西洛布雷定是一种 HCN 通道阻滞剂；神经元 Ih 和相关心脏 If 通道的开放通道阻滞剂。
| Cas No. | 186097-54-1 |
| 别名 | 西洛雷定盐酸盐,DK-AH 269 |
| 化学名 | 3-[[(3S)-1-[2-(3,4-dimethoxyphenyl)ethyl]-3-piperidinyl]methyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-2H-3-benzazepin-2-one, monohydrochloride |
| Canonical SMILES | COC1=CC=C(CCN2CC(CN(CCC(C=C(OC)C(OC)=C3)=C3C4)C4=O)CCC2)C=C1OC.Cl |
| 分子式 | C28H38N2O5.HCl |
| 分子量 | 519.1 |
| 溶解度 | DMF: 3 mg/ml,DMSO: 3 mg/ml,Ethanol: 0.5 mg/ml,PBS (pH 7.2): 2 mg/ml |
| 储存条件 | Store at -20°C |
| 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 | DK-AH 269 (Cilobradine) is an HCN Channel blocker; an open channel blocker of neuronal Ih and related cardiac If channels.
Target: HCN Channel blocker
DK-AH 269 is a HCN channel blocker that is about 3 times more potent than ZD7288. At a concentration of 10 μM, DK-AH 269 inhibits WT mHCN2 channel current by 86 ± 2% (n = 5). In contrast, I432A and A425G channel currents were only reduced by 14 ± 1% (n = 4) and 19 ± 2% (n = 8), respectively, by this concentration of DK-AH 269. The double mutant (I432A/A425G) channel was even less sensitive to 10 μM DK-AH 269 (8 ± 2% inhibition; n = 4). References
[1]. Cheng L, et al. Molecular mapping of the binding site for a blocker of hyperpolarization-activated, cyclic nucleotide-modulated pacemaker channels. J Pharmacol Exp Ther. 2007 Sep;322(3):931-939. |
