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Basimglurant

Catalog No. T12717 CAS 802906-73-6

Synonyms: CTEP Derivative, RG7090

Basimglurant (CTEP Derivative) is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM).

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Basimglurant, CAS 802906-73-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 127.00
5 mg	In stock	$ 297.00
10 mg	In stock	$ 443.00
25 mg	In stock	$ 732.00
50 mg	In stock	$ 987.00
100 mg	In stock	$ 1,390.00
500 mg	In stock	$ 2,790.00
1 mL * 10 mM (in DMSO)	In stock	$ 342.00

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Purity: 99.38%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Basimglurant (CTEP Derivative) is a potent, selective and orally available modulator of mGlu5 negative allosteric(Kd of 1.1 nM).
Targets&IC50	mGlu5 receptor:1.1 nM (Kd)
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].

Synonyms	CTEP Derivative, RG7090
Molecular Weight	325.77
Formula	C18H13ClFN3
CAS No.	802906-73-6

Storage

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

Solubility Information

DMSO: 33.33 mg/mL (102.31 mM)

References and Literature

1. Lindemann L, et al. Pharmacology of basimglurant (RO4917523, RG7090), a unique metabotropic glutamate receptor 5 negative allosteric modulator in clinical development for depression. J Pharmacol Exp Ther. 2015 Apr;353(1):213-33. 2. Jaeschke G, et al. Metabotropic glutamate receptor 5 negative allosteric modulators: discovery of 2-chloro-4-[1-(4-fluorophenyl)-2,5-dimethyl-1H-imidazol-4-ylethynyl]pyridine (basimglurant, RO4917523), a promising novel medicine for psychiatric diseases.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Neurodegenerative Disease Compound Library Drug Repurposing Compound Library Bioactive Compound Library Covalent Inhibitor Library Bioactive Compounds Library Max NO PAINS Compound Library Antidepressant Compound Library Neuronal Signaling Compound Library Neurotransmitter Receptor Compound Library ReFRAME Related Library

Related Products

Related compounds with same targets

VU0155041 Dasolampanel CX717 Evans blue CTEP 3-MATIDA TAT-GluA2 3Y acetate(1404188-93-7 free base) VU0155094

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Basimglurant 802906-73-6 Neuroscience GluR Inhibitor RG-7090 Metabotropic glutamate receptors mGluR inhibit CTEP Derivative RG7090 RG 7090 inhibitor

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