Carazolol
(Synonyms: 卡拉洛尔; (±)-Carazolol; DL-Carazolol; Suacron) 目录号 : GC13180A β-AR ligand
Cas No.:57775-29-8
Sample solution is provided at 25 µL, 10mM.
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 | |
别名 | 卡拉洛尔; (±)-Carazolol; DL-Carazolol; Suacron | ||
化学名 | 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 | ||
分子式 | C18H22N2O2 | 分子量 | 298.4 |
溶解度 | ≥ 14.8mg/mL in DMSO | 储存条件 | Store at -20°C |
General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。 储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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 |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
计算结果:
工作液浓度: mg/ml;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL,
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
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Quality Control & SDS
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- Purity: >98.00%
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