产品说明
一般描述
A blood-brain barrier permeable and bioavailable chromenone compound that acts as a potent, selective, and reversible antagonist of mGlu7 receptor (IC50 = 3.5 and 2.8 µM for mGlu7a and mGlu7b in CHO cells). Docks within the Venus flytrap domain (VFTD) close to the binding site of L-glutamate and functions as an orthosteric-like antagonist. Reduces DL-2-amino-4-phosphonobutyric acid (DL-AP4)-induced activation of human mGlu7b receptor (IC50 = 2.8 µM), but does not affect DL-AP4-induced activation of [35S]GTPγS binding by mGlu4 and mGlu6. Shown to diminish [35S]GTPγS binding by the human mGlu7/6 chimeric receptor harboring mGlu7 VFTD (IC50 = 2.5 µM). Displays weak binding affinity towards mGlu5 and mGlu8 receptors (IC50 >20 and 33 µM, respectively) and has no effect on GABA-induced activation of [35S]GTPγS binding by GABA-B receptors. Displays antidepressant and anxiolytic-like properties and selectively blocks long-term potentiation (LTP) in the lateral amygdala of wild type (IC50 = 88 nM), but not of mGlu7- deficient mice.
Please note that the molecular weight for this compound is batch-specific due to variable water content.
A blood-brain barrier permeable and bioavailable chromenone compound that acts as a potent, selective, and reversible antagonist of mGlu7 receptor (IC50 = 3.5 and 2.8 µM for mGlu7a and mGlu7b in CHO cells). Docks within the Venus flytrap domain (VFTD) close to the binding site of L-glutamate and functions as an orthosteric-like antagonist. Reduces DL-2-amino-4-phosphonobutyric acid (DL-AP4)-induced activation of human mGlu7b receptor (IC50 = 2.8 µM), but does not affect DL-AP4-induced activation of [35S]GTPγS binding by mGlu4 and mGlu6. Shown to diminish [35S]GTPγS binding by the human mGlu7/6 chimeric receptor harboring mGlu7 VFTD (IC50 = 2.5 µM). Displays weak binding affinity towards mGlu5 and mGlu8 receptors (IC50 >20 and 33 µM, respectively) and has no effect on GABA-induced activation of [35S]GTPγS binding by GABA-B receptors. Displays antidepressant and anxiolytic-like properties and selectively blocks long-term potentiation (LTP) in the lateral amygdala of wild type (IC50 = 88 nM), but not of mGlu7- deficient mice.
生化/生理作用
Cell permeable: yes
Primary Target
mGlu7R
Target IC50: 3.5 and 2.8 µ
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 6 months at -20°C.
其他说明
Gee, C.E., et al. 2014. J. Biol. Chem.289, 10975.
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 | C15H9IO4 |
分子量 | 380.13 |
MDL编号 | MFCD00525548 |
产品性质
质量水平 | 100 |
测定 | ≥97% (HPLC) |
形式 | powder |
manufacturer/tradename | Calbiochem® |
储存条件 | OK to freeze protect from light |
颜色 | pale yellow |
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