TRPM8 拮抗剂
| 中文名称 | TRPM8 拮抗剂 |
|---|---|
| 中文同义词 | 化合物TRPM8 ANTAGONIST 2;(S)-2-(二苄氨基)-3-(1H-吲哚-3-基)丙酸甲酯;TRPM8 ANTAGONIST 2 游离 |
| 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;Methyl Na,Na-dibenzyl-L-tryptophanate;TRPM8 antagonist 2,inhibit,Transient receptor potential channels,TRP Channel,Inhibitor,TRPM-8 antagonist 2 |
| 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 |
| 结构式 |  |
TRPM8 拮抗剂 性质
| 沸点 | 567.5±50.0 °C(Predicted) |
|---|---|
| 密度 | 1.195±0.06 g/cm3(Predicted) |
| 储存条件 | under inert gas (nitrogen or Argon) at 2-8°C |
| 溶解度 | 二甲基亚砜：160 mg/mL（401.51 mM） |
| 酸度系数(pKa) | 17.02±0.30(Predicted) |
| 形态 | 固体 |
| 颜色 | 浅黄至黄色 |
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。
| Target | Value |
|
TRPM8
(Cell-free assay) | 0.2 nM |
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).
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.
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-112430 | 259674-19-6 TRPM8 antagonist 2 | 259674-19-6 | 5mg | 900元 |
| 2024/04/30 | HY-112430 | 259674-19-6 TRPM8 antagonist 2 | 259674-19-6 | 10mM * 1mLin DMSO | 990元 |