Cat. No.: HY-122537A

Arotinolol

2 Cited Publications

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Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker. Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to 5HT_1B-serotonergic receptor sites. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.

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Pureté: 99.93%
CAS No.: 68377-92-4
Formule: C₁₅H₂₁N₃O₂S₃
Masse moléculaire:371.54

Stockage:

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

Arotinolol Chemical Structure

CAS No.: 68377-92-4

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Activité biologique
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (2)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

Arotinolol is a nonselective α/β-adrenergic receptor blocker and a vasodilating β-blocker^[1]. Arotinolol also shows potency for inhibiting the binding of the radioligand ¹²⁵I-ICYP to 5HT_1B-serotonergic receptor sites^[2]. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases^[1].

IC₅₀ & Target^[2]

5-HT_1B Receptor

5-HT_2A Receptor

Voir tous les produits spécifiques à Isoform Adrenergic Receptor :

Voir tous les produits spécifiques à Isoform 5-HT Receptor :

In Vitro

Arotinolol shows its selectivity of β-adrenergic receptors, the result of Arotinolol for β1 and β2 adrenoceptors in ¹²⁵I-ICYP binding to rat cerebral cortical membranes with pK_i value of 9.74 and 9.26 respectively. The selectively of β1 and β2 is equal^[2].
Arotinolol shows its potency for inhibiting the binding of the same radioligand to 5HT1B-serotonergic receptor site, Arotinolol displaces ¹²⁵I-ICYP binding to 5HT1B-receptors with the pK_i values of 7.97 and 8.16 resepectively for β1 and β2 adrenergic receptors^[2].

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

In Vivo

Arotinolol (oral gavage; 200 mg/kg; 8 weeks) can significantly decrease central arterial pressure (CAP) and pulse wave velocity (PWV), in addition, it reduces aortic collagen depositions and finally improves arterial stiffness in SHR mouse^[1].

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

Animal Model:

SHR mice^[1]
Dosage:

200 mg/kg
Administration:

Orally gavage; 200 mg/kg; once daily; 8 weeks
Result:

Improved arterial stiffness in SHR.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 68377-92-4
Appearance Solid
Masse moléculaire 371.54
Formule C₁₅H₂₁N₃O₂S₃
Color Off-white to light yellow
SMILES

O=C(C1=CC=C(C2=CSC(SCC(O)CNC(C)(C)C)=N2)S1)N
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (2)

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ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576

Solvant et solubilité

In Vitro:

DMSO : 125 mg/mL (336.44 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

2.6915 mL

13.4575 mL

26.9150 mL

5 mM

0.5383 mL

2.6915 mL

5.3830 mL

10 mM

0.2692 mL

1.3458 mL

2.6915 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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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: ≥ 2.08 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (5.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (273 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)
Instruction de manipulation (2659 KB)

Références

[1]. Zhou W, et al. Mechanisms of improved aortic stiffness by arotinolol in spontaneously hypertensive rats.PLoS One. 2014 Feb 12;9(2):e88722. [Content Brief]

[2]. Hiroshi TSUCHIHASHI, et al. Characteristics of 1251-lodocyanopindolol Binding to 8-Adrenergic and Serotonin-1B Receptors of Rat Brain: Selectivity of 19-Adrenergic Agents

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	2.6915 mL	13.4575 mL	26.9150 mL	67.2875 mL
	5 mM	0.5383 mL	2.6915 mL	5.3830 mL	13.4575 mL
	10 mM	0.2692 mL	1.3458 mL	2.6915 mL	6.7288 mL
	15 mM	0.1794 mL	0.8972 mL	1.7943 mL	4.4858 mL
	20 mM	0.1346 mL	0.6729 mL	1.3458 mL	3.3644 mL
	25 mM	0.1077 mL	0.5383 mL	1.0766 mL	2.6915 mL
	30 mM	0.0897 mL	0.4486 mL	0.8972 mL	2.2429 mL
	40 mM	0.0673 mL	0.3364 mL	0.6729 mL	1.6822 mL
	50 mM	0.0538 mL	0.2692 mL	0.5383 mL	1.3458 mL
	60 mM	0.0449 mL	0.2243 mL	0.4486 mL	1.1215 mL
	80 mM	0.0336 mL	0.1682 mL	0.3364 mL	0.8411 mL
	100 mM	0.0269 mL	0.1346 mL	0.2692 mL	0.6729 mL

Keywords

Arotinolol

2 Cited Publications

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Arotinolol

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Publications Citing Use of MedChemExpress (MCE) Arotinolol

Voir tous les produits spécifiques à Isoform Adrenergic Receptor

Voir tous les produits spécifiques à Isoform 5-HT Receptor

Activité biologique

Chemical Information

Publications (2)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Arotinolol Related Classifications

HY-122537A Related Classifications