1. GPCR/G Protein
    Neuronal Signaling
  2. mGluR
  3. Mavoglurant

Mavoglurant (Synonyms: AFQ056)

Cat. No.: HY-15257 Purity: 99.99%
Handling Instructions

Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinson's disease.

For research use only. We do not sell to patients.

Mavoglurant Chemical Structure

Mavoglurant Chemical Structure

CAS No. : 543906-09-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 462 In-stock
Estimated Time of Arrival: December 31
5 mg USD 420 In-stock
Estimated Time of Arrival: December 31
10 mg USD 540 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

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Description

Mavoglurant (AFQ056) is a potent, selective, non-competitive and orally active mGluR5 antagonist, with an IC50 of 30 nM. Mavoglurant shows a >300 fold selectivity for the mGluR5 over all targets (238) tested. Mavoglurant can be used for the research of Fragile X syndrome (FXS), and L-dopa induced dyskinesias in Parkinson's disease[1][1][2].

IC50 & Target[1]

mGluR5

30 nM (IC50)

In Vitro

Mavoglurant (1 nM-10 μM; 10 min) fully antagonizes hmGluR5-mediated responses with IC50s of 110 and 30 nM in Ca2+- and PI-turnover assays in L(tk-) cells stably expressing mGluR5a[1].
Mavoglurant (0.01 nM-10 μM) displaces the binding of the allosteric binding ligand [3H]-AAE327 in a concentration-dependent manner in rat brain membranes, with an IC50 of 47 nM[1].

In Vivo

Mavoglurant (0.1-10 mg/kg; a single p.o.) inhibits the stress-induced hyperthermia (SIH) in a dose-dependent manner in mice[1].
Mavoglurant (9.4 mg/kg; a single p.o.) exhibits moderate oral bioavailability (32%), terminal half-life (2.9 h) and Cmax (plasma; brain) (950 pmol/mL; 3500 pmol/g)[1].
Mavoglurant (3.1 mg/kg; a single i.v.) exhibits terminal half-life (0.69 h), Cmax (plasma; brain) (3330 pmol/mL; 8400 pmol/g) and Tmax (≤0.08 h)[1].

Animal Model: Male OF1/IC mice[1]
Dosage: 0.1, 1, 10 mg/kg
Administration: A single p.o. administration
Result: Attenuated the stress-induced hyperthermia.
Was comparable to the positive control Chlordiazepoxide.
Animal Model: Male Sprague-Dawley rats (175-250 g)[1]
Dosage: 3.1 mg/kg for i.v.; 9.4 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: A single i.v. or p.o. administration
Result: P.o.: F=32%; T1/2=2.9 h; Tmax≤0.25 h.
I.v.: T1/2=0.69 h; Cmax (plasma/brain)=3330 pmol•mL-1/8400 pmol•g-1; Tmax≤0.08 h.
Clinical Trial
Molecular Weight

313.39

Formula

C₁₉H₂₃NO₃

CAS No.

543906-09-8

SMILES

CC1=CC(C#C[[email protected]]2(O)CCC[[email protected]]3([H])[[email protected]@]2([H])CCN3C(OC)=O)=CC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 120 mg/mL (382.91 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1909 mL 15.9546 mL 31.9091 mL
5 mM 0.6382 mL 3.1909 mL 6.3818 mL
10 mM 0.3191 mL 1.5955 mL 3.1909 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3 mg/mL (9.57 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 3 mg/mL (9.57 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3 mg/mL (9.57 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.99%

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Keywords:

MavoglurantAFQ056AFQ 056AFQ-056mGluRMetabotropic glutamate receptorsmGluR5FragileXsyndromeFXSL-dopadyskinesiasParkinson'sInhibitorinhibitorinhibit

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