NS-638 - Calcium Channel 抑制剂 - 生命科学试剂 - 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作靶点: Calcium Channel作通路: Membrane Transporter/Ion Channel; Neuronal Signaling储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO :

2、 34 mg/mL (104.38 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液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请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。BIOLOGICAL ACTIVITY物活性 NS-638具有阻断Ca2+-离通道性质的

3、肽类分。细胞内阻断由K+激活的Ca2+浓度升的IC50值为3.4M。IC50 & Target IC50: 3.4 M (K+-stimulated intracellular Ca2+-elevation) 1体外研究NS-638 dose dependently inhibits K+-stimulated 45 Ca2+-uptake in chick cortical synaptosomes and 2-1/2 Master of Small Molecules 您边的抑制剂师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.体内研究 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