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)
| 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
Approval Year
| Substance Class |
Chemical
Created
by
admin
on
Edited
Sat Dec 16 12:06:09 GMT 2023
by
admin
on
Sat Dec 16 12:06:09 GMT 2023
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| Record UNII |
8RAL5N48VT
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| Record Status |
Validated (UNII)
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| Record Version |
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68109743
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DB15124
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1387633-03-5
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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.
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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.
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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.
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