| Identification | Back Directory | [Name]
DGAT-1 inhibitor | [CAS]
959122-11-3 | [Synonyms]
CS-121
A922500
DGAT-1 inhibitor
DGAT-1 Inhibitor 4a
DGAT-1 Inhibitor, A 922500
DGAT-1 inhibitor USP/EP/BP
A922500(DGAT-1 Inhibitor 4a)
DGAT-1 INHIBITOR 4A; A-922500; A922500
Diacyl glycerolacyltransferase 1 inhibitor
DGAT-1 Inhibitor, A 922500 - CAS 959122-11-3 - Calbiochem
enylureido)biphenyl(1R,2R)-2-(4'-(3-phcarbonyl)cyclopentanecarboxylic acid
(1R,2R)-2-(4'-(3-phenylureido)biphenylcarbonyl)cyclopentanecarboxylic acid
(1R,2R)-2-(4,-(3-phenylureido)-[1,1,-biphenyl]-4-carbonyl)cyclopentanecarboxylic acid
(1R,2R)-2-[[4'-[[(Phenylamino)carbonyl]amino][1,1'-biphenyl]-4-yl]carbonyl]cyclopentanecarboxylic acid
Cyclopentanecarboxylic acid, 2-[[4'-[[(phenylamino)carbonyl]amino][1,1'-biphenyl]-4-yl]carbonyl]-, (1R,2R)- | [Molecular Formula]
C26H24N2O4 | [MDL Number]
MFCD12828780 | [MOL File]
959122-11-3.mol | [Molecular Weight]
428.48 |
| Chemical Properties | Back Directory | [density ]
1.323 | [storage temp. ]
-20°C | [solubility ]
≥21.25 mg/mL in DMSO; insoluble in H2O; insoluble in EtOH | [form ]
Light yellow solid | [color ]
light yellow | [biological source]
synthetic (organic) |
| Hazard Information | Back Directory | [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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