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Carazolol (Synonyms: BM 51052,(±)-Carazolol)

Catalog No.GC13180

high-affinity, lipophilic, non-selective ligand of the β-adrenergic receptors

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Carazolol Chemical Structure

Cas No.: 57775-29-8

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Sample solution is provided at 25 µL, 10mM.

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Background

Carazolol is a high-affinity, lipophilic, and non-selective ligand of the β-adrenergic receptors [1,2].

β-adrenergic receptors have been involved in mediating the physiological responses of the catecholamines, epinephrine and norepinephrine and modulating a myriad of physiological functions, such as relaxation of smooth muscle, chronotropic and inotropic cardiac responses, and lipolysis in adipose tissue. The β-adrenergic receptors exist in nearly all mammalian tissues. Until now, three β-adrenergic receptors have been identified, β1-, β2- and β3-adrenergic receptors [3].

In CHO cells expressing the human β3-adrenoceptor, the Ki value of carazolol was 2.0 ± 0.2 and the IC50 was 11.3 ± 1.2 nM. Carazolol exhibited an ECs0 of 25 nM and behaved as a full agonist (intrinsic activity = 0.97) towards the murine β3-adrenoceptor. In murine 3T3-F442A-derived adipocytes express the β3-adrenoceptor, carazolol stimulated lipolysis [1]. Carazolol bound to cortical β-receptors with a Kd value of 0.15 nM. Carazolol showed equal displacements constants when binding with calf cerebral cortex (which contained mainly β1 receptors) and calf cerebellum (which contained mainly β2 receptors), indicating that carazolol bound with equal affinity to β1 and β2 receptors [2].

References:
[1] Méjean A, Guillaume J L, Strosberg A D.  Carazolol: a potent, selective β3-adrenoceptor agonist[J]. European Journal of Pharmacology: Molecular Pharmacology, 1995, 291(3): 359-366.
[2] Innis R B, Corrêa F M A, Snyder S H.  Carazolol, an extremely potent β-adrenergic blocker: Binding to β-receptors in brain membranes [J]. Life sciences, 1979, 24(24): 2255-2264.
[3] Pellegrino S M, Lee N H, Fraser C M.  β-Adrenergic receptors[J]. Biomembranes: A Multi-Volume Treatise, 1996, 2: 245-279.

Chemical Properties

Cas No. 57775-29-8 SDF
Synonyms BM 51052,(±)-Carazolol
Chemical Name 1-(9H-carbazol-4-yloxy)-3-[(1-methylethyl)amino]-2-propanol
Canonical SMILES OC(CNC(C)C)COC1=C(C(C=CC=C2)=C2N3)C3=CC=C1
Formula C18H22N2O2 M.Wt 298.4
Solubility ≥ 14.8mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 3.3512 mL 16.756 mL 33.5121 mL
5 mM 0.6702 mL 3.3512 mL 6.7024 mL
10 mM 0.3351 mL 1.6756 mL 3.3512 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 39 reference(s) in Google Scholar.)

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