Art. -Nr.: HY-A0249

Bevantolol

Name: Bevantolol
Brand: MedChemExpress
SKU: HY-A0249
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(Synonyms: SOM3355 free base)

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Bevantolol (SOM3355 (free base)) is a selective β1-adrenergic receptor antagonist, with an IC₅₀ of 35 nM for β₁-adrenergic receptor and an IC₅₀ of 60 nM for VMAT2. Bevantolol blocks β1-adrenergic receptors, exerts partial agonistic effects on α-adrenoceptor, inhibits calcium currents in the sinoatrial and atrioventricular nodes as well as sodium currents in cardiomyocytes, delays repolarization, and shortens the action potential duration of Purkinje cells. Bevantolol reduces peripheral vascular resistance, increases subendocardial blood flow, inhibits VMAT2, elevates the serum HDL/LDL ratio, and does not affect glomerular filtration rate or cause cold extremities. Bevantolol is applicable to research related to angina pectoris, hypertension, arrhythmia, and Huntington's disease.

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Reinheit: 98.19%
CAS. Nr.: 59170-23-9
Formel: C₂₀H₂₇NO₄
Molecular Weight:345.43

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Bevantolol Chemical Structure

CAS. Nr.: 59170-23-9

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

^[1]^[2]

Beta-1 adrenergic receptor

35 nM (IC₅₀)

VMAT2

60 nM (IC₅₀)

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen :

In Vitro

Bevantolol (1.0-10.0 μmol/L) directly reduces the spontaneous rate of isolated rabbit atria^[1].
Bevantolol potently inhibits the β₁-adrenergic receptor with an IC₅₀ of 35 nM^[2].
Bevantolol blocks the isoproterenol-induced chronotropic response in isolated rabbit atria, with a pA₂ value of approximately 7.6 to 8.1^[1].
Bevantolol exhibits 32-fold higher affinity for β-1 adrenergic receptors in guinea pig atria (K_B = 0.9 × 10^-8) than for β-2 adrenergic receptors in guinea pig trachea (K_B = 3.0 × 10^-7)^[1].
Bevantolol (2-8 μmol/L) inhibits the inward calcium current in rabbit sinoatrial and atrioventricular nodal cells, reduces MRD and shifted pacemaker potential, and delays repolarization, thereby inducing bradycardia without affecting the slope of diastolic slow potential^[1].
Bevantolol (2-8 μmol/L) exerts class I antiarrhythmic effects on rabbit atrial cells, Purkinje cells and ventricular cells, reduces the MRD of most cells, delays repolarization, and shortens the action potential duration of preterminal Purkinje cells^[1].
Bevantolol exerts no negative inotropic effect on rabbit atrial or ventricular cardiomyocytes, nor does it inhibit calcium-mediated positive inotropic effects^[1].
Bevantolol exhibits higher binding affinity for α-1 adrenergic receptors in rat brain cell membranes than norepinephrine^[1].
Bevantolol acts as an α-adrenergic receptor antagonist in isolated rabbit aortic strips, inhibits phenylephrine-induced contractions, and has no agonist activity^[1].
Bevantolol (1-10 μM) induces dose-dependent bradycardia, inhibits calcium-induced tachycardia, and blocks β-adrenergic receptors without exerting negative inotropic effects in isolated rabbit atria^[3].
Bevantolol (2-8 μM; 40 min) dose-dependently decreases the heart rate, peak action potential amplitude, and depolarization/repolarization rate of rabbit sinoatrial node cells and sinoatrial node transitional cells, while increasing the pacemaker potential and prolonging the repolarization duration^[3].
Bevantolol (2-8 μM; 40 min) dose-dependently prolongs the conduction time of the atrioventricular conduction pathway in rabbits, with the strongest inhibitory effect on the atrioventricular node itself. It also reduces the depolarization rate of atrioventricular node cells and prolongs the action potential duration^[3].
Bevantolol (2-8 μM; 40 min) reduces the maximum depolarization rate and action potential amplitude in a dose-dependent manner, alters action potential duration in a region-specific manner, and has no effect on the resting potential of rabbit prepurkinje and purkinje cells^[3].
Bevantolol (2-8 μM; 40 min) reduces the maximum depolarization rate and action potential amplitude of rabbit atrial and ventricular cardiomyocytes in a dose-dependent manner, and prolongs the action potential duration^[3].
Bevantolol exhibits inhibitory effects on VMAT2, with an IC₅₀ value of 60 nM^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	T_max	T_1/2α	T_1/2β
Rat^[1]	10 mg/kg	p.o.	30 min	4.1 h	12.6 h

In Vivo

Bevantolol (0.72-18.0 μmol/kg; intravenous injection; single administration) is selective for β-1 adrenergic receptors, induces dose-dependent bradycardia in spinal cord-transected rats, and exhibits no intrinsic sympathomimetic activity in catecholamine-depleted rats^[1].
Bevantolol (0.3-10.0 mg/kg; intravenous injection; single administration) induces dose-dependent increases in mean blood pressure, decreases in heart rate, and potentiates the pressor response induced by phenylephrine in pentobarbital-anesthetized spinal rats^[1].
Bevantolol (1.0 mg/kg; intravenous injection; single administration) significantly improves subendocardial blood flow and systolic function in the ischemic region of dogs with partial coronary artery occlusion^[1].
Bevantolol (0.3-10 mg/kg; intravenous injection; single administration) induces variable hemodynamic effects in anesthetized dogs, accompanied by dose-dependent changes in total peripheral resistance and mean arterial pressure, and also increases cardiac output and total peripheral resistance in dogs after coronary artery ligation^[1].
Bevantolol (1.0-1.5 mg/kg; intravenous injection; single administration) induces dose-dependent decreases in mean arterial pressure, bradycardia, and reduced cardiac output in anesthetized, thoracotomized Sus scrofa domesticus with high baseline sympathetic nerve activity^[1].
Bevantolol (0.72-18.0 μmol/kg; intravenous injection; cumulative administration every 30 min) acts as a β₁-selective adrenoceptor antagonist in spinal cord-transected rats, producing dose-dependent bradycardia, hypertension, enhanced norepinephrine-induced pressor responses, and atrioventricular/bundle branch block, with minimal effects on isoproterenol-mediated β₂-dependent hypotensive responses at lower doses^[3].
Bevantolol (intravenous injection, 0.2-10.0 mg/kg) induces bradycardia and mild hypotension in anesthetized dogs, and selectively blocks β₁ receptor-mediated effects of isoproterenol; high doses increase blood pressure and peripheral vascular resistance, while moderate doses improve stroke volume after coronary artery ligation^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Rats (conscious, catecholamine-depleted; anesthetized, catecholamine-depleted; pithed)^[1]
Dosage:

0.72 μmol/kg; 3.6 μmol/kg; 18.0 μmol/kg
Administration:

i.v.; single dose
Result:

Demonstrated no significant effect on heart rate in conscious or anesthetized catecholamine-depleted rats, showing no intrinsic sympathomimetic activity.
Reduced heart rate by 8.3%, 9.0%, and 15.3% at doses of 0.72, 3.6, and 18.0 μmol/kg i.v., respectively.
Progressively blocked the chronotropic responses to intravenous isoproterenol (20 ng, 50 ng) at doses of 0.72, 3.6, and 18.0 μmol/kg i.v.
Did not affect falls in blood pressure in pithed rats in response to intravenous isoproterenol (20 ng, 50 ng) at 0.72 and 3.6 μmol/kg i.v., and only slightly reduced this response (not significant) at 18.0 μmol/kg i.v., confirming beta-1 adrenoceptor selectivity.

Animal Model:

Rats (anesthetized, pentobarbital-treated, pithed)^[1]
Dosage:

0.3 mg/kg; 1.0 mg/kg; 3.0 mg/kg; 10.0 mg/kg
Administration:

i.v.; single dose
Result:

Caused mean increases in mean blood pressure of 9, 8, 9, and 15 mmHg at doses of 0.3, 1.0, 3.0, and 10.0 mg/kg i.v., respectively.
Reduced mean heart rate by 19, 43, 62, and 144 beats/min at doses of 0.3, 1.0, 3.0, and 10.0 mg/kg i.v., respectively.
Increased phenylephrine-induced mean blood pressure increase from 89 mmHg before administration to 98 mmHg after administration in a subgroup of rats.

Animal Model:

Dogs (anesthetized, open-chest)^[1]
Dosage:

1.0 mg/kg
Administration:

i.v.; single dose
Result:

Increased subendocardial blood flow in the ischemic region by 20%.
Increased contractile force in the ischemic region by 36%.
Raised the endocardial-epicardial flow ratio from 0.59 to 0.93.

Animal Model:

Dogs (anesthetized; anesthetized, post coronary ligation)^[1]
Dosage:

0.3 mg/kg; 3.0 mg/kg; 1.0 mg/kg; 10 mg/kg
Administration:

i.v.; single dose
Result:

In one anesthetized dog, increased total peripheral resistance from 51.98 to 61.64 and 77.0 mmHg/min/L at doses of 0.3 and 3.0 mg/kg i.v., respectively, while mean blood pressure fell from 118 to 98 and 77 mmHg, respectively.
In another anesthetized dog, reduced total peripheral resistance from 60.68 to 44.16 and 37.07 mmHg/min/L at doses of 0.3 and 3.0 mg/kg i.v., respectively, while mean blood pressure fell from 125 to 102 and 79 mmHg, respectively.
In anesthetized dogs after coronary ligation, increased stroke volume at 1.0 mg/kg i.v., and elevated mean blood pressure from 110 to 140 mmHg and increased total peripheral resistance by 80% at 10 mg/kg i.v.

Animal Model:

Pigs (anesthetized, open-chest, high background sympathetic activity)^[1]
Dosage:

1.0 mg/kg; 1.5 mg/kg
Administration:

i.v.; single dose
Result:

Induced dose-related falls in mean blood pressure, associated with bradycardia and reduced cardiac output.

Animal Model:

Either sex, 300-400 g (anaesthetized with pentobarbitone sodium, pithed, artificially ventilated)^[3]
Dosage:

0.72 μmol/kg; 3.6 μmol/kg; 18.0 μmol/kg
Administration:

i.v.; cumulative doses at 30-minute intervals
Result:

Caused dose-related sinus bradycardia, with mean heart rate depressions of -8.3%, -9.0%, and -15.0% from a control mean of 196 beats/min for the 0.72, 3.6, and 18.0 μmol/kg doses, respectively.
Progressively blocked the chronotropic responses to intravenous isoprenaline for the 0.72, 3.6, and 18.0 μmol/kg doses.
Induced dose-related increases in mean arterial blood pressure (MAP) to mean peaks of 69, 115, and 120 mmHg for the 0.72, 3.6, and 18.0 μmol/kg doses, respectively; baseline MAP rose progressively from 55 mmHg to 65, 68, and 75 mmHg at 10 minutes post-recovery from each dose.
Potentiated pressor responses to noradrenaline: in normally innervated rats, 0.72, 3.6, and 18.0 μmol/kg doses increased responses to 20 ng noradrenaline by 15%, 100%, and 146%, respectively, and increased responses to 50 ng noradrenaline by 9%, 64%, and 67%, respectively; this potentiation was attenuated in guanethidine-pretreated rats.
Did not reduce isoprenaline-induced hypotension at 0.72 and 3.6 μmol/kg doses, while the 18.0 μmol/kg dose caused a slight, non-significant attenuation.
Caused ECG changes including QRS widening, delayed repolarization, P-R interval lengthening, and induction of 2:1, 3:1, or 4:1 atrioventricular block, plus right or left bundle branch block.

Animal Model:

Dog (anaesthetized)^[3]
Dosage:

0.2 mg/kg; 0.6 mg/kg; 2.0 mg/kg; 6.0 mg/kg; 1.0 mg/kg; 10.0 mg/kg
Administration:

i.v.
Result:

Reduced heart rate by 20, 23, 22, and 16 beats/min respectively for intravenous doses of 0.2, 0.6, 2.0, and 6.0 mg/kg, with no dose-related bradycardia; mean blood pressure was reduced by 2, 2, 3, and 10 mmHg respectively.
Reduced tachycardic responses to 0.3 μg/kg i.v. isoprenaline by 70-80% with little effect on hypotensive responses at a 1.0 mg/kg i.v. dose.
Increased stroke volume in dogs after coronary ligation at a 1.0 mg/kg i.v. dose.
Raised mean blood pressure from 110 to 140 mmHg and increased total peripheral resistance by 80% at a 10.0 mg/kg i.v. dose.

Chemical Information

CAS. Nr. 59170-23-9
Appearance Solid
Molecular Weight 345.43
Formel C₂₀H₂₇NO₄
Color White to off-white
SMILES

OC(COC1=CC=CC(C)=C1)CNCCC2=CC=C(OC)C(OC)=C2
Synonyms

SOM3355 free base
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (289.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.8949 mL

14.4747 mL

28.9494 mL

5 mM

0.5790 mL

2.8949 mL

5.7899 mL

10 mM

0.2895 mL

1.4475 mL

2.8949 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.24 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (292 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Vaughan Williams EM, et al. Bevantolol: a beta-1 adrenoceptor antagonist with unique additional actions. Journal of clinical pharmacology. 1987 Jul;27(7):450-60. [Content Brief]

[2]. Gamez J, et al. A proof-of-concept study with SOM3355 (bevantolol hydrochloride) for reducing chorea in Huntington's disease. British journal of clinical pharmacology. 2023 May;89(5):1656-1664.

[3]. Dukes ID, et al. Cardiovascular effects of bevantolol, a selective beta 1-adrenoceptor antagonist with a novel pharmacological profile. British journal of pharmacology. 1985 Feb;84(2):365-80. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.8949 mL	14.4747 mL	28.9494 mL	72.3736 mL
	5 mM	0.5790 mL	2.8949 mL	5.7899 mL	14.4747 mL
	10 mM	0.2895 mL	1.4475 mL	2.8949 mL	7.2374 mL
	15 mM	0.1930 mL	0.9650 mL	1.9300 mL	4.8249 mL
	20 mM	0.1447 mL	0.7237 mL	1.4475 mL	3.6187 mL
	25 mM	0.1158 mL	0.5790 mL	1.1580 mL	2.8949 mL
	30 mM	0.0965 mL	0.4825 mL	0.9650 mL	2.4125 mL
	40 mM	0.0724 mL	0.3619 mL	0.7237 mL	1.8093 mL
	50 mM	0.0579 mL	0.2895 mL	0.5790 mL	1.4475 mL
	60 mM	0.0482 mL	0.2412 mL	0.4825 mL	1.2062 mL
	80 mM	0.0362 mL	0.1809 mL	0.3619 mL	0.9047 mL
	100 mM	0.0289 mL	0.1447 mL	0.2895 mL	0.7237 mL

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Bevantolol

Alle Adrenergic Receptor Isoform-spezifische Produkte anzeigen