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Mavoglurant (AFQ056) is a potent, selective, non-competitive, and orally active metabotropic glutamate receptor 5 (mGluR5) antagonist with an IC50 of 30 nM, demonstrating greater than 300-fold selectivity over 238 tested targets, and it is widely applied in research on Fragile X syndrome and L-dopa-induced dyskinesias in Parkinson’s disease, while Mavoglurant incorporated alkyne functional group, which enables copper-catalyzed azide–alkyne cycloaddition click chemistry, facilitating target engagement and molecular tracking studies.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $347 | - | In Stock | |
| 50 mg | $1,490 | - | In Stock | |
| 100 mg | $1,990 | - | In Stock | |
| 1 mL x 10 mM (in DMSO) | $382 | - | In Stock |
| Description | Mavoglurant (AFQ056) is a potent, selective, non-competitive, and orally active metabotropic glutamate receptor 5 (mGluR5) antagonist with an IC50 of 30 nM, demonstrating greater than 300-fold selectivity over 238 tested targets, and it is widely applied in research on Fragile X syndrome and L-dopa-induced dyskinesias in Parkinson’s disease, while Mavoglurant incorporated alkyne functional group, which enables copper-catalyzed azide–alkyne cycloaddition click chemistry, facilitating target engagement and molecular tracking studies. |
| Targets&IC50 | mGluR5 (rat):47 nM |
| In vitro | In functional assays using L(tk-) cells expressing human mGluR5a, Mavoglurant antagonized agonist-induced signaling, inhibiting phosphoinositide turnover (IC50 = 30 nM) and intracellular Ca2+ mobilization (IC50 = 110 nM). Radioligand binding assays confirmed its interaction with the transmembrane allosteric site by displacing 3H-AAE327 with an IC50 of 47 nM [1]. |
| In vivo | In a mouse model of Stress-Induced Hyperthermia (SIH), oral administration of Mavoglurant (0.1 - 10 mg/kg) attenuated the stress response in a dose-dependent manner. Pharmacokinetic analysis in rats shows that the compound penetrates the blood-brain barrier; following intravenous injection (3.1 mg/kg), the Cmax in the brain (8400 pmol/g) was higher than in plasma (3330 pmol/mL). Oral administration (9.4 mg/kg) in rats demonstrated a bioavailability of 32% with a terminal half-life (T1/2) of 2.9 hours [1]. |
| Synonyms | AFQ-056, AFQ056, AFQ 056 |
| Molecular Weight | 313.39 |
| Formula | C19H23NO3 |
| Cas No. | 543906-09-8 |
| Smiles | C(#CC1=CC(C)=CC=C1)[C@@]2(O)[C@]3([C@](N(C(OC)=O)CC3)(CCC2)[H])[H] |
| Relative Density. | 1.21 |
| Storage | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 100 mg/mL (319.09 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (10.53 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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