| 产品描述: | BMS 191011 (BMS-A) is a potent BKCa channel opener (large-conductance Ca2+-activated potassium channel). BMS-191011 shows neuroprotective activities in rodent models of stroke |
| 靶点: |
Potassium Channel;PotassiumChannel |
| 体外研究: |
BMS-191011 (20 or 40 µM) activates BK channels in IGR39 cells, and leads to potentiation in Panc-1 cells. Cell Viability Assay Cell Line: IGR39 and Panc-1 cells Concentration: 20 or 40 µM Incubation Time: Result: Activated BK channels in less than 50% IGR39 cells and led to less than two-fold potentiation in Panc-1 cells.Promoted the activation of a voltage-independent K+ conductance at negative voltages. |
| 体内研究: |
BMS-191011 (intravenous injection; 10-100 µg/kg; once) dilates rat retinal arterioles through activation of iberiotoxin-sensitive BK(Ca) channels in vivo. Animal Model: Male Wistar rats (8- to 10-week-old) treated with Tetrodotoxin (50 µg/kg, intravenously (i.v.)) Dosage: 10-100 µg/kg Administration: Intravenous injection; 10-100 µg/kg; once Result: Increased the diameter of retinal arterioles, showed no significant effect on mean arterial pressure and heart rate. |
| 参考文献: |
1. Romine JL, et al. 3-[(5-Chloro-2-hydroxyphenyl)methyl]-5-[4-(trifluoromethyl)phenyl ]-1,3,4-oxadiazol-2(3H)-one, BMS-191011: opener of large-conductance Ca(2+)-activated potassium (maxi-K) channels, identification, solubility, and SAR. J Med Chem. 2007 Feb 8;50(3):528-42. 2. Asami Mori, et al. BMS-191011, an opener of large-conductance Ca2+-activated potassium channels, dilates rat retinal arterioles in vivo. Biol Pharm Bull. 2011;34(1):150-2. 3. Remigante A, et al. NS-11021 Modulates Cancer-Associated Processes Independently of BK Channels in Melanoma and Pancreatic Duct Adenocarcinoma Cell Lines. Cancers (Basel). 2021 Dec 6;13(23):6144. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-20℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.698 ml |
13.488 ml |
26.975 ml |
| 5 mM |
0.54 ml |
2.698 ml |
5.395 ml |
| 10 mM |
0.27 ml |
1.349 ml |
2.698 ml |
| 50 mM |
0.054 ml |
0.27 ml |
0.54 ml |
|
| 注意: |
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