CAS NO: | 864864-17-5 |
包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
Cas No. | 864864-17-5 |
Canonical SMILES | O=C1N(C2CC2)CC3=C1C=CC(C4=C(C)N(C5=CC=CN=C5F)N=N4)=C3 |
分子式 | C19H16FN5O |
分子量 | 349.36 |
溶解度 | DMSO : 6.2 mg/mL (17.75 mM) |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | CFMTI is a potent and selective metabotropic glutamate receptor (mGluR) 1 allosteric antagonist with IC50 of 2.6 nM. The selectivity of CFMTI to mGluR1 over mGluR5 was >2000-fold.target : mGluRIC 50: 2.6 nMIn vitro: The IC50 values of CFMTI against human mGluR5 were 5400 ± 1200 nM, showing that the activity of CFMTI is more than 2000-fold weaker against human mGluR5 than against human mGluR1. CFMTI up to 10 μM exhibited no agonistic activity toward any group I mGluR subtypes (data not shown). The IC50 values of CFMTI were higher than 10 μM against all targets, such as NMDA receptorsIn vivo: CFMTI can dissolve in ethanol, polyethylene glycol 400, and distilled water (1:4:5, v/v/v) for intravenous administration. Oral administration of CFMTI inhibited DHPG-induced face-washing behavior in a dose-dependent manner. CFMTI produced dose-dependent inhibition of specific ex vivo binding of [3H]FTIDC to striatal and cerebellar slices in mice. CFMTI significantly inhibit hyperlocomotion induced by MAP at a dose of 2 mg/kg. [1]. Satow A et al. Unique antipsychotic activities of the selective metabotropic glutamate receptor 1 allosteric antagonist 2-cyclopropyl-5-[1-(2-fluoro-3-pyridinyl)-5-methyl-1H-1,2,3-triazol-4-yl]-2,3-dihydro-1H-isoindol-1-one. J Pharmacol Exp Ther. 2009 Jul;330(1):179-90. |