Details
| Stereochemistry | RACEMIC |
| Molecular Formula | C20H17F3N2O5 |
| Molecular Weight | 422.3554 |
| Optical Activity | ( + / - ) |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COc1ccc(cc1C(=NCc2ccc(cc2)C(F)(F)F)O)CC3C(=NC(=O)O3)O
InChI
InChIKey=ORZMUVMQJPGFOM-UHFFFAOYSA-N
InChI=1S/C20H17F3N2O5/c1-29-15-7-4-12(9-16-18(27)25-19(28)30-16)8-14(15)17(26)24-10-11-2-5-13(6-3-11)20(21,22)23/h2-8,16H,9-10H2,1H3,(H,24,26)(H,25,27,28)
| Molecular Formula | C20H17F3N2O5 |
| Molecular Weight | 422.3554 |
| Charge | 0 |
| Count |
|
| Stereochemistry | RACEMIC |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 1 |
| E/Z Centers | 0 |
| Optical Activity | ( + / - ) |
MK-0767 is a potent hypoglycaemic insulin sensitizer being evaluated by Kyorin with potential as an antidiabetic agent. MK-0767 acts as a dual agonist of the peroxisome proliferator-activated receptors alpha and gamma, induced high-affinity interactions of PPARα and PPARγ with the transcriptional coactivator CBP in vitro. In ob/ob mice, MK-0767 normalized hyperglycemia and hyperinsulinemia with equal or greater potency and efficacy than pioglitazone. Treatment of hamsters with MK-0767 produced substantial reductions in blood cholesterol and triglycerides. In dogs, MK-0767 reduced serum cholesterol levels with a potency more than 10-fold greater than simvastatin. The efficacies of MK-0767 and simvastatin were additive when given together.
Approval Year
PubMed
| Title | Date | PubMed |
|---|---|---|
| A novel insulin sensitizer acts as a coligand for peroxisome proliferator-activated receptor-alpha (PPAR-alpha) and PPAR-gamma: effect of PPAR-alpha activation on abnormal lipid metabolism in liver of Zucker fatty rats. | 1998 Dec |
|
| (3-substituted benzyl)thiazolidine-2,4-diones as structurally new antihyperglycemic agents. | 1999 Feb 22 |
|
| Fatty-acyl-CoA thioesters inhibit recruitment of steroid receptor co-activator 1 to alpha and gamma isoforms of peroxisome-proliferator-activated receptors by competing with agonists. | 2001 Jan 15 |
|
| [KRP-297, MCC-555]. | 2001 Nov |
|
| MK-767. Kyorin/Banyu/Merck. | 2003 Apr |
|
| Combination therapy with PPARgamma and PPARalpha agonists increases glucose-stimulated insulin secretion in db/db mice. | 2003 May |
|
| MK-0767, a novel dual PPARalpha/gamma agonist, displays robust antihyperglycemic and hypolipidemic activities. | 2004 May 28 |
Patents
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Jun 26 06:24:15 UTC 2021
by
admin
on
Sat Jun 26 06:24:15 UTC 2021
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| Record UNII |
Y180U02GSB
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| Record Status |
Validated (UNII)
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| Record Version |
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934017-32-0
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Y180U02GSB
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DB12055
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56842109
Created by
admin on Sat Jun 26 06:24:16 UTC 2021 , Edited by admin on Sat Jun 26 06:24:16 UTC 2021
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METABOLIC ENZYME -> SUBSTRATE |
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ACTIVE MOIETY |
