货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S85700-5mg	≥99%	￥810.00 S85700-5mg ￥810.00 3-5天	0 货期：3-5天	-	-	-	-
S85700-10mg	≥99%	￥1220.00 S85700-10mg ￥1220.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S85700-5mg

≥99%

￥810.00

货期：3-5天

S85700-10mg

≥99%

￥1220.00

货期：3-5天

产品描述：

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

靶点：

mGluR5:30 nM (IC50)

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

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.

参考文献：

1. Vranesic I, et al. AFQ056/mavoglurant, a novel clinically effective mGluR5 antagonist: identification, SAR and pharmacological characterization. Bioorg Med Chem. 2014 Nov 1;22(21):5790-5803. 2. Jacquemont AS, et, al. Epigenetic modification of the FMR1 gene in fragile X syndrome is associated with differential response to the mGluR5 antagonist AFQ056. Sci Transl Med. 2011 Jan 5;3(64):64ra1. 3. Petrov D, et, al. Mavoglurant as a treatment for Parkinson's disease. Expert Opin Investig Drugs. 2014 Aug;23(8):1165-79

溶解性：

Soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	3.191 ml	15.955 ml	31.909 ml
5 mM	0.638 ml	3.191 ml	6.382 ml
10 mM	0.319 ml	1.595 ml	3.191 ml
50 mM	0.064 ml	0.319 ml	0.638 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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