DGAT-1 inhibitor
DGAT-1 inhibitor Basic information
- Product Name:
- DGAT-1 inhibitor
- Synonyms:
-
- (1R,2R)-2-[[4'-[[(Phenylamino)carbonyl]amino][1,1'-biphenyl]-4-yl]carbonyl]cyclopentanecarboxylic acid
- DGAT-1 inhibitor
- Diacyl glycerolacyltransferase 1 inhibitor
- A922500
- A922500(DGAT-1 Inhibitor 4a)
- enylureido)biphenyl(1R,2R)-2-(4'-(3-phcarbonyl)cyclopentanecarboxylic acid
- DGAT-1 Inhibitor 4a
- (1R,2R)-2-(4'-(3-phenylureido)biphenylcarbonyl)cyclopentanecarboxylic acid
- CAS:
- 959122-11-3
- MF:
- C26H24N2O4
- MW:
- 428.48
- Product Categories:
-
- Inhibitor
- Inhibitors
- APIs
- Mol File:
- 959122-11-3.mol
DGAT-1 inhibitor Chemical Properties
- Density
- 1.323
- storage temp.
- -20°C
- solubility
- ≥21.25 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH
- form
- Light yellow solid
DGAT-1 inhibitor Usage And Synthesis
Uses
A922500 has been used in the inhibition of diacylglycerol acyltransferase (DGAT) in epithelial human breast cancer cell line (MDA-MB-231), digitonin-permeabilized human cancer cells, human myotubes and macrophages.
Definition
ChEBI: A 922500 is an aromatic ketone.
Biological Activity
Diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC 50 values are 7 and 24 nM at human and mouse DGAT-1 respectively) that is devoid of activity at DGAT-2, ACAT1 or ACAT2. Induces significant weight loss without altering food intake, and decreases liver and plasma triglyceride levels in vivo . Orally active.
Biochem/physiol Actions
The diacylglycerol acyltransferase (DGAT) 1 inhibitor A922500 was shown to effectively reduce postprandial serum triglyceride levels in rodents at concentrations of 0.03, 0.3 and 3 mg/kg. These results suggest A922500 may have beneficial effects in reducing the risk of cardiovascular disease.
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