CAS NO: | 64208-32-8 |
包装 | 价格(元) |
50mg | 电议 |
10mg | 电议 |
Cas No. | 64208-32-8 |
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 | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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: |