1. Metabolic Enzyme/Protease
  2. Acyltransferase

A 922500 (Synonyms: DGAT-1 Inhibitor 4a)

Cat. No.: HY-10038 Purity: 98.50%
Handling Instructions

A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor exhibiting IC50 values of 9 and 22 nM against human and mouse DGAT-1, respectively.

For research use only. We do not sell to patients.
A 922500 Chemical Structure

A 922500 Chemical Structure

CAS No. : 959122-11-3

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 139 In-stock
5 mg USD 126 In-stock
10 mg USD 176 In-stock
50 mg USD 563 In-stock
100 mg USD 840 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References


A 922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor exhibiting IC50 values of 9 and 22 nM against human and mouse DGAT-1, respectively.

IC50 & Target

IC50: 9 nM (human DGAT-1), 22 nM (mouse DGAT-1)[1]

In Vitro

A 922500 (A-922500) demonstrates excellent selectivity over other acyltransferases, including DGAT-2 (IC50=53 μM) and the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 (IC50=296 μM) [1].

In Vivo

DGAT-1 inhibitor A 922500 (A-922500) reduces serum triglyceride levels from baseline at all doses tested; however, this is only statistically significant at the 3 mg/kg dose, which lowers serum triglycerides by 53%. Similarly, the 3 mg/kg dose of A 922500 significantly reduces serum FFA concentrations by 55% and total cholesterol by 25%. DGAT-1 inhibition has no significant effect on body weight at any dose tested. Although A 922500 dpes not significantly affect LDL-cholesterol or HDL-cholesterol individually, the serum LDL/HDL-cholesterol ratio is significantly improved by A 922500 at 0.3 and 3 mg/kg. Similar to the dyslipidemic hamster, treatment with 3 mg/kg A 922500 significantly reduces serum triglyceride concentrations (39%). FFA levels significantly increase over the 14-day period in vehicle-treated animals. This increase is inhibited in a dose-dependent manner by A 922500 such that FFA concentrations are 32% lower after 14 days of treatment with the DGAT-1 inhibitor at 3 mg/kg, compared with the vehicle group (p < 0.05). HDL-cholesterol is significantly increased from baseline levels by A 922500 at 0.3 and 3 mg/kg; however, this is only significantly increased compared with vehicle at the 3 mg/kg dose. Body weight significantly increases over the 2-week period in vehicle-treated rats, and this is not affected by A 922500. LDL-cholesterol is significantly reduced in the vehicle treated group. DGAT-1 inhibition does not further reduce LDL-cholesterol and has no effect on total cholesterol[1].

Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 2.3338 mL 11.6692 mL 23.3383 mL
5 mM 0.4668 mL 2.3338 mL 4.6677 mL
10 mM 0.2334 mL 1.1669 mL 2.3338 mL
Please refer to the solubility information to select the appropriate solvent.
Animal Administration

A 922500 (A-922500) is prepared in vehicle [20:80 (v/v), polyethylene glycol/hydroxypropyl-β-cyclodextrin (10% w/v)] (Mice and Hamsters)[1].

Mice and Hamsters[1]
Thirteen-week-old male Golden Syrian hamsters (n=40), initially weighing approximately 140 g, are used. Ten-week-old Male Zucker fatty rats (n=32), weighing between 270 and 330 g, are used. After collection of baseline lipid profiles, hyperlipidemic hamsters (n=10/group) and Zucker fatty rats (n=8/group) are administered vehicle [20:80 (v/v), polyethylene glycol/hydroxypropyl-β-cyclodextrin (10% w/v)] or DGAT-1 inhibitor A 922500 (A-922500) at 0.03, 0.3, and 3 mg/kg, once daily by oral gavage. The dosing volume is 5 mL/kg. Serum lipid profiles are then measured 3 h after the dose on day 7 and day 14. Hamsters continue to be fed a high-fat diet with 10% fructose in the drinking water throughout the treatment period. Zucker fatty rats remain on standard rodent diet throughout the study.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight







O=C(NC1=CC=C(C2=CC=C(C([[email protected]@H]3CCC[[email protected]]3C(O)=O)=O)C=C2)C=C1)NC4=CC=CC=C4

Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month

Room temperature in continental US; may vary elsewhere

Solvent & Solubility


* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 98.50%

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