259674-19-6

中文名称:

259674-19-6

中文同义词:

英文名称:

TRPM8 Antagonist

英文同义词:

TRPM8 Antagonist;TRPM8 ANTAGONIST;259674-19-6;TRPM8 antagonist 2;L-Tryptophan, N,N-bis(phenylmethyl)-, methyl ester;Methyl N,N-dibenzyl-L-tryptophanate

CAS号:

259674-19-6

分子式:

C26H26N2O2

分子量:

398.5

EINECS号:

相关类别:

API

Mol文件:

259674-19-6.mol

沸点 

567.5±50.0 °C(Predicted)

密度 

1.195±0.06 g/cm3(Predicted)

储存条件 

Inert atmosphere,2-8°C

酸度系数(pKa)

17.02±0.30(Predicted)

生物活性

TRPM8 antagonist 2 (TRPM8 Antagonist)是一种有效的 TRPM8 的拮抗剂，IC50值为0.2 nM，可用于神经性疼痛综合征的药理治疗。

靶点

Target Value TRPM8 (Cell-free assay) 0.2 nM

Target

Value

TRPM8 (Cell-free assay)

0.2 nM

体外研究

TRPM8 antagonist 2 (Compound 14) is a potent and selective TRPM8 antagonist, with an IC 50 of 0.2 nM, used in the research of neuropathic pain syndromes. TRPM8 antagonist 2 potently inhibits menthol-induced increase in intracellular Ca 2+ levels in Ca 2+ fluorimetric assays in HEK293 cells stably expressing the rat isoform of TRPM8 channels (IC 50 , 40 nM).

体内研究

TRPM8 antagonist 2 (1, 10, and 30 mg/kg, s.c.) shows a marked, dose-dependent antinociceptive activity, and inhibits wet-dog shakes (WDS)-like cold hypersensitivity in mice by 63% at 30 mg/kg. In addition, TRPM8 antagonist 2 (0.1 and 1 μg, s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice.