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Details

Stereochemistry ACHIRAL
Molecular Formula C19H21ClN4O4S
Molecular Weight 436.912
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of PF-05241328

SMILES

CC(C)COC1=C(Cl)C=C(C=N1)N2N=C(C)C3=C2C=CC(=C3)C(=O)NS(C)(=O)=O

InChI

InChIKey=RVTSXVZXEGFIPW-UHFFFAOYSA-N
InChI=1S/C19H21ClN4O4S/c1-11(2)10-28-19-16(20)8-14(9-21-19)24-17-6-5-13(7-15(17)12(3)22-24)18(25)23-29(4,26)27/h5-9,11H,10H2,1-4H3,(H,23,25)

HIDE SMILES / InChI

Molecular Formula C19H21ClN4O4S
Molecular Weight 436.912
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

PF-05241328 is a novel, potent and selective inhibitor of human Nav1.7 voltage-dependent sodium channels (Nav1.7). It was developed for the pain treatment. It is highly plasma protein bound. PF-05241328 was ruled out based on half-life as the peak to trough ratios for this compound on twice-daily administration would require high therapeutic indices.

Originator

Sources: DOI: 10.1358/dof.2015.40.1.2273384

Approval Year

PubMed

PubMed

TitleDatePubMed
Clinical Micro-Dose Studies to Explore the Human Pharmacokinetics of Four Selective Inhibitors of Human Nav1.7 Voltage-Dependent Sodium Channels.
2016 Jul

Sample Use Guides

Single dose - 100 ug
Route of Administration: Other
Substance Class Chemical
Created
by admin
on Sat Dec 16 12:06:09 GMT 2023
Edited
by admin
on Sat Dec 16 12:06:09 GMT 2023
Record UNII
8RAL5N48VT
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
PF-05241328
Common Name English
1-(5-CHLORO-6-(2-METHYLPROPOXY)-3-PYRIDINYL)-3-METHYL-N-(METHYLSULFONYL)-1H-INDAZOLE-5-CARBOXAMIDE
Systematic Name English
1H-INDAZOLE-5-CARBOXAMIDE, 1-(5-CHLORO-6-(2-METHYLPROPOXY)-3-PYRIDINYL)-3-METHYL-N-(METHYLSULFONYL)-
Systematic Name English
Code System Code Type Description
FDA UNII
8RAL5N48VT
Created by admin on Sat Dec 16 12:06:09 GMT 2023 , Edited by admin on Sat Dec 16 12:06:09 GMT 2023
PRIMARY
PUBCHEM
68109743
Created by admin on Sat Dec 16 12:06:09 GMT 2023 , Edited by admin on Sat Dec 16 12:06:09 GMT 2023
PRIMARY
DRUG BANK
DB15124
Created by admin on Sat Dec 16 12:06:09 GMT 2023 , Edited by admin on Sat Dec 16 12:06:09 GMT 2023
PRIMARY
CAS
1387633-03-5
Created by admin on Sat Dec 16 12:06:09 GMT 2023 , Edited by admin on Sat Dec 16 12:06:09 GMT 2023
PRIMARY
Related Record Type Details
ACTIVE MOIETY
RESULTS: Plasma clearance, volume of distribution and bioavailability ranged from 45 to 392 mL/min/kg, 13 to 36 L/kg and 38 to 110 %, respectively. The PBPK model for PF-05089771 predicted a 1 g oral dose would be required to achieve exposures of approximately 12 Nav1.7 IC50 at maximum concentration (C max), and approximately 3 IC50 after 12 h (minimum concentration (C min) for a twice-daily regimen). Lower multiples of Nav1.7 IC50 were predicted with the same oral doses of PF-05150122, PF-05186462, and PF-05241328.
ACTIVE MOIETY
Official Title: An Exploratory, Open Label, Randomized, Parallel Group Study To Investigate The Pharmacokinetics Of Single Intravenous And Oral Micro Doses Of PF-05186462, PF-05089771, PF-05241328 And PF-05150122 In Healthy Male Subjects Purpose: The purpose of this study is to calculate the pharmacokinetics (concentration of compound in and rate of excretion from the blood) following a very low dose of compound which will not have any pharmacological activity and to monitor for the safety and tolerability of each of the compounds in the study.
ACTIVE MOIETY
Drugs: PF 5089771(Primary), PF 5089771(Primary), PF 5141328(Primary), PF 5141328(Primary), PF 5150122(Primary), PF 5150122(Primary), PF 5186462(Primary), PF 5186462(Primary); Indication: Pain; Focus: Adverse reactions, Pharmacokinetics; Sponsor: Pfizer; Most Recent Events: 19 Feb 2016 Results of two phase I studies published in the Clinical Pharmacokinetics., 23 Aug 2010 Status changed from recruiting to completed as reported by ClinicalTrials.gov., 10 Aug 2010 Actual initiation date added to 1 Jul 2010 as reported by ClinicalTrials.gov.