2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor 5-HT Receptor
  4. Arotinolol

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. Arotinolol is an antihypertensive agent for the treatment of a variety of cardiovascular pathologies as well as non-cardiovascular diseases.

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Arotinolol Chemical Structure

Arotinolol Chemical Structure

CAS No. : 68377-92-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 55 In-stock
Solution
10 mM * 1 mL in DMSO USD 55 In-stock
Solid
5 mg USD 50 In-stock
10 mg USD 75 In-stock
25 mg USD 130 In-stock
50 mg USD 195 In-stock
100 mg USD 275 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Arotinolol:

Arotinolol Related Antibodies

Top Publications Citing Use of Products

View All Adrenergic Receptor Isoform Specific Products:

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α adrenergic receptor β adrenergic receptor

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5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor 5-HT Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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 5HT1B-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-HT2A 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 pKi 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 pKi 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.

Arotinolol Related Antibodies
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.
Clinical Trial
Molecular Weight

371.54

Formula

C15H21N3O2S3
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6915 mL 13.4575 mL 26.9150 mL
5 mM 0.5383 mL 2.6915 mL 5.3830 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Volume
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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V2

In Vivo:

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

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.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • 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.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.93%

COA (245 KB) HNMR (255 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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Arotinolol Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Arotinolol68377-92-4Adrenergic Receptor5-HT ReceptorBeta ReceptorSerotonin Receptor5-hydroxytryptamine Receptorhypertensionheart failuremyocardial infarctionischemic cardiac eventInhibitorinhibitorinhibit

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