CGP 12177 hydrochloride
目录号 : GC17717β1/β2-AR拮抗剂，β3 AR部分激动剂
Cas No.:64208-32-8
Sample solution is provided at 25 µL, 10mM.
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CGP 12177 hydrochloride is a partial agonist of β3-adrenoceptor and an antagonist of β1- and β2-adrenoceptors with Ki values of 0.9, 4 and 88 nM for β1-, β2- and β3-adrenoceptors, respectively.
β3-adrenoceptor is exists mainly in adipose tissue and plays an important role in the regulation of thermogenesis and lipolysis.
CGP 12177 hydrochloride is a partial agonist of β3-adrenoceptor and an antagonist of β1- and β2-adrenoceptors. In human ventricular myocytes (HVMs), CGP12177 slightly activated L-type Ca2+ current (ICa,L) [1].
In sympathectomized (SX) interscapular brown adipose tissue (BAT) isolated from rats, CGP-12177 restored normal thyroxine (T4) deiodination, which suggested that CGP-12177 activated 5’-deiodinase type II through β3-adrenoceptor [2]. In spontaneously hypertensive rats (SHR) and normotensive rats, CGP12177 induced vasorelaxant effects and decreased hindquarters
perfusion pressure in a dose-dependent way induced by 5-hydroxytryptamine (5-HT), which was inhibited by bupranolol, a β1LA-adrenoceptor antagonist. These results suggested that CGP12177 induced vasorelaxant effects through activation of β1LA-adrenoceptor [3].
References:
[1]. Treinys R, Zablockaitė D, Gendvilienė V, et al. β₃-Adrenergic regulation of L-type Ca²⁺ current and force of contraction in human ventricle. J Membr Biol, 2014, 247(4): 309-318.
[2]. Hofer D, Raíces M, Schauenstein K, et al. The in vivo effects of beta-3-receptor agonist CGP-12177 on thyroxine deiodination in cold-exposed, sympathectomized rat brown fat. Eur J Endocrinol, 2000, 143(2): 273-277.
[3]. Holopherne D, Mallem MY, Le Strat E, et al. CGP12177-induced haemodynamic and vascular effects in normotensive and hypertensive rats. Eur J Pharmacol, 2008, 591(1-3): 196-202.
| Cas No. | 64208-32-8 | SDF | |
| 化学名 | (R)-4-(3-(tert-butylamino)-2-hydroxypropoxy)-1H-benzo[d]imidazol-2(3H)-one hydrochloride | ||
| Canonical SMILES | O[C@@H](COC1=CC=CC(N2)=C1NC2=O)CNC(C)(C)C.Cl | ||
| 分子式 | C14H21N3O3.HCl | 分子量 | 315.8 |
| 溶解度 | Soluble to 50 mM in water | 储存条件 | Store at RT |
| 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 | 3.1666 mL | 15.8328 mL | 31.6656 mL |
| 5 mM | 0.6333 mL | 3.1666 mL | 6.3331 mL |
| 10 mM | 0.3167 mL | 1.5833 mL | 3.1666 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。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet