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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
Structure of PF-06282999

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)

HIDE SMILES / InChI
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.

Approval Year

Targets

Targets

Primary TargetPharmacologyConditionPotency
1.9 µM [IC50]
PubMed

PubMed

TitleDatePubMed
Establishing Transcriptional Signatures to Differentiate PXR-, CAR-, and AhR-Mediated Regulation of Drug Metabolism and Transport Genes in Cryopreserved Human Hepatocytes.
2018 May
Myeloperoxidase inhibition in mice alters atherosclerotic lesion composition.
2019

Sample Use Guides

5 and 15 mg/kg twice a day
Route of Administration: Oral
Name Type Language
PF-06282999
Common Name English
1(2H)-PYRIMIDINEACETAMIDE, 6-(5-CHLORO-2-METHOXYPHENYL)-3,4-DIHYDRO-4-OXO-2-THIOXO-
Systematic Name English
2-(6-(5-CHLORO-2-METHOXYPHENYL)-4-OXO-2-THIOXO-3,4-DIHYDROPYRIMIDIN-1(2H)-YL)ACETAMIDE
Systematic Name English
Code System Code Type Description
PUBCHEM
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
PRIMARY
SMS_ID
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
PRIMARY
CAS
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
PRIMARY
FDA UNII
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
PRIMARY
DRUG BANK
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
PRIMARY