1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIsoguvacine hydrochlorideCat. No.: HY-100810CAS No.: 68547-97-7分式: CHClNO分量: 163.6作靶點: GABA Receptor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

2、解性數據體外實驗 DMSO : 30 mg/mL (183.37 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 6.1125 mL 30.5623 mL 61.1247 mL5 mM 1.2225 mL 6.1125 mL 12.2249 mL10 mM 0.6112 mL 3.0562 mL 6.1125 mL請根據產品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內實驗請根據您的實驗動物和給藥式選擇適當的溶解案，配制

3、前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結果的可靠性，體內實驗的作液，建議您現現配，當天使；澄的儲備液可以根據儲存條件，適當保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (15.28 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (15.28 mM); Clear solution3.

4、請依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (15.28 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Isoguvacine hydrochlorideGABA 受體激動劑。IC50 & Target GABA 1體外研究 Isoguvacine binds to a mouse forebrain synaptic membrane preparation. The specific bind

5、ing is displaceableby GABA, muscimol and bicuculline but not by picrotoxin or diaminobutyric acid. Kinetic data suggest twobinding affinities. Highest levels of binding are observed in the cerebellum, cortex and hippocampus 1.Isoguvacine binds to membrane preparations of rat forebrain with pharmacol

6、ogical characteristics similar tothe postsynaptic GABA recognition site: that it is transported into synaptosomal preparations by an uptakesystem similar to the high-affinity GABA uptake system; and that recently accumulated isoguvacine isreleased in a Ca2+-dependent manner and by heteroexchange wit

7、h external GABA 2. Isoguvacine at aconcentration of 50 M blocks the seizure like events in 2 out of 6 organotypic hippocampal slice cultures.Isoguvacine inhibits the low magnesium induced seizure like events dose dependently 3.PROTOCOLKinase Assay 1 The assay for 3H-Isoguvacine binding is carried ou

8、t as follows: membranes suspended in Tris-citrate bufferpH 7.1 are incubated at 4C for 10 min with 8 nM 3H-Isoguvacine. Identical samples are incubated in thepresence of cold 0.5 mM GABA or 10 M cold isoguvacine. The assay is terminated by centrifugation for 10min at 4C in a micro-centrifuge. The su

9、pernatants are rapidly aspirated and the surface of the pelletswashed (2x) with ice-cold buffer. The pellet is resuspended in I00 L of 0.1% Triton and placed in ascintillation vial. The assay tube is washed with I00 L of distilled water and the wash added to the vial alongwith 10 ml of PCS: xylene (

10、2:1). Counting efficiency is determined to be 40-45% in a Beckman liquidscintillation counter. Specific binding is defined as those radioactive cpm of bound 3H-Isoguvacine that aredisplaced by excess cold isoguvacine or GABA 1.MCE has not independently confirmed the accuracy of these methods. They a

11、re for reference only.REFERENCES1. Morin AM, et al. The binding of 3H-isoguvacine to mouse brain synapticmembranes. Life Sci. 1980 Apr 14;26(15):1239-45.2. White WF, et al. Isoguvacine binding, uptake, and release: relation to the GABA system. J Neurochem. 1983 Jun;40(6):1701-8.3. Wahab A, et al. Effects of gamma-aminobutyric acid (GABA) agonists and a GABA uptake inhibitor on pharmacoresistant seizure likeevents in organotypic hippocampal slice cultures. Epilepsy Res. 2009 Oct;86(2-3):113-23.McePdfHeightCaution: Produc