产品
编 号：F385294
分子式：C19H23NO3
分子量：313.39
分子式：C19H23NO3
分子量：313.39
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
询价
询价
5mg
询价
询价
10mg
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询价
结构图
CAS No: 543906-09-8
产品详情
生物活性：
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. Mavoglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
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).Animal Model:Male OF1/IC mice
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)
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.
体外研究：
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 (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. Mavoglurant is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
体内研究：
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).Animal Model:Male OF1/IC mice
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)
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.
体外研究：
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.
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