| 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： |
-80℃（运输条件：冰袋低温运输） |
| 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京