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Chemical Structure : RGM8-51
Catalog No.: PC-72354Not For Human Use, Lab Use Only.
RGM8-51 is a β-lactam derivative, potent, selective TRPM8 antagonist with IC50 of 1.06 and 1.74 uM for rat and human TRPM8, respectively.
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RGM8-51 is a β-lactam derivative, potent, selective TRPM8 antagonist with IC50 of 1.06 and 1.74 uM for rat and human TRPM8, respectively.
RGM8-51 does not have any ability to activate TRPM8 channels, but produces a concentration-dependent inhibition of menthol activation.
RGM8-51 is selective for cold-activated TRPM8 channels, displays no agonist or antagonist profile in cool-activated TRPA1 channels and has negligible activity as TRPV3 and ASIC3 channel antagonists.
RGM8-51 (1 µM) inhibited menthol-activated currents in rTRPM8-expressing HEK293 cells.
RGM8-51 exhibits in vivo antinociceptive activity in response to cold, in a mouse model of oxaliplatin-induced peripheral neuropathy.
RGM8-51 reduces cold, mechanical and heat hypersensitivity in a rat model of neuropathic pain arising after chronic constriction of the sciatic nerve.
RGM8-51 exhibits mechanical hypersensitivity-relieving activity, in a mouse model of NTG-induced hyperesthesia.
| M.Wt | 588.792 | |
| Formula | C39H44N2O3 | |
| Appearance | Solid | |
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1. Martín-Escura C, et al. Int J Mol Sci. 2022 Feb 28;23(5):2692.
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