Levcromakalim-minus-Cromakalim-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemELevcromakalimCat. No.: HY-14255CAS No.: 94535-50-9Synonyms: (-)-Cromakalim; BRL 38227分式: CHNO分量: 286.33作靶点: Potassium Channel作通路: Membrane Transporter/Ion Channel储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 m

2、onth溶解性数据体外实验 DMSO : 50 mg/mL (174.62 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (8.73 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Molecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (8.73 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Levcromakalim (-)-C

3、romakalim)是ATP 敏感性的 K+ 通道 (KATP) 激活剂。IC50 & Target K+ channel 1体外研究 Levcromakalim (-)-Cromakalim) inhibits spontaneous contractions completely in a glibenclamide-sensitivemanner. LevCromakalim (5 M) inhibits spontaneous contractions, which are recovered by glibenclamide.Levcromakalim (1, 5 and 10 M)

4、 inhibits phasic contractions to 3421.1%, 20.120.0% and 0% of the control(n=5, respectively; P 2.The function of the KATP channels is examined with the specific channel openerLevCromakalim (Cromakalim). LevCromakalim induces dose-dependent relaxation in both the young and oldmesenteric artery (MAs);

5、 and there is no difference in relaxation with age. However, the relaxation ismarkedly reduced in response to the high-salt (HS) diet in the old MAs (P-4 M) are 97 3% in the young MAsversus 98 1% in the young salt arteries, while dilations are 990.7% in the old MAs when compared with 85 5% in the ol

6、d salt arteries (P 3.PROTOCOLKinase Assay 3 Levcromakalim (Cromakalim) is dissolved in 10% DMSO and Krebs solution 3.The endothelium-dependent relaxation is tested by performing concentration-response experiments withacetylcholine (ACh; 10 nM-10 M). Typically, MAs are exposed to each dose of ACh for

7、 at least 6 minutesand maximal responses are determined. Function of the KATP channels are examined with 10 M ofglibenclamide (a selective KATP channel inhibitor) and Levcromakalim (Cromakalim) (10 nM to 100 M), aKATP channel opener. The addition of glibenclamide to the arterial bath 10 minutes prio

8、r to ACh does notalter passive maximum internal diameters of any MAs in our groups.The vessel diameter changes arepresented as percentages (%) of dilation of the preconstricted vessels, calculated 3.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERE

9、NCES1. Matsumoto T, et al. Tunicamycin-Induced Alterations in the Vasorelaxant Response in Organ-Cultured Superior Mesenteric Arteries ofRats. Biol Pharm Bull. 2016;39(9):1475-81.2. Hong SH, et al. Regulation of myometrial contraction by ATP-sensitive potassium (KATP) channel via activation of SUR2B and Kir 6.2 inmouse. J Vet Med Sci. 2016 Aug 1;78(7):1153-9.3. Whidden MA, Altered potassium ATP channel signaling in mesenteric arteries of old high salt-fed rats. J Exerc Nutrition Biochem. 2016Jun;20(2):58-64.McePdfHeightCaution: Product has not been fully validate