Mavoglurant (AFQ056) | mGlu5 NAM | Probechem Biochemicals

Chemical Structure : Mavoglurant

CAS No.: 543906-09-8

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Mavoglurant (AFQ056, AFQ-056)

货号: 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.

规格	价格	库存
5 mg	￥780	In stock
10 mg	￥1180	In stock
25 mg	￥1980	In stock
50 mg	￥3280	In stock
100 mg		Get quote

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生物&药学活性

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).

物理化学性质&存储条件

分子量	313.40
分子式	C19H23NO3
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	methyl (3aR,4S,7aR)-4-hydroxy-4-(m-tolylethynyl)octahydro-1H-indole-1-carboxylate

参考文献

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.

Mavoglurant (AFQ056, AFQ-056)

生物&药学活性

物理化学性质&存储条件

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Mavoglurant (AFQ056, AFQ-056)

生物&药学活性

物理化学性质&存储条件

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