CGP 20712 dihydrochloride
目录号 : GC15354
β1 antagonist,highly potent and selective
Cas No.:1216905-73-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >96.00% (HPLC)
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
CGP 20712 dihydrochloride is a potent and selective antagonist of β1-adrenoceptor with IC50 value of 0.7 nM [1].
β1-adrenoceptor is a G-protein coupled receptor and mediates uncoupling protein-1 (UCP1) gene expression induced by norepinephrine (NE) [2].
CGP 20712 dihydrochloride is a potent and selective β1-adrenoceptor antagonist. In neocortical membranes, CGP 20712 A exhibited affinity for β1-adrenoceptor and β2-adrenoceptor with IC50 values of 0.7 and 6700 nM, respectively [1]. In brown adipocytes, CGP-20712A significantly inhibited UCP1 gene expression induced by NE. However, CGP-20712A had no effect on lipolysis. These results suggested that β1-adrenoceptor mediated UCP1 gene expression [2]. In ventricular membranes from rats, CGP 20712A (300 nM) completely occupied its high-affinity binding sites. In ventricular myocytes isolated from rats, CGP 20712A (10, 100, 1000 nM) didn’t cause the activation of adenylate cyclase mediated by β2-adrenoceptors, which suggested that β2-adrenoceptors were not present on rat ventricular myocytes [3]. In adult rat cardiac myocytes, CGP 20712A inhibited β1-AR-stimulated apoptosis, which was mediated by a cAMP-dependent mechanism [4].
References:
[1]. Dooley DJ, Bittiger H, Reymann NC. CGP 20712 A: a useful tool for quantitating beta 1- and beta 2-adrenoceptors. Eur J Pharmacol, 1986, 130(1-2): 137-139.
[2]. Chaudhry A, Granneman JG. Differential regulation of functional responses by beta-adrenergic receptor subtypes in brown adipocytes. Am J Physiol, 1999, 277(1 Pt 2): R147-153.
[3]. Kitagawa Y, Adachi-Akahane S, Nagao T. Determination of beta-adrenoceptor subtype on rat isolated ventricular myocytes by use of highly selective beta-antagonists. Br J Pharmacol. 1995, 116(1): 1635-1643.
[4]. Communal C, Singh K, Sawyer DB, et al. Opposing effects of beta(1)- and beta(2)-adrenergic receptors on cardiac myocyte apoptosis : role of a pertussis toxin-sensitive G protein. Circulation, 1999, 100(22): 2210-2212.
| Cas No. | 1216905-73-5 | SDF | |
| 化学名 | 2-hydroxy-5-(2-((2-hydroxy-3-(4-(1-methyl-4-(trifluoromethyl)-1H-imidazol-2-yl)phenoxy)propyl)amino)ethoxy)benzimidic acid dihydrochloride | ||
| Canonical SMILES | CN(C(C1=CC=C(OCC(O)CNCCOC2=CC(C(O)=N)=C(O)C=C2)C=C1)=N3)C=C3C(F)(F)F.Cl.Cl | ||
| 分子式 | C23H25F3N4O5.2HCl | 分子量 | 567.39 |
| 溶解度 | ≥ 16.25mg/mL in Water | 储存条件 | Desiccate at +4°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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.7625 mL | 8.8123 mL | 17.6246 mL |
| 5 mM | 0.3525 mL | 1.7625 mL | 3.5249 mL |
| 10 mM | 0.1762 mL | 0.8812 mL | 1.7625 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。
3. 以上所有助溶剂都可在 GlpBio 网站选购。