半岛bd体育手机客户端 说明
一般描述
A brain-permeable (thiazole-pyridine)alkyne compound that acts as a potent, selective and non-competitive mGluR5 (metabotropic glutamate receptor subtype-5) antagonist (IC50= 5 nM in Ca2+-flux assay; Ki= 16 nM) within vivoanxiolytic activity in a rodent model (ED50= 1 mg/kg, ip and 7 mg/kg, po). Devoid of any side effects seen with MPEP and benzodiazepines. Reported to weakly affect the activities of other enzymes and receptors tested (IC50= 30 ?M for MAO-A, >100 ?M for mGlu1R, 2R & 7R, and >300 ?M for NR2BR).
包装
5 mg in Plastic ampoule
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Target Ki: 16 nM for mGluR5 (metabotropic glutamate receptor subtype-5)
Target IC50: 5 nM in Ca2+-flux assay
Product does not compete with ATP.
Reversible: no
Primary Target
mGluR5
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
其他说明
Bradbury, M.J., et al. 2005.J. Pharmacol. Exp. Ther.313,395.
Busse, C.S., et al. 2004.Neuropsychopharmacology29,1971.
Roppe, J.R., et al. 2004.Bioorg. Med. Chem. Lett.14,3993.
Klodzinska, A., et al. 2004.Neuropharmacology47,342.
Cosford, N.D.P., et al. 2003.J. Med. Chem.46,204.
Brodkin, J., et al. 2002.Eur. J. Neurosci.16,2241.
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 | C11H8N2S |
| 分子量 | 200.26 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | solid |
| manufacturer/tradename | Calbiochem? |
| 储存条件 | OK to freeze protect from light |
| 颜色 | white to yellow |
| 溶解性 | methanol: 1 mg/mL DMSO: 5 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 1 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
Sigma-Aldrich
m.cnreagent.com
