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Arotinolol

Name: Arotinolol
Brand: TargetMol
SKU: T10371
Rating: 4.5 (1 reviews)

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Catalog No. T10371Cas No. 68377-92-4

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 [5HT1B-serotonergic] receptor sites. It is an antihypertensive agent.

Arotinolol

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Catalog No. T10371Cas No. 68377-92-4

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Product Introduction

Bioactivity

Description	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 [5HT1B-serotonergic] receptor sites. It is an antihypertensive agent.
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 pKi value of 9.74 and 9.26 respectively. Arotinolol shows its potency for inhibiting the binding of the same radioligand to the 5HT1B-serotonergic receptor site, Arotinolol displaces 125I-ICYP binding to 5HT1B-receptors (pKis: 7.97 and 8.16 for β1 and β2 adrenergic receptors) [2].
In vivo	Arotinolol (oral gavage; 200 mg/kg; 8 weeks) significantly decreases central arterial pressure (CAP) and pulse wave velocity (PWV), reduces aortic collagen depositions, and improves arterial stiffness in SHR mouse [1].

Chemical Properties

Molecular Weight	371.54
Formula	C₁₅H₂₁N₃O₂S₃
Cas No.	68377-92-4
Smiles	CC(C)(C)NCC(O)CSc1nc(cs1)-c1ccc(s1)C(N)=O
Relative Density.	1.35 g/cm3

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 250 mg/mL (672.88 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (8.88 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.6915 mL	13.4575 mL	26.9150 mL	134.5750 mL
5 mM	0.5383 mL	2.6915 mL	5.3830 mL	26.9150 mL
10 mM	0.2692 mL	1.3458 mL	2.6915 mL	13.4575 mL
20 mM	0.1346 mL	0.6729 mL	1.3458 mL	6.7288 mL
50 mM	0.0538 mL	0.2692 mL	0.5383 mL	2.6915 mL
100 mM	0.0269 mL	0.1346 mL	0.2692 mL	1.3458 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc