| CAS NO: | 1216905-73-5 |
| 包装 | 价格(元) |
| 10mg | 电议 |
| 50mg | 电议 |
| Cas No. | 1216905-73-5 |
| 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 | Store at -20℃ |
| 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 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: |
m.cnreagent.com