Details
Stereochemistry | ACHIRAL |
Molecular Formula | C21H24N4O4 |
Molecular Weight | 396.4397 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
NC1=C2C(OCCN(C3=CC=C(C=C3)[C@H]4CC[C@H](CC(O)=O)CC4)C2=O)=NC=N1
InChI
InChIKey=GEVVQZHMFVFGLN-HDJSIYSDSA-N
InChI=1S/C21H24N4O4/c22-19-18-20(24-12-23-19)29-10-9-25(21(18)28)16-7-5-15(6-8-16)14-3-1-13(2-4-14)11-17(26)27/h5-8,12-14H,1-4,9-11H2,(H,26,27)(H2,22,23,24)/t13-,14-
Molecular Formula | C21H24N4O4 |
Molecular Weight | 396.4397 |
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/23871442 | https://www.ncbi.nlm.nih.gov/pubmed/24900321Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800030035
Sources: https://www.ncbi.nlm.nih.gov/pubmed/23871442 | https://www.ncbi.nlm.nih.gov/pubmed/24900321
Curator's Comment: Description was created based on several sources, including http://adisinsight.springer.com/drugs/800030035
PF-04620110 is an orally active, selective and potent DGAT1 (Acyl-CoA:diacylglycerol acyltransferase 1) inhibitor that inhibits triacylglycerol synthesis in cells and in rodents. PF-04620110 inhibits DGAT-1 with an IC50 of 19 nM and shows high selectivity versus a broad panel of off-target pharmacologic end points. In vivo DGAT-1 inhibition has been demonstrated through reduction of plasma triglyceride levels in rodents at doses of ≥0.1 mg/kg following a lipid challenge. On the basis of this pharmacologic and pharmacokinetic profile, PF-04620110 has been advanced to human clinical studies. PF-4620110 had been in phase I clinical trials by Pfizer for the treatment of type 2 diabetes. But this research was discontinued in 2011.
Originator
Sources: http://adisinsight.springer.com/drugs/800030035
Curator's Comment: # Pfizer
Approval Year
Sample Use Guides
In Vivo Use Guide
Sources: https://clinicaltrials.gov/ct2/show/NCT01166217
The five treatments are:
A) single dose of 5 mg immediate release tablets in the fasted state; B) single dose of 5 mg modified release osmotic capsule with a short duration of modified release 1 (MR1) in the fasted state; C) single dose of 5 mg modified release osmotic capsule with a long duration of modified release 2 (MR2) in the fasted state; D) single dose of 5 mg modified release osmotic capsule with a short duration of modified release 1 (MR1) in the fed state; E) single dose of 5 mg modified release osmotic capsule with a long duration of modified release 2 (MR2) in the fed state.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/24900321
PF-04620110 inhibits human DGAT-1 with an IC50 of 19 nM
Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 01:27:30 GMT 2023
by
admin
on
Sat Dec 16 01:27:30 GMT 2023
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Record UNII |
CQ4M18RLJW
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Record Status |
Validated (UNII)
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Record Version |
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