U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

Details

Stereochemistry ACHIRAL
Molecular Formula C17H16ClN5O2
Molecular Weight 357.794
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PF-04531083

SMILES

COC1=CC=C(Cl)C(=C1)C2=C(N)N=C(NC(=O)C3=CC=NN3C)C=C2

InChI

InChIKey=ZRJGMDIPCQOGNI-UHFFFAOYSA-N
InChI=1S/C17H16ClN5O2/c1-23-14(7-8-20-23)17(24)22-15-6-4-11(16(19)21-15)12-9-10(25-2)3-5-13(12)18/h3-9H,1-2H3,(H3,19,21,22,24)

HIDE SMILES / InChI

Molecular Formula C17H16ClN5O2
Molecular Weight 357.794
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

PF-04531083 is selective Nav1.8 blocker. It has been investigated for the treatment of chronic pain, heart pain, post-surgical dental pain. However, these trials were discontinued.

Approval Year

PubMed

PubMed

TitleDatePubMed
Recent progress in sodium channel modulators for pain.
2014 Aug 15

Sample Use Guides

Single dose - 1000 mg or 2000 mg
Route of Administration: Oral
Substance Class Chemical
Created
by admin
on Sat Dec 16 01:46:59 GMT 2023
Edited
by admin
on Sat Dec 16 01:46:59 GMT 2023
Record UNII
40497CY7Y3
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PF-04531083
Common Name English
PF-4531083
Code English
1H-PYRAZOLE-5-CARBOXAMIDE, N-(6-AMINO-5-(2-CHLORO-5-METHOXYPHENYL)-2-PYRIDINYL)-1-METHYL-
Systematic Name English
Code System Code Type Description
DRUG BANK
DB12468
Created by admin on Sat Dec 16 01:46:59 GMT 2023 , Edited by admin on Sat Dec 16 01:46:59 GMT 2023
PRIMARY
CAS
1079400-07-9
Created by admin on Sat Dec 16 01:46:59 GMT 2023 , Edited by admin on Sat Dec 16 01:46:59 GMT 2023
PRIMARY
CLINICAL_TRIALS.GOV
PF-04531083
Created by admin on Sat Dec 16 01:46:59 GMT 2023 , Edited by admin on Sat Dec 16 01:46:59 GMT 2023
PRIMARY 6 studies found for: PF-04531083
MANUFACTURER PRODUCT INFORMATION
PF-04531083
Created by admin on Sat Dec 16 01:46:59 GMT 2023 , Edited by admin on Sat Dec 16 01:46:59 GMT 2023
PRIMARY PF-04531083: Synonym: N-(6-Amino-5-(2-chloro-5-methoxyphenyl)-2-pyridinyl)-1-methyl-1H-pyrazole-5-carboxamide, N-(6-Amino-5-(2-chloro-5-methoxyphenyl)pyridin-2-yl)-1-methyl-1H-pyrazole-5-carboxamide, PF 4531083
SMS_ID
300000041337
Created by admin on Sat Dec 16 01:46:59 GMT 2023 , Edited by admin on Sat Dec 16 01:46:59 GMT 2023
PRIMARY
PUBCHEM
57582353
Created by admin on Sat Dec 16 01:46:59 GMT 2023 , Edited by admin on Sat Dec 16 01:46:59 GMT 2023
PRIMARY
FDA UNII
40497CY7Y3
Created by admin on Sat Dec 16 01:46:59 GMT 2023 , Edited by admin on Sat Dec 16 01:46:59 GMT 2023
PRIMARY
ChEMBL
CHEMBL3544951
Created by admin on Sat Dec 16 01:46:59 GMT 2023 , Edited by admin on Sat Dec 16 01:46:59 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY
Originator: Pfizer; Class: Analgesic; Orphan Drug Status: No; On Fast track: No; Highest Development Phases: Discontinued for Pain, Postoperative pain; Most Recent Events: 10 Jul 2012 Pfizer terminates phase II trial in Postoperative pain in USA (NCT01512160), 22 May 2012 Pfizer completes enrolment in its phase II trial for Postoperative pain in USA (NCT01512160), 10 May 2012 Discontinued - Phase-I for Pain in Belgium (PO)
ACTIVE MOIETY
Compound: PF-04531083; Company: Pfizer; Pharmacology: Nav1.8; Phase: I; Therapeutic indication: Neuropathic/Inflammatory pain (oral)