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Levcromakalim  ≥98%

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包装规格：2mg 5mg 10mg 50mg in glass bottle
溶解性：溶于DMSO(≥50mg/ml)
产品描述：基本信息 产品编号： L10517 产品名称： Levcromakalim CAS: 94535-50-9   储存条件 粉末 -20℃ 四年     分子式： C16H18N2O3 溶于液体 -80℃ 6个月 分子量： 286.33 -20℃ 1个月 化学名：  2H-1-Benzopyran-6-carbonitrile,3,4-dihydro-3-hydroxy-2,2-dimethyl-4-(2-oxo-1-pyrrolidinyl)-,(3S,trans)- Solubility (25°C)：   体外:   DMSO   Ethanol   Water   体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 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；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 3.4925mL 17.4624mL 34.9247mL 5mM 0.6985mL 3.4925mL 6.9849mL 10mM 0.3492mL 1.7462mL 3.4925mL   生物活性 产品描述 一种ATP敏感性的K+通道(KATP)激活剂。 靶点 K+channel   体外研究 Levcromakalim ((-)-Cromakalim) inhibits spontaneous contractions completely in a glibenclamide-sensitive manner.LevCromakalim (5µM) inhibits spontaneous contractions,which are recovered by glibenclamide. Levcromakalim (1,5 and 10µM) inhibits phasic contractions to 34±21.1%,20.1±20.0% and 0% of the control (n=5,respectively;P<0.05).Glibenclamide reverses the inhibition of spontaneous isometric contractions caused by LevCromakalim (5µM) to 84±1.5% of the control (n=5;P<0.05).Levcromakalim (20 and 100µM) also inhibits oxytocin (OXT) (10nM-induced phasic contractions to 34±21.4% and 14±12.6% of the control (n=6 and 4,respectively;P<0.05).Glibenclamide reverses the inhibition of spontaneous isometric contractions by LevCromakalim (100µM) to 79±3.5% of the control (n=4;P<0.05).Tonic contraction by OXT is also suppressed by Cromakalim in a glibenclamide-sensitive manner.The function of the KATP channels is examined with the specific channel opener LevCromakalim (Cromakalim).LevCromakalim induces dose-dependent relaxation in both the young and old mesenteric artery (MAs);and there is no difference in relaxation with age.However,the relaxation is markedly reduced in response to the high-salt (HS) diet in the old MAs (P<0.05).Maximum dilations to Levcromakalim (10-4 M) are 97±3% in the young MAs versus 98±1% in the young salt arteries,while dilations are 99±0.7% in the old MAs when compared with 85±5% in the old salt arteries (P<0.05).   推荐实验方法(仅供参考) 激酶实验： Levcromakalim (Cromakalim) is dissolved in 10% DMSO and Krebs solution.The endothelium-dependent relaxation is tested by performing concentration-response experiments with acetylcholine (ACh;10 nM-10μM).Typically,MAs are exposed to each dose of ACh for at least 6 minutes and maximal responses are determined.Function of the KATP channels are examined with 10µM of glibenclamide (a selective KATP channel inhibitor) and Levcromakalim (Cromakalim) (10nM to 100μM),a KATP channel opener.The addition of glibenclamide to the arterial bath 10 minutes prior to ACh does not alter passive maximum internal diameters of any MAs in our groups.The vessel diameter changes are presented as percentages (%) of dilation of the preconstricted vessels,calculated.
保存条件：-20℃

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