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Chemical Structure : Mavoglurant
Catalog No.: PC-49747Not For Human Use, Lab Use Only.
AFQ056 (Mavoglurant, AFQ-056) is a potent, subtype-selective and non-competitive inhibitor of mGluR5 with IC50 of 30 nM.
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AFQ056 (Mavoglurant, AFQ-056) is a potent, subtype-selective and non-competitive inhibitor of mGluR5 with IC50 of 30 nM.
AFQ056 displays >300 fold selectivity for the mGluR5 over other metabotropic family of GPCRs.
AFQ056 antagonizes hmGluR5-mediated responses with IC50s of 110 and 30 nM in Ca2+- and PI-turnover assays in L(tk-) cells stably expressing mGluR5. AFQ056 (Mavoglurant) (0.1-10 mg/kg; a single p.o.) inhibits the stress-induced hyperthermia (SIH) in a dose-dependent manner in mice.
Fmr1 KO mice have a deficit in inhibition of the startle response after a prepulse and that AFQ056 can rescue this phenotype, shows potential for treatment of fragile X syndrome (FXS).
| M.Wt | 313.40 | |
| Formula | C19H23NO3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Jacquemont S, et al. Sci Transl Med. 2011 Jan 5;3(64):64ra1.
2. Ivo Vranesic, et al. Bioorg Med Chem. 2014 Nov 1;22(21):5790-803
3. Levenga J, et al. Neurobiol Dis. 2011 Jun;42(3):311-7.
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