Basimglurant

SKU: orb1309164

Description

Basimglurant is a potent, selective, and orally bioavailable negative allosteric modulator of the mGlu5 receptor, exhibiting a Kd of 1.1 nM. It has been utilized in preclinical research for investigating neurological disorders, including depression and anxiety, in both in vitro and in vivo models.

Research Area

Neuroscience

Key Properties

• CAS Number: 802906-73-6
• MW: 325.77
• Purity: 98.35% (May vary between batches)
• Formula: C₁₈H₁₃ClFN₃
• SMILES: Cc1nc(C#Cc2ccnc(Cl)c2)c(C)n1-c1ccc(F)cc1
• Target: GluR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.14 mM);DMSO:60 mg/mL (184.18 mM)

Bioactivity

• Target IC50:
  mGluR5:1.1 nM (Kd)
• 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.
• 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.

Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, Metabotropic glutamate receptors, mGlu5, mGluR5, mGluR, CTEP Derivative, Basimglurant, RG 7090, RG7090, RG-7090

Compound Identifiers

PubChem CID

11438771