| Description | Cathepsin Inhibitor 1 is an inhibitor of Cathepsin (L, L2, S, K, B) with pIC50 of 7.9, 6.7, 6.0, 5.5 and 5.2, respectively. |
| In vivo | Ciproxifan通过静脉注射，剂量为1 mg/kg，能够降低雄性瑞士小鼠血清中的H3受体配体浓度，分布相和消除相的半衰期分别为13分钟和87分钟。Ciproxifan（1 mg/kg, p.o.）能迅速提高雄性瑞士小鼠大脑中t-MeHA的水平，在30分钟后显著增加，90至180分钟间达到高峰，270分钟后仍然保持增高。在雄性Wistar大鼠中，Ciproxifan导致大脑皮层、纹状体和下丘脑的ED50值分别为0.23 mg/kg、0.28 mg/kg和0.30 mg/kg。Ciproxifan（3 mg/kg, i.p.）显著提高了在短暂刺激持续时间的五选一任务中的选择准确性。Ciproxifan（0.15-2 mg/kg, p.o.）在猫中诱导明显的新皮层电脑图激活迹象，表现为快速节律密度增强和几乎完全的清醒状态。[1] Ciproxifan（10 mg/kg, i.p.）增强了DBA/2品系小鼠的预脉冲抑制。[3] Ciproxifan（3 mg/kg, i.p.）减轻了阿尔茨海默病模型小鼠APP Tg2576的过动和认知缺陷。[4] Ciproxifan（3 mg/kg, i.p.）提高了成年雄性hooded Lister大鼠的准确性并降低了冲动性。[5] |
| Target activity | Cathepsin L2:6.7(pIC50), Cathepsin B:5.2(pIC50), Cathepsin S:6(pIC50), Cathepsin K:5.5(pIC50), Cathepsin L:7.9(pIC50) |
| molecular weight | 401.89 |
| Molecular formula | C20H24ClN5O2 |
| CAS | 225120-65-0 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility | DMSO: 74 mg/mL (184.1 mM) Ethanol: 47 mg/mL (116.9 mM) H2O: < 1 mg/mL (insoluble or slightly soluble) |
| References | 1. Asaad N, et al. Bioorg Med Chem Lett, 2009, 19(15), 4280-4283. |