NS-638 - Calcium Channel 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemENS-638Cat. No.: HY-101428CAS No.: 150493-34-8分式: CHClFN分量: 325.72作靶點: Calcium Channel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、 34 mg/mL (104.38 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 3.0701 mL 15.3506 mL 30.7012 mL5 mM 0.6140 mL 3.0701 mL 6.1402 mL10 mM 0.3070 mL 1.5351 mL 3.0701 mL請根據(jù)產(chǎn)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。BIOLOGICAL ACTIVITY物活性 NS-638具有阻斷Ca2+-離通道性質(zhì)的

3、肽類分。細(xì)胞內(nèi)阻斷由K+激活的Ca2+濃度升的IC50值為3.4M。IC50 & Target IC50: 3.4 M (K+-stimulated intracellular Ca2+-elevation) 1體外研究NS-638 dose dependently inhibits K+-stimulated 45 Ca2+-uptake in chick cortical synaptosomes and 2-1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEamino-3-(3-hydroxy-5-methylisoxazol-4-yl)p

4、ropionic acid (AMPA)- stimulated 3HGABA-release fromcultured cortical neurons with IC50 values of 2.3 and 4.3 M, respectively. K+-stimulated intracellular Ca2+-elevation in cultured cerebellar granule cells is equipotently blocked with an IC50 value of 3.4 M. At thisconcentration no effect on Ca2+-i

5、nduced contractions in K+-depolarized guinea pig taenia coli is observed.NS-638 reversibly blocks N- and L-type Ca2+-channels in cultured chick dorsal root ganglion cells in theconcentration range of 1-30 M 1.體內(nèi)研究 In the mouse middle cerebral artery occlusion model, NS-638 administered i.p. (50 mg k

6、g-1) at 1 h and 6 hpost-ischemia, and once a day for the next two days, results in a 48% reduction in total infarct volume. Itdoes not show protection against ischemic neuronal damage in the gerbil model of bilateral carotid arteryocclusion 1.PROTOCOLCell Assay 1 The effect of NS-638 on neuronal Ca2

7、+-channels is evaluated using whole cell patch clamp techniques 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice: In the mouse middle cerebral artery occlusion model, NS-638 is administered i.p. (50 mg kg-1) at 1 hAdministration 1 and 6 h p

8、ost-ischemia, and once a day for the next two days 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Mller A, et al. Pharmacological profile and anti-ischemic properties of the Ca(2+)-channel blocker NS-638. Neurol Res. 1995Oct;17(5):353-60.McePdfHeightCaution: Product has not been fully validated for medical applications