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.
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产品名称 | Adrenergic Receptor ↓ ↑ | α-adrenergic receptor ↓ ↑ | β-adrenergic receptor ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Ivabradine HCl | ✔ | 98% | |||||||||||||||||
Maprotiline HCl | ✔ | 98% | |||||||||||||||||
Cisatracurium besylate | ✔ | 96% | |||||||||||||||||
Yohimbine HCI | ✔ | 99+% | |||||||||||||||||
BMY 7378 |
++
α2C-adrenoceptor, pKi: 6.54 α1D-adrenoceptor, pKi: 5.1 |
+
β1-adrenoceptor, pIC50: 5.1 |
97% | ||||||||||||||||
Asenapine maleate |
++++
α2A-adrenergic receptor, pKi: 8.9 α2B-adrenergic receptor, pKi: 8.9 |
97% | |||||||||||||||||
Piribedil |
++
adrenoceptor α2C, pKi: 7.2 adrenoceptor α2A, pKi: 7.1 |
98% | |||||||||||||||||
Prazosin HCl | ✔ | 95% | |||||||||||||||||
Silodosin | ✔ | 98% | |||||||||||||||||
Phenoxybenzamine HCl | ✔ | 98% | |||||||||||||||||
Labetalol HCl | ✔ | 98+% | |||||||||||||||||
Naftopidil |
+++
α1D-adrenergic receptor, Ki: 20 nM α1A-adrenergic receptor, Ki: 3.7 nM |
98% | |||||||||||||||||
Naftopidil 2HCl |
+
α1-adrenergic receptor, IC50: 0.2 μM |
99% | |||||||||||||||||
Alfuzosin HCl | ✔ | 98% | |||||||||||||||||
Terazosin HCl | ✔ | 99% | |||||||||||||||||
Atipamezole | ✔ | 95% | |||||||||||||||||
Phentolamine methanesulfonate salt | ✔ | 99% | |||||||||||||||||
Carvedilol | ✔ | 98% | |||||||||||||||||
Doxazosin mesylate | ✔ | 99% | |||||||||||||||||
Tolazoline HCl | ✔ | 98% | |||||||||||||||||
Esmolol HCl | ✔ | 95% | |||||||||||||||||
Propranolol HCl |
++
β-adrenergic receptor, IC50: 12 nM |
98% | |||||||||||||||||
Zenidolol HCl |
++++
β2-adrenergic receptor, Ki: 0.7nM β1-adrenergic receptor, Ki: 611nM |
98% | |||||||||||||||||
Acebutolol HCl | ✔ | 97+% | |||||||||||||||||
Carteolol HCl | ✔ | 98+% | |||||||||||||||||
Betaxolol | ✔ | 95% | |||||||||||||||||
Betaxolol HCl |
+
β1-adrenergic receptor, IC50: 6 μM |
97% | |||||||||||||||||
Bisoprolol | ✔ | 97% | |||||||||||||||||
Sotalol HCl | ✔ | 95+% | |||||||||||||||||
Nebivolol HCl |
+++
β1-adrenoceptor, IC50: 0.8 nM |
99% | |||||||||||||||||
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。 |
靶点 |
|
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]. |
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 << |
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 |
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 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
|
动物实验配方 |
PO 0.5% CMC-Na 50 mg/mL clear |