1. GPCR/G Protein
    Neuronal Signaling
  2. Adenosine Receptor
    5-HT Receptor
  3. Arotinolol

Arotinolol 

Cat. No.: HY-122537A
Handling Instructions

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.

For research use only. We do not sell to patients.

Arotinolol Chemical Structure

Arotinolol Chemical Structure

CAS No. : 68377-92-4

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 74 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 330 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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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].

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].

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.
Molecular Weight

371.54

Formula

C₁₅H₂₁N₃O₂S₃

CAS No.

68377-92-4

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

Please store the product under the recommended conditions in the Certificate of Analysis.

Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (672.88 mM; Need ultrasonic)

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
10 mM 0.2692 mL 1.3458 mL 2.6915 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

ArotinololAdenosine Receptor5-HT ReceptorP1 receptorSerotonin Receptor5-hydroxytryptamine Receptorhypertensionheart failuremyocardial infarctionischemic cardiac eventInhibitorinhibitorinhibit

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Arotinolol
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