Olprinone (Loprinone) 是一种有效的磷酸二酯酶(PDE) 3抑制剂，对 PDE1，PDE2，PDE3，PDE4 的IC50分别为 150、100、0.35 和 14 μM。Olprinone 因其正性肌力和血管扩张作用而被用于心力衰竭的研究。Olprinone 具有抗炎活性。
| 生物活性 | Olprinone (Loprinone) is a potentphosphodiesterase (PDE)3inhibitor, withIC50s of 150, 100, 0.35 and 14 μM forPDE1,PDE2,PDE3andPDE4, respectively. Olprinone is used for the research of heart failure due to its positive inotropic and vasodilative effects. Anti-inflammatory activity[1][2]. |
| IC50& Target[1] | PDE1 150 μM (IC50) | PDE2 100 μM (IC50) | PDE3 0.35 μM (IC50) | PDE4 14 μM (IC50) |
|
体内研究
(In Vivo) | Olprinone (Loprinone) (0.2 mg/kg; i.p.) modulates the inflammation associated with myocardial ischemia-reperfusion injury in rats[1].
| Animal Model: | Male adult Wistar rats (250-300 g) (ischemia–reperfusion rats)[1] | | Dosage: | 0.2 mg/kg | | Administration: | I.p. (administered 15 min after ischemia) | | Result: | Significantly reduced the: (1) histological evidence of myocardial injury, (2) pro-inflammatory cytokines: tumor necrosis factor-α (TNF-α) and Interleukin-1β (IL-1β), (3) adhesion molecules: Inter-Cellular Adhesion Molecule 1 (ICAM-1) and P-Selectin, (4) nitrotyrosine formation, (5) nuclear factor kappa-B (NF-κB) expression, (6) Poly (ADP-ribose) (PAR) formation, and (7) apoptosis (Bax, Bcl-2, Fas-L and terminal deoxynucleotidyl transferase-mediated UTP end labeling (TUNEL). |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
m.cnreagent.com