| Name | Basimglurant |
| Description | Basimglurant (CTEP Derivative) is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM). |
| In vitro | In competition binding experiments on human recombinant mGlu5, Basimglurant (RG7090) fully displaces [3H]-MPEP with a Ki of 35.6 nM and [3H]-ABP688 with a Ki of 1.4 nM. In HEK293 cells stably expressing human mGlu5, Basimglurant (RG7090) inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and [3H]-inositolphosphate accumulation (IC50 of 5.9 nM). Basimglurant shows similar potencies in radioligand binding and functional assay on human and rodent mGlu5 receptor orthologues[1]. |
| In vivo | Basimglurant is selective and safe inhibitor of mGlu5 with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. Basimglurant has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features[1]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 60 mg/mL (184.18 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (6.14 mM), Sonication is recommended.
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| Keywords | RG-7090 | RG 7090 | mGluR5 | mGluR | mGlu5 | Metabotropic glutamate receptors | Inhibitor | inhibit | Basimglurant |
| Inhibitors Related | S-Sulfo-L-cysteine sodium salt | IDRA-21 | Urethane | Decanoic Acid | DCB | L-Cysteic acid monohydrate | Evans blue | L-Glutamine | Direct Blue 1 | L-Glutamic acid monosodium salt | Memantine hydrochloride | O-Phospho-L-serine |
| Related Compound Libraries | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Antidepressant Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Glutamine Metabolism Compound Library | Drug Repurposing Compound Library | Neuroprotective Compound Library | Bioactive Compounds Library Max | Covalent Inhibitor Library | Fluorochemical Library | Human Metabolite Library |
United States
