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mGluR2 antagonist 1

Catalog No. T38910 CAS 1432728-49-8

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.

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mGluR2 antagonist 1, CAS 1432728-49-8

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Biological Description

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Storage & Solubility Information

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 action of mGluR2 agonist LY379268 on amphetamine-induced hyperlocomotion and demonstrates 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

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Youheng Shu,et al. Discovery of 4-arylquinoline-2-carboxamides, Highly Potent and Selective Class of mGluR2 Negative Allosteric Modulators: From HTS to Activity in Animal Models. Bioorg Med Chem Lett. 2020 May 1;30(9):127066.

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Keywords

mGluR2 antagonist 1 1432728-49-8 mGluR-2 antagonist 1 inhibitor inhibit

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