Revizinone (R80122) 是一种新型选择性磷酸二酯酶 (PDE) 抑制剂,该酶的 IC50 值为 0.036 microM。
Cas No. | 133718-29-3 |
别名 | 瑞维齐农,R80122 |
Canonical SMILES | O=C(N(C1CCCCC1)C)CO/N=C(C2=CC=CC=C2)/C3=CC4=C(N=C(NC(C5)=O)N5C4)C=C3.[(E)] |
分子式 | C26H29N5O3 |
分子量 | 459.54 |
溶解度 | DMSO : ≥ 4.6 mg/mL (10.01 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 | Revizinone is a novel selective phosphodiesterase (PDE) inhibitor with IC50 values on this enzyme to 0.036 microM. target: phosphodiesterase (PDE)[3]; IC 50: 0.036 microM; [3]In vivo: The administration of Revizinone improved the haemodynamic profile with an increase in cardiac output, a decrease in systemic vascular resistance and a stable heart rate and mean arterial blood pressure. [1] With regard to reconstitution of contractility and cardiac function Revizinone (E-isomer) was 10 fold more potent than R 79595 and nearly 100 fold more potent than R 80123 (Z-isomer). [2] Revizinone significantly increased global LV function and systolic wall thickening in ischemic areas at doses greater than or equal to 0.16 mg/kg i.v. [4] [1]. Herregods L et al. Haemodynamic effects of R 80122 immediately after cardiopulmonary bypass; preliminary results. Anaesthesia. 1994 Aug;49(8):719-22. [2]. Schneider J et al. Cardiac effects of R 79595 and its isomers (R 80122 and R 80123) in an acute heart failure model. A new class of cardiotonic agents with highly selective phosphodiesterase III inhibitory properties. Naunyn Schmiedebergs Arch Pharmacol. 1992 Nov;346(5):563-72. [3]. de Cheffoy de Courcelles D et al. Inhibition of human cardiac cyclic AMP-phosphodiesterases by R 80122, a new selective cyclic AMP-phosphodiesterase III inhibitor: a comparison with other cardiotonic compounds. J Pharmacol Exp Ther. 1992 Oct;263(1):6-14. [4]. Vandeplassche GM et al. Comparative effects of R 80122, enoximone, and milrinone on left ventricular phosphodiesterase isoenzymes in vitro and on contractility of normal and stunned myocardium in vivo in dogs. J Cardiovasc Pharmacol. 1992 May;19(5):714-22. |