- 商品介绍
- 规格参数
- 包装参数
General description
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.
Biochem/physiol Actions
Cell permeable: yes
Primary Target
mGlu7R
Reversible: yes
Target IC50: 3.5 and 2.8 µ
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Other Notes
Gee, C.E., et al. 2014. J. Biol. Chem.289, 10975.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
| assay | ≥97% (HPLC) |
| Quality Segment | 100 |
| form | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze,protect from light |
| color | pale yellow |
| solubility | DMSO: 100 mg/mL |
| storage temp. | 2-8°C |
| SMILES string | Ic1ccc(cc1)Oc2[c](c3c([o]c2)cc(cc3)O)=O |
| InChI | 1S/C15H9IO4/c16-9-1-4-11(5-2-9)20-14-8-19-13-7-10(17)3-6-12(13)15(14)18/h1-8,17H |
| InChI key | XXZKJJYWINSUMJ-UHFFFAOYSA-N |
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¥ 2528.88
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¥ 1573.49
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¥ 2068.25
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¥ 4390.38
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¥ 3319.60
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