KUL-7211 racemate
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| 包装规格: | 25mg 50mg 100mg in glass bottle |
| 产品描述: | 基本信息 产品编号: K10116 产品名称: KUL-7211 racemate CAS: 911196-40-2 储存条件 粉末 -20℃ 四年 分子式: C19H23NO5 溶于液体 -80℃ 二年 分子量: 345.39 化学名: 2-[4-[2-[[1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]phenoxy]acetic Acid 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。 生物活性 产品描述 是 KUL-7211的外消旋体。KUL-7211 是一种选择性 β-肾上腺素受体激动剂。 靶点 β-adrenoceptor 体外研究 KUL-7211 is a new β-adrenoceptor agonist in vitro.In rat isolated organs,its selectivities,for inhibition of spontaneous uterine contraction (mediated via β2-adrenergic stimulation) and inhibition of colonic contraction (via β3-adrenergic stimulation) versus increase in atrial rate (via β1-adrenergic stimulation),are 56.3 and 242.2,respectively.KUL-7211 relaxes 80 mM KCl induced tonic contractions in both rabbit (pD2 value:5.86±0.13,whose ureteral relaxation is mediated via β2-adrenergic stimulation) and canine (pD2 value:6.52±0.16,via β3-adrenergic stimulation) isolated ureters in a concentrationdependent manner.These KUL-7211-induced relaxing effects are antagonized by ICI-118,551 (selective β2-adrenoceptor antagonist,pKB value: 8.91±0.24) in the rabbit ureter and by bupranolol (non-selective β-adernoceptor antagonist,pKB value:6.85±0.12) in the canine ureter.KUL-7211 also reduces the spontaneous rhythmic contraction in a canine ureteral spiral preparation in a concentration-dependent manner,the pD2 value being 6.83±0.20.These data clearly demonstrate that KUL-7211 selectively stimulates both ureteral β2- and β3-adrenoceptors and potently relaxes ureteral smooth muscle. |
| 保存条件: | -20℃ |
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