RGM8-51
Published date: 2022-06-22 21:57:40
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Name | RGM8-51 | CAS# | 2064172-83-2 |
|---|---|---|---|---|
| Price | $Inquiry/100mg $Inquiry/250mg $Inquiry/1g | Purity | 98.0% | |
| Stocking Period |
3 Day | Stock | 3 | |
| Product Webpage: | https://www.dcchemicals.com/product_show-rgm8-51.html | |||
| Detail
Product Information
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. |
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