1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENBQXCat. No.: HY-15068CAS No.: 118876-58-7Synonyms: FG9202分式: CHNOS分量: 336.28作靶點: iGluR作通路: Membrane Transporter/Ion Channel; Neuronal Signaling儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO

2、 : 75 mg/mL (223.03 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (7.43 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (7.43 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility:

3、 2.5 mg/mL (7.43 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 NBQX度選擇性，競爭型的AMPA受體拮抗劑。IC50 & Target AMPA receptor 1體外研究 NBQX has a high affinity for AMPA and kainate binding sites with little or no affinity for the glutamaterecognition site on the NMDA receptor complex 1.體內(nèi)研究 NBQX is neuroprotective in

4、a focal ischaemia model in the rat when given as an i.v. bolus dose of 30 mg/kgat the time of MCA occlusion and again at 1 h post occlusion 1. NBQX provides potent anticonvulsantprotection against AMPA. The ED50 values for the protection against AMPA-induced seizures by NBQX (30min, i.p.) is 23.6 (1

5、1.6- 48.0) 2.PROTOCOLAnimal Rats 1Administration 1 Male Sprague-Dawley rats weighing 350-390 g are used for study. 30 mg/kg of NBQX (2x15 mg/mL) isadministered i.v. as a bolus dose followed by an infusion of 10 mg/kg/h for 4 h, the bolus dose and infusionare started immediately after MCA occlusion.

6、Blood samples are taken from these animals at 1, 2, 3 and 4 hafter the start of the infusion and the plasma level of NBQX in each sample is measured 1.Mice 1The time course for the anticonvulsant action of NBQX and of GYKI 52466 against AMPA-induced seizuresis determined by pretreating groups (n=10)

7、 of Swiss mice with 30 and 60/zmol/kg NBQX or GYKI 52466 (i.p.)15-120 min before challenging the mice with a convulsant dose of AMPA (5 nmol) i.c.v 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Nat Med. 2019 Feb;25(2):337-349.See more cu

8、stomer validations on HYPERLINK / www.MedChemEREFERENCES1. Fukushima K, et al. Characterization of Human Hippocampal Neural Stem/Progenitor Cells and Their Application to PhysiologicallyRelevant Assays for Multiple Ionotropic Glutamate Receptors. J Biomol Screen. 2014 Sep; 19(8):1174-84.McePdfHeight2/2 Master of Small Molecules 您邊的抑制劑師www.MedChemECaution: Product has not been fully validated for medical applicatio