半岛bd体育手机客户端 说明
一般描述
A cell-permeable, readily bioavailable 2-picolinamide derivative that acts as a highly potent antagonist of transient receptor potential cation channel subfamily M member 8 (TRPM8; IC50= 10.9 nM in icilin evoked Ca2+ currents in HEK293 cells stably expressing human TRPM8). At much higher levels it is shown to activate human TRPA1 (EC50= 2.8 ?M) and inhibit human TRPV1 (IC50= 3.0 ?M). Selectively reduces behavioral and neural responses to cooling in spinal ligated rats (~ 30 mg/kg), but not in na?ve rats.
A cell-permeable, readily bioavailable 2-picolinamide derivative that acts as a highly potent antagonist of transient receptor potential cation channel subfamily M member 8 (TRPM8; IC50= 10.9 nM in icilin evoked Ca2+ currents in HEK293 cells stably expressing human TRPM8). At much higher levels it is shown to activate human TRPA1 (EC50= 2.8 ?M) and inhibit human TRPV1 (IC50= 3.0 ?M). Selectively reduces behavioral and neural responses to cooling in spinal ligated rats (~ 30 mg/kg), but not in na?ve rats.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
生化/生理作用
Primary Target
TRPM8
Reversible: yes
包装
Packaged under inert gas
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
其他说明
Patel, R., et al. 2014.J. Pharm. Exp. Ther.345,in press.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C18H16F4N2O4 |
| 分子量 | 400.32 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | solid |
| 效能 | 10.9 nM IC50 |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | white |
| 溶解性 | DMSO: 100 mg/mL |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
