Labetalol (Synonyms: AH5158; Sch-15719W free base)
目录号: PL14291 纯度: ≥99%
CAS No. :36894-69-6
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中文名称
Labetalol
中文别名
柳胺苄心定;拉本他乐;降压乐;拉贝洛尔;拉贝洛尔标准品;2-羟基-5-{1-羟基-2-[(1-甲基-3-苯基丙基)氨基]乙基}苯甲酰胺
英文名称
Labetalol
英文别名
2-Hydroxy-5-(1-hydroxy-2-((4-phenylbutan-2-yl)amino)ethyl)benzamide;5-[1-HYDROXY-2-[(1-METHYL-3-PHENYLPROPYLAMINO)ETHYL]]SALICYLAMIDE;LABETALOL;rac Labetalol;2-Hydroxy-5-{1-hydroxy-2-[(1-methyl-3-phenylpropyl)amino]ethyl}benzamide;Labetolol;Albetol;Ibidomide;Labetalolum;Normodyne;Trandate;Labetalolum [INN-Latin];Labetalol [INN:BAN];AH 5158;5-(1-Hydroxy-2-(1-methyl-3-phenylpropylamino)ethyl)salicylamide;2-hydroxy-5-[1-hydroxy-2-(4-phenylbutan-2-ylamino)ethyl]benzamide;ScH 15719W;3-Carboxamido-4-hydroxy-alpha-((1-methyl-3-phenylpropylamino)methyl)benzyl alcohol;SGUAFYQXFOLMHL-UHFFFAO;Labetalol
Cas No.
36894-69-6
分子式
C19H24N2O3
分子量
328.41
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Labetalol (AH5158) 是一种具有口服活性的选择性 α1- 和非选择性 β-肾上腺素能受体 (adrenergic receptor) 竞争性拮抗剂。Labetalol 是一种抗高血压药物,可用于心血管疾病的研究,如妊娠期高血压。
生物活性
Labetalol (AH5158) is an orally active selective α1- and non-selective β-adrenergic receptors competitive antagonist. Labetalol, an anti-hypertensive agent, can be used for the research of cardiovascular disease, such as hypertension in pregnancy.
性状
Solid
IC50 & Target[1][2]
α1-adrenergic receptor β-adrenoceptor
体外研究(In Vitro)
Labetalol exhibits greater affinity for β-adrenergic sites on guinea pig heart and lung membranes (IC50=0.8 and 4.0 μM respectively) .
Labetalol has affinity for α-adrenergic binding sites (IC50=15 uM) on rabbit uterine membranes.Labctalol has 19 times greater binding affinity for β binding sites in heart membranca than α binding sites in uterine membranes. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Labetalol (10 mg/kg; i.h.) passes the blood-brain barrier, reaching a level of 2.1 ug/g tissue in the 10-day-old rat pups brain 90 min after injection. Labetalol (5.0 mg/kg; i.p.) attenuates circulating IL-1β and IL-6 in tailshock stress rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Brogden RN, et al. Labetalol: a review of its pharmacology and therapeutic use in hypertension. Drugs. 1978;15(4):251-270.
[2]. Greenslade FC, et al. Labetalol binding to specific alpha- and beta-adrenergic sites in vitro and its antagonism of adrenergic responses in vivo. J Mol Cell Cardiol. 1979 Aug;11(8):803-11.
溶解度数据
In Vitro: DMSO : 125 mg/mL (380.62 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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