Details
| Stereochemistry | ABSOLUTE |
| Molecular Formula | C26H24N2O4 |
| Molecular Weight | 428.4798 |
| Optical Activity | UNSPECIFIED |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)[C@@H]1CCC[C@H]1C(=O)C2=CC=C(C=C2)C3=CC=C(NC(=O)NC4=CC=CC=C4)C=C3
InChI
InChIKey=BOZRFEQDOFSZBV-DHIUTWEWSA-N
InChI=1S/C26H24N2O4/c29-24(22-7-4-8-23(22)25(30)31)19-11-9-17(10-12-19)18-13-15-21(16-14-18)28-26(32)27-20-5-2-1-3-6-20/h1-3,5-6,9-16,22-23H,4,7-8H2,(H,30,31)(H2,27,28,32)/t22-,23-/m1/s1
| Molecular Formula | C26H24N2O4 |
| Molecular Weight | 428.4798 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ABSOLUTE |
| Additional Stereochemistry | No |
| Defined Stereocenters | 2 / 2 |
| E/Z Centers | 0 |
| Optical Activity | UNSPECIFIED |
DescriptionSources: https://www.ncbi.nlm.nih.gov/pubmed/19478132Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/18183944
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19478132
Curator's Comment: Description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/18183944
A-922500 is a potent, selective, and orally bioavailable DGAT-1 inhibitor. 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. A-922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the maximal postprandial rise in serum triglyceride concentrations. DGAT-1 inhibition by A-922500 can be a novel therapeutic approach to the treatment of hypertriglyceridemia in humans.
Originator
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/19478132
Zucker fatty rats and diet-induced dyslipidemic hamsters were dosed orally with A-922500 (0.03, 0.3, and 3-mg/kg) for 14 days. Serum triglycerides were significantly reduced by the 3 mg/kg dose
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/18183944
A922500 inhibits human recombinant DGAT1 expressed in Sf9 cells with IC50 of 7 nM
| Substance Class |
Chemical
Created
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Edited
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