Carazolol (Synonyms: BM 51052,(±)-Carazolol) |
Catalog No.GC13180 |
high-affinity, lipophilic, non-selective ligand of the β-adrenergic receptors
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 57775-29-8
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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.
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. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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