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Betaxolol HCl/盐酸倍他洛尔 {[allProObj[0].p_purity_real_show]}

货号:A461855 同义名: SL75212; Betaxolol (hydrochloride)

Betaxolol HCl is a competitive and cardioselective β1 adrenergic receptor antagonist, used to treat hypertension, arrhythmias, coronary heart disease, glaucoma, and reduce non-fatal cardiac events in patients with heart failure with elimination half-life of 14–22 hours.

Betaxolol HCl/盐酸倍他洛尔 化学结构 CAS号:63659-19-8
Betaxolol HCl/盐酸倍他洛尔 化学结构
CAS号:63659-19-8
Betaxolol HCl/盐酸倍他洛尔 3D分子结构
CAS号:63659-19-8
Betaxolol HCl/盐酸倍他洛尔 化学结构 CAS号:63659-19-8
Betaxolol HCl/盐酸倍他洛尔 3D分子结构 CAS号:63659-19-8
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Betaxolol HCl/盐酸倍他洛尔 纯度/质量文件 产品仅供科研

货号:A461855 标准纯度: {[allProObj[0].p_purity_real_show]}
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Betaxolol 95%
Betaxolol HCl +

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97%
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Sotalol HCl 95+%
Nebivolol HCl +++

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Metoprolol 98+%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Betaxolol HCl/盐酸倍他洛尔 生物活性

靶点
  • β-adrenergic receptor

    β1-adrenergic receptor, IC50:6 μM

描述 Betaxolol hydrochloride (BH) is a cardioselective betaadrenergic receptor blocking agent used in the treatment of hypertension and glaucoma[3]. Betaxolol inhibited specific [3H]-batrachotoxinin-A 20-α-benzoate ([3H]-BTX-B) binding to neurotoxin site 2 in a concentration-dependent manner with an IC50 value of 9.8 μM. Betaxolol inhibited veratridine-stimulated Na+ influx in rat cortical synaptosomes with an IC50 value of 28.3 μM[4]. Moreover, the anxiolytic-like effect of betaxolol on cocaine-induced anxiety may be related to its effect on amygdalar beta(1)-adrenergic receptors that are up-regulated during early phases of drug withdrawal[5].

Betaxolol HCl/盐酸倍他洛尔 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT01316952 - Completed - -
NCT02617459 Primary Open-angle Glaucoma ... 展开 >> Ocular Hypertension 收起 << Phase 3 Unknown November 2016 China, Guangdong ... 展开 >> Zhongshan ophthalmic center, Sun Yat-sen University Recruiting Guangzhou, Guangdong, China, 510060 Contact: Jian Ge, MD    0+86-20-87330000       Principal Investigator: Jian Ge, MD 收起 <<
NCT00000132 Open-Angle Glaucoma Phase 3 Unknown - Sweden ... 展开 >> Department of Ophthalmology, Helsingborg Hospital Helsingborg, Sweden Department of Ophthalmology, Malmo University Hospital, University of Lund Malmo, Sweden 收起 <<

Betaxolol HCl/盐酸倍他洛尔 参考文献

[1]Wood JP, Schmidt KG, et al. The beta-adrenoceptor antagonists metipranolol and timolol are retinal neuroprotectants: comparison with betaxolol. Exp Eye Res. 2003 Apr;76(4):505-16.

[2]Tang LQ, Hong PH, et al. Effect of beta-adrenergic agents on intracellular potential of rabbit ciliary epithelium. Curr Eye Res. 1998 Jan;17(1):24-30.

[3]Auvity, S., Chiadmi, F., Cisternino, S., et al. A Rapid Stability-Indicating RP-HPLC Method for the Determination of Betaxolol Hydrochloride in Pharmaceutical Tablets. Anal Chem Insight. 2013; 8: 1-7.

[4]Chidlow, G., Melena, J., Osborne, NN. Betaxolol, a beta(1)-adrenoceptor antagonist, reduces Na(+) influx into cortical synaptosomes by direct interaction with Na(+) channels: comparison with other beta-adrenoceptor antagonists. Br J Pharmacol. 2000 Jum; 130(4):759-66.

[5]Rudoy, CA., Bockstaele, EJV. Betaxolol, a selective beta(1)-adrenergic receptor antagonist, diminishes anxiety-like behavior during early withdrawal from chronic cocaine administration in rats. Prog Neuropsychopharmacol Biol Psychiatry. 2007 Jun 30; 31(5): 1119-29.

Betaxolol HCl/盐酸倍他洛尔 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.91mL

0.58mL

0.29mL

14.54mL

2.91mL

1.45mL

29.08mL

5.82mL

2.91mL

Betaxolol HCl/盐酸倍他洛尔 技术信息

CAS号63659-19-8
分子式C18H30ClNO3
分子量 343.89
SMILES Code OC(CNC(C)C)COC1=CC=C(CCOCC2CC2)C=C1.[H]Cl
MDL No. MFCD00242959
别名 SL75212; Betaxolol (hydrochloride); ALO 140102; Kerlon; Betoptic; Kerlone; Betoptima; SL 75212 HCl; Betaxolol hydrochloride
运输蓝冰
InChI Key CHDPSNLJFOQTRK-UHFFFAOYSA-N
Pubchem ID 107952
存储条件

In solvent -20°C:3-6个月-80°C:12个月

Pure form Inert atmosphere, room temperature

溶解方案

DMSO: 105 mg/mL(305.33 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 10 mg/mL(29.08 mM),配合低频超声助溶

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
方案二
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案一
动物实验配方

PO 0.5% CMC-Na 50 mg/mL clear

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