Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C13H12ClN3O3S |
| Molecular Weight | 325.771 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
COC1=CC=C(Cl)C=C1C2=CC(=O)NC(=S)N2CC(N)=O
InChI
InChIKey=ICYNYWFGIDGBRD-UHFFFAOYSA-N
InChI=1S/C13H12ClN3O3S/c1-20-10-3-2-7(14)4-8(10)9-5-12(19)16-13(21)17(9)6-11(15)18/h2-5H,6H2,1H3,(H2,15,18)(H,16,19,21)
| Molecular Formula | C13H12ClN3O3S |
| Molecular Weight | 325.771 |
| Charge | 0 |
| Count |
|
| Stereochemistry | ACHIRAL |
| Additional Stereochemistry | No |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 0 |
| Optical Activity | NONE |
PF-06282999 is selective myeloperoxidase inactivator. PF-06282999 selectively activated human pregnane X receptor (PXR). Treatment of human HepaRG cells with PF-06282999 led to ∼14-fold induction in CYP3A4 mRNA and 5-fold increase in midazolam-1'-hydroxylase activity. [18F]-Fluoro-deoxy-glucose (FDG) was administered to Ldlr-/- mice with established atherosclerosis that had been treated with clinically relevant doses of PF-06282999, and reduced FDG signal was observed in animals treated with a dose of PF-06282999 that corresponded with reduced necrotic core area. PF-06282999 was developed for the treatment of acute coronary syndromes.
Originator
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 11:52:01 GMT 2023
by
admin
on
Sat Dec 16 11:52:01 GMT 2023
|
| Record UNII |
YO3O4Q2NC8
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| Record Status |
Validated (UNII)
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| Record Version |
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-
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Systematic Name | English | ||
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Systematic Name | English |
| Code System | Code | Type | Description | ||
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71571306
Created by
admin on Sat Dec 16 11:52:02 GMT 2023 , Edited by admin on Sat Dec 16 11:52:02 GMT 2023
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300000041364
Created by
admin on Sat Dec 16 11:52:02 GMT 2023 , Edited by admin on Sat Dec 16 11:52:02 GMT 2023
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1435467-37-0
Created by
admin on Sat Dec 16 11:52:02 GMT 2023 , Edited by admin on Sat Dec 16 11:52:02 GMT 2023
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PRIMARY | |||
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YO3O4Q2NC8
Created by
admin on Sat Dec 16 11:52:02 GMT 2023 , Edited by admin on Sat Dec 16 11:52:02 GMT 2023
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DB11683
Created by
admin on Sat Dec 16 11:52:02 GMT 2023 , Edited by admin on Sat Dec 16 11:52:02 GMT 2023
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PRIMARY |
| Related Record | Type | Details | ||
|---|---|---|---|---|
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EXCRETED UNCHANGED |
within 24 hours postdose at the 200-mg dose
URINE
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TRANSPORTER -> SUBSTRATE | |||
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METABOLIC ENZYME -> INDUCER |
MODERATE INDUCER THROUGH MEDIATED BY THE PREGNANE X RECEPTOR
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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METABOLITE -> PARENT |
Metabolite was observed in liver microsomes and hepatocytes from preclinical species and humans.
TRACE
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METABOLITE -> PARENT |
Metabolite was observed in liver microsomes and hepatocytes from preclinical species and humans.
TRACE
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| Related Record | Type | Details | ||
|---|---|---|---|---|
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ACTIVE MOIETY |
| Name | Property Type | Amount | Referenced Substance | Defining | Parameters | References |
|---|---|---|---|---|---|---|
| Tmax | PHARMACOKINETIC |
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P.O. ADMINISTRATION |
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| Tmax | PHARMACOKINETIC |
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P.O. ADMINISTRATION |
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| Biological Half-life | PHARMACOKINETIC |
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SINGLE DOSE |
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| Biological Half-life | PHARMACOKINETIC |
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SINGLE DOSE |
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