| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Bevantolol targets β1-adrenoceptors as a selective antagonist, with a pKi of 7.83 in rat cerebral cortex. It also targets α1-adrenoceptors as an antagonist, with a pKi of 6.9. Additionally, bevantolol acts as a calcium channel blocker (Ca²⁺ antagonist). By blocking β1-adrenoceptors, it reduces heart rate and cardiac contractility. By blocking α1-adrenoceptors and calcium channels, it causes vasodilation. This dual mechanism makes bevantolol effective for treating angina and hypertension.
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| ln Vitro |
On β2-adrenergic receptors, bevanol hydrochloride has a pKi of 6.23[1].
In vitro, bevantolol is a selective β1/α1-adrenergic receptor antagonist and a calcium channel blocker. It has a pKi of 7.83 for β1-adrenoceptors and 6.9 for α1-adrenoceptors in rat cerebral cortex. In cell-based assays, bevantolol treatment results in inhibition of β1-adrenoceptor-mediated signaling, inhibition of calcium influx, and vasodilation. The compound's effects on adrenergic receptors and calcium channels are assessed using radioligand binding assays and electrophysiology. |
| ln Vivo |
The expression level of β1-adrenergic receptor mRNA can be considerably reduced by bevanol hydrochloride (200 mg/kg; oral; for 6 weeks) [2].
In vivo, bevantolol hydrochloride is used for the treatment of angina and hypertension. It has a peripheral vasodilatory effect. Bevantolol blocks β1-adrenoceptors, inhibiting epinephrine-mediated sympathetic actions such as increased heart rate. Its calcium channel blocking activity contributes to its vasodilatory and antihypertensive effects. Bevantolol has been used clinically for the treatment of angina pectoris and hypertension. It is available as a prescription medication in some countries. |
| Enzyme Assay |
In vitro receptor binding assays for bevantolol involve measuring its binding affinity to β1 and α1-adrenoceptors. The receptors are incubated with a radiolabeled ligand and varying concentrations of bevantolol. The displacement of the radiolabeled ligand is measured, and the pKi values (7.83 for β1, 6.9 for α1) are calculated. Calcium channel blocking activity is assessed using patch-clamp electrophysiology in isolated cardiac or vascular smooth muscle cells. These assays confirm the compound's dual mechanism.
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| Cell Assay |
In vitro cell-based assays for bevantolol evaluate its effects on adrenergic receptor signaling and calcium influx. Cells expressing β1 or α1-adrenoceptors are cultured and treated with bevantolol. Receptor signaling is assessed by measuring cAMP accumulation or calcium mobilization. Calcium influx is measured using fluorescent calcium indicators. These assays confirm the compound's functional activity as an adrenergic receptor antagonist and calcium channel blocker.
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| Animal Protocol |
Animal/Disease Models: Male Wistar rats, body weight 250-300 g [2]
Doses: 200 mg/kg Route of Administration: Oral administration with water; lasted for 6 weeks. Experimental Results: The expression level of β1 adrenergic receptor mRNA was Dramatically diminished. In vivo animal experiments for bevantolol have been conducted in animal models of hypertension and angina. Animals are treated with bevantolol, and blood pressure, heart rate, and cardiac function are assessed. The compound's efficacy in reducing blood pressure and improving cardiac function has been demonstrated in preclinical studies. Pharmacokinetic studies are conducted to determine the compound's absorption, distribution, metabolism, and excretion. Comprehensive in vivo studies are available from clinical development. |
| ADME/Pharmacokinetics |
Bevantolol is absorbed after oral administration and is metabolized in the liver. It has a molecular weight of 381.90 g/mol. The compound's half-life, bioavailability, and excretion profile have been characterized in clinical studies. Bevantolol hydrochloride is a racemic mixture. It is available as a prescription medication in some countries.
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| Toxicity/Toxicokinetics |
The toxicity of bevantolol includes common beta-blocker side effects such as bradycardia, hypotension, and fatigue. It should be used with caution in patients with heart failure, asthma, or bradycardia. Bevantolol is available as a prescription medication in some countries.
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| References |
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| Additional Infomation |
Bevantolol Hydrochloride is a selective β1/α1-adrenergic receptor antagonist and calcium channel blocker. It has a peripheral vasodilatory effect and is used for the treatment of angina and hypertension. Bevantolol has a pKi of 7.83 for β1 and 6.9 for α1 receptors. It is a racemic mixture. Bevantolol is available as a prescription medication in some countries.
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| Molecular Formula |
C20H28CLNO4
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|---|---|
| Molecular Weight |
381.8936
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| Exact Mass |
381.17
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| CAS # |
42864-78-8
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| Related CAS # |
Bevantolol;59170-23-9
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| PubChem CID |
39324
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| Appearance |
White to off-white solid powder
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| Boiling Point |
518.3°C
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| LogP |
3.777
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
26
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| Complexity |
355
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
FJTKCFSPYUMXJB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C20H27NO4.ClH/c1-15-5-4-6-18(11-15)25-14-17(22)13-21-10-9-16-7-8-19(23-2)20(12-16)24-3;/h4-8,11-12,17,21-22H,9-10,13-14H2,1-3H3;1H
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| Chemical Name |
1-[2-(3,4-dimethoxyphenyl)ethylamino]-3-(3-methylphenoxy)propan-2-ol;hydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~163.66 mM)
H2O : ~4.55 mg/mL (~11.91 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 6.25 mg/mL (16.37 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication (<60°C).
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6186 mL | 13.0928 mL | 26.1856 mL | |
| 5 mM | 0.5237 mL | 2.6186 mL | 5.2371 mL | |
| 10 mM | 0.2619 mL | 1.3093 mL | 2.6186 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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