RGM8-51 | TRPM8 antagonist | Probechem Biochemicals

Chemical Structure : RGM8-51

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RGM8-51 (TRPM8 antagonist)

货号: 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.

规格	价格	库存	数量
25 mg		Get quote
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	588.792
分子式	C39H44N2O3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	tert-butyl (2S,3S)-2-benzyl-1-((S)-2-(dibenzylamino)-3-phenylpropyl)-3-methyl-4-oxoazetidine-2-carboxylate

参考文献

1. Martín-Escura C, et al. Int J Mol Sci. 2022 Feb 28;23(5):2692.