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mGluR2 antagonist 1 is a potent and selective class of negative allosteric modulator targeting the metabotropic glutamate receptor 2 (mGluR2) with high oral bioavailability. It displays a remarkable affinity for mGluR2, with an IC50 value of 9 nM. Furthermore, it exhibits excellent permeability across the blood-brain barrier, making it a promising candidate for central nervous system-related studies or therapies.
Description | mGluR2 antagonist 1 is a potent and selective class of negative allosteric modulator targeting the metabotropic glutamate receptor 2 (mGluR2) with high oral bioavailability. It displays a remarkable affinity for mGluR2, with an IC50 value of 9 nM. Furthermore, it exhibits excellent permeability across the blood-brain barrier, making it a promising candidate for central nervous system-related studies or therapies. |
Targets&IC50 | mGluR2:9 nM (IC50) |
In vivo | In vivo, mGluR2 antagonist 1 (Compound 25) effectively counteracts the effects of mGluR2 agonist LY379268 on amphetamine-induced hyperlocomotion and exhibits significant efficacy in the mouse delayed non-match to position assay at a dosage of 10 mg/kg. |
Molecular Weight | 377.375 |
Formula | C21H16FN3O3 |
Cas No. | 1432728-49-8 |
Relative Density. | 1.415 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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