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A 922500

🥰Excellent
Catalog No. T6365Cas No. 959122-11-3
Alias DGAT-1 Inhibitor 4a, A922500

A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor of human and mouse DGAT-1 with IC50 values of 7 nM and 24 nM, respectively, demonstrating good selectivity over related acyltransferases, hERG, and a panel of anti-targets.

A 922500

A 922500

🥰Excellent
Purity: 97.66%
Catalog No. T6365Alias DGAT-1 Inhibitor 4a, A922500Cas No. 959122-11-3
A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor of human and mouse DGAT-1 with IC50 values of 7 nM and 24 nM, respectively, demonstrating good selectivity over related acyltransferases, hERG, and a panel of anti-targets.
Pack SizePriceAvailabilityQuantity
1 mg42 €In Stock
2 mg59 €In Stock
5 mg92 €In Stock
10 mg135 €In Stock
25 mg255 €In Stock
50 mg430 €In Stock
100 mg633 €In Stock
1 mL x 10 mM (in DMSO)106 €In Stock
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Purity:97.66%
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Product Introduction

Bioactivity
Description
A 922500 (DGAT-1 Inhibitor 4a) is an inhibitor of human and mouse DGAT-1 with IC50 values of 7 nM and 24 nM, respectively, demonstrating good selectivity over related acyltransferases, hERG, and a panel of anti-targets.
Targets&IC50
DGAT-1 (human):7 nM, DGAT-1 (mouse):24 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]
AliasDGAT-1 Inhibitor 4a, A922500
Chemical Properties
Molecular Weight428.48
FormulaC26H24N2O4
Cas No.959122-11-3
SmilesOC(=O)[C@@H]1CCC[C@H]1C(=O)c1ccc(cc1)-c1ccc(NC(=O)Nc2ccccc2)cc1
Relative Density.1.323g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 70 mg/mL (163.37 mM), Sonication is recommended.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.3338 mL11.6692 mL23.3383 mL116.6916 mL
5 mM0.4668 mL2.3338 mL4.6677 mL23.3383 mL
10 mM0.2334 mL1.1669 mL2.3338 mL11.6692 mL
20 mM0.1167 mL0.5835 mL1.1669 mL5.8346 mL
50 mM0.0467 mL0.2334 mL0.4668 mL2.3338 mL
100 mM0.0233 mL0.1167 mL0.2334 mL1.1669 mL

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