1. GPCR/G Protein
  2. mGluR

RG7090 (Synonyms: Basimglurant; CTEP Derivative)

Cat. No.: HY-15446 Purity: 98.15%
Data Sheet SDS Handling Instructions

RG7090 (Basimglurant, RO4917523) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.

For research use only. We do not sell to patients.
RG7090 Chemical Structure

RG7090 Chemical Structure

CAS No. : 802906-73-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO $385 In-stock
5 mg $350 In-stock
10 mg $500 In-stock
50 mg $1500 In-stock
100 mg $2100 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

RG7090 (Basimglurant, RO4917523) is a potent, selective and orally available mGlu5 negative allosteric modulator with a Kd of 1.1 nM.

IC50 & Target

Kd: 1.1 nM (mGlu5)[1]

In Vitro

[3H]-basimglurant saturation analysis on recombinant human mGlu5 reveals monophasic saturation isotherms with Kd of 1.1 nM. In competition binding experiments on human recombinant mGlu5, basimglurant 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 inhibits quisqualate induced Ca2+ mobilization with an IC50 of 7.0 nM and [3H]-inositolphosphate accumulation with an 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 a potent, selective, and safe mGlu5 inhibitor with good oral bioavailability and long half-life supportive of once-daily administration, good brain penetration, and high in vivo potency. It has antidepressant properties which are corroborated by its functional magnetic imaging (fMRI) profile, as well as anxiolytic-like and antinociceptive features[1]. It is currently in phase II clinical studies for the treatment of depression and fragile X syndrome. In the Vogel conflict drinking test, Basimglurant dose dependently increases the drinking time. The total plasma exposure of efficacious doses of Basimglurant ranges from 5 ng/mL (0.03 mg/kg) to 37 ng/mL (0.3 mg/kg)[2].

Clinical Trial
NCT Number Sponsor Condition Start Date Phase
NCT02433093 Hoffmann-La Roche Major Depressive Disorder, Healthy Volunteer April 2015 Phase 1
NCT02433093 Hoffmann-La Roche Major Depressive Disorder, Healthy Volunteer April 2015 Phase 1
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References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 3.0697 mL 15.3483 mL 30.6965 mL
5 mM 0.6139 mL 3.0697 mL 6.1393 mL
10 mM 0.3070 mL 1.5348 mL 3.0697 mL
Animal Administration
[1]

Rat: For intravenous PK, basimglurant is formulated in N-methyl-pyrollidone (NMP)/saline (30%/70%) as vehicle and administered at a volume of 2 mL/kg. For oral gavage (p.o.) the compound is administered as suspension using gelatine/saline (7.5%/0.62% in water) at an administration volume of 4 mL/kg[1].

Monkey: For intravenous PK, basimglurant is formulated in cyclodextrin solution as vehicle and administered at a volume of 2 mL/kg. For oral gavage (p.o.), the compound is administered in capsule (2 mg in size-2 capsules, i.e. ~0.3 mg/kg) to fasted or fed monkeys in a cross-over design[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

325.77

Formula

C₁₈H₁₃ClFN₃

CAS No.

802906-73-6

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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RG7090
Cat. No.:
HY-15446
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