PF-05241328

Investigational

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

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	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

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

Approval Year

PubMed

PubMed

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Title	Date	PubMed
Clinical Micro-Dose Studies to Explore the Human Pharmacokinetics of Four Selective Inhibitors of Human Nav1.7 Voltage-Dependent Sodium Channels.	2016 Jul	26895021

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Sample Use Guides

In Vivo Use Guide

Single dose - 100 ug

Route of Administration: Other

Substance Class	Chemical
Record UNII	8RAL5N48VT
Record Status	`Validated (UNII)`
Record Version

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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

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Code System

Code

Type

Description

FDA UNII

8RAL5N48VT

PRIMARY

PUBCHEM

68109743

PRIMARY

DRUG BANK

DB15124

PRIMARY

CAS

1387633-03-5

PRIMARY

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Related Record

Type

Details


					8RAL5N48VT

PF-05241328

ACTIVE MOIETY

Comments:

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.


					8RAL5N48VT

PF-05241328

ACTIVE MOIETY

Comments:

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.


					8RAL5N48VT

PF-05241328

ACTIVE MOIETY

Comments:

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.

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