3. King AJ, et al. Eur J Pharmacol. 2010, 637(1-3), 155-161. 4. Masouleh S K. Lipid droplet formation drives pathogenic ILC2 responses in airway inflammation . 5. Karagiannis F, Masouleh S K, Wunderling K, et al. Lipid-Droplet Formation Drives Pathogenic Group 2 Innate Lymphoid Cells in Airway Inflammation[J]. Immunity. 2020, 52(4): 620-634. e6.

TargetMolCitations

1. Masouleh S K. Lipid droplet formation drives pathogenic ILC2 responses in airway inflammation. Immunity. 2020 2. Karagiannis F, Masouleh S K, Wunderling K, et al. Lipid-Droplet Formation Drives Pathogenic Group 2 Innate Lymphoid Cells in Airway Inflammation. Immunity. 2020, 52(4): 620-634. e6. 3. Wang W, Qu Y, Wang X, et al.Genetic variety of ORF3a shapes SARS‐CoV‐2 fitness through modulation of lipid droplet.Journal of Medical Virology.2023

Related compound libraries

This product is contained In the following compound libraries:
Bioactive Compound Library Orally Active Compound Library Lipid Metabolism Compound Library Anti-Obesity Compound Library Metabolism Compound Library Inhibitor Library Bioactive Compounds Library Max Covalent Inhibitor Library NO PAINS Compound Library

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Keywords

A 922500 959122-11-3 Metabolism Acyltransferase Transferase inhibit Inhibitor Diglyceride acyltransferase A922500 mono- acylglycerol acyltransferase acyl-CoA:cholesterol acyltransferase Diacylglycerol acyltransferase DGAT-1 Inhibitor 4a A-922500 inhibitor

 

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