[CAS NO. 133718-29-3] Revizinone
PRODUCTS SPECIFICATIONS [133718-29-3]
DESCRIPTION [133718-29-3]
Overview
| MDL | MFCD00867129 |
|---|---|
| Molecular Weight | 459.54 |
| Molecular Formula | C26H29N5O3 |
| 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)] |
Summary
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]
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 4.6 mg/mL ( 10.01 mM )
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.1761 mL | 10.8804 mL | 21.7609 mL |
| 5 mM | 0.4352 mL | 2.1761 mL | 4.3522 mL |
| 10 mM | 0.2176 mL | 1.0880 mL | 2.1761 mL |
References
- [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
- [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
