Mavoglurant, aslo known as AFQ056, is an experimental drug candidate for the treatment of fragile X syndrome. Mavoglurant exerts its effect as an antagonist of the metabotropic glutamate receptor 5 (mGLU5). Novartis discontinued development of mavoglurant for fragile X syndrome in April 2014 following disappointing trial results. Currently Novartis is conducting a clinical trial with this drug on obsessive compulsive disorder.
Chemical Formula: C19H23NO3
Exact Mass: 313.1678
Molecular Weight: 313.397
Elemental Analysis: C, 72.82; H, 7.40; N, 4.47; O, 15.32
InChi Code: InChI=1S/C19H23NO3/c1-14-5-3-6-15(13-14)8-11-19(22)10-4-7-17-16(19)9-12-20(17)18(21)23-2/h3,5-6,13,16-17,22H,4,7,9-10,12H2,1-2H3/t16-,17-,19-/m1/s1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
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.
Mavoglurant (0.1-10 mg/kg; a single p.o.) inhibits the stress-induced hyperthermia (SIH) in a dose-dependent manner in mice.
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).
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).
Berry-Kravis E, Des Portes V, Hagerman R, Jacquemont S, Charles P, Visootsak J, Brinkman M, Rerat K, Koumaras B, Zhu L, Barth GM, Jaecklin T, Apostol G, von Raison F. Mavoglurant in fragile X syndrome: Results of two randomized, double-blind, placebo-controlled trials. Sci Transl Med. 2016 Jan 13;8(321):321ra5. doi: 10.1126/scitranslmed.aab4109. PubMed PMID: 26764156.
Wendling T, Dumitras S, Ogungbenro K, Aarons L. Application of a Bayesian approach to physiological modelling of mavoglurant population pharmacokinetics. J Pharmacokinet Pharmacodyn. 2015 Dec;42(6):639-57. doi: 10.1007/s10928-015-9430-4. Epub 2015 Aug 1. PubMed PMID: 26231433.
Sivasubramanian R, Chakraborty A, Rouzade-Dominguez ML, Neelakantham S, Jakab A, Mensinga T, Legangneux E, Woessner R, Ufer M. Effect of mavoglurant (AFQ056), a selective mGluR5 antagonist, on the pharmacokinetics of a combined oral contraceptive containing ethinyl estradiol and levonorgestrel in healthy women. Int J Clin Pharmacol Ther. 2015 Jul;53(7):550-6. doi: 10.5414/CP202321. PubMed PMID: 25943176.
Wendling T, Ogungbenro K, Pigeolet E, Dumitras S, Woessner R, Aarons L. Model-based evaluation of the impact of formulation and food intake on the complex oral absorption of mavoglurant in healthy subjects. Pharm Res. 2015 May;32(5):1764-78. doi: 10.1007/s11095-014-1574-1. Epub 2014 Nov 26. PubMed PMID: 25425054.
Vranesic I, Ofner S, Flor PJ, Bilbe G, Bouhelal R, Enz A, Desrayaud S, McAllister K, Kuhn R, Gasparini F. AFQ056/mavoglurant, a novel clinically effective mGluR5 antagonist: identification, SAR and pharmacological characterization. Bioorg Med Chem. 2014 Nov 1;22(21):5790-803. doi: 10.1016/j.bmc.2014.09.033. Epub 2014 Sep 20. PubMed PMID: 25316499.
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