A-1165442 - CAS 1221443-94-2
Category: Inhibitor
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Molecular Formula:
Molecular Weight:
TRP Channel
A-1165442 is a potent, competitive and orally available modality-differentiated second-generation TRPV1 antagonist with good analgesic efficacy and a temperature-neutral profile (IC50= 9 nM for human TRPV1).
Brife Description:
A potent, competitive and orally available TRPV1 antagonist (IC50= 9 nM for human TRPV1)
1-[(4R)-7-chloro-2,2-bis(fluoromethyl)-3,4-dihydrochromen-4-yl]-3-(3-methylisoquinolin-5-yl)urea; 1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea
DMSO:10 mM
Store in a cool and dry place (or refer to the Certificate of Analysis).
Boiling Point:
574.4±50.0 ℃ at 760 Torr
1.38±0.1 g/cm3
Canonical SMILES:
1.Discovery of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442): a temperature-neutral transient receptor potential vanilloid-1 (TRPV1) antagonist with analgesic efficacy.
Voight EA;Gomtsyan AR;Daanen JF;Perner RJ;Schmidt RG;Bayburt EK;DiDomenico S;McDonald HA;Puttfarcken PS;Chen J;Neelands TR;Bianchi BR;Han P;Reilly RM;Franklin PH;Segreti JA;Nelson RA;Su Z;King AJ;Polakowski JS;Baker SJ;Gauvin DM;Lewis LR;Mikusa JP;Joshi SK;Faltynek CR;Kym PR;Kort ME J Med Chem. 2014 Sep 11;57(17):7412-24. doi: 10.1021/jm500916t. Epub 2014 Aug 21.
The synthesis and characterization of a series of selective, orally bioavailable 1-(chroman-4-yl)urea TRPV1 antagonists is described. Whereas first-generation antagonists that inhibit all modes of TRPV1 activation can elicit hyperthermia, the compounds disclosed herein do not elevate core body temperature in preclinical models and only partially block acid activation of TRPV1. Advancing the SAR of this series led to the eventual identification of (R)-1-(7-chloro-2,2-bis(fluoromethyl)chroman-4-yl)-3-(3-methylisoquinolin-5-yl)urea (A-1165442, 52), an analogue that possesses excellent pharmacological selectivity, has a favorable pharmacokinetic profile, and demonstrates good efficacy against osteoarthritis pain in rodents.
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Chemical Structure

CAS 1221443-94-2 A-1165442

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