Chemical Name: 4-[5-[3,5-Bis(1,1-dimethylethyl)phenyl]-1-[4-[(4-methyl-1-piperazinyl)carbonyl]phenyl]-1H-pyrazol-3-yl]benzoic acid
Biological ActivityHigh affinity and selective RARγ antagonist (Ki values are 1.1 nM, >1.7 μM and >2.9 μM for RARγ, RARα and RARβ respectively). Displays analgesic efficacy in a mouse model of osteoarthritis-like joint pain.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Identification of potent and selective retinoic acid receptor gamma (RARγ) antagonists for the treatment of osteoarthritis pain using structure based drug design.
Hughes et al.
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