PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM).
| Cas No. | 128837-71-8 |
| Canonical SMILES | NC[C@@H]1CC[C@@H](C(N[C@@H](CC2=CC=CC=C2)C(NC3=CC=C(CC(O)=O)C=C3)=O)=O)CC1.Cl |
| 分子式 | C25H31N3O4•HCl |
| 分子量 | 474 |
| 溶解度 | Water: 10 mM |
| 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 | PKSI-527 is an inhibitor of plasma kallikrein (Ki = 0.81 μM). It is selective for plasma kallikrein over glandular kallikrein, plasmin, thrombin, urokinase, and Factor Xa (Kis = >500, 390, >500, 200, and >500 μM, respectively). PKSI-527 reduces bradykinin generation induced by kaolin and λ-carrageenan ex vivo in human plasma. It also prolongs partial thromboplastin and euglobulin clot lysis times. In vivo, PKSI-527 (300 mg/kg per day) reduces hyperplasia, pannus formation, and infiltration of inflammatory cells in the tarsal joint of mice with collagen-induced arthritis. |
