N-(2,6-dimethylphenyl)-2-(4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)piperazin-1-yl)acetamide
Ranolazine
CAS: 95635-55-5;142387-99-3
Molecular Formula: C24H33N3O4
N-(2,6-dimethylphenyl)-2-(4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)piperazin-1-yl)acetamide - Names and Identifiers
N-(2,6-dimethylphenyl)-2-(4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)piperazin-1-yl)acetamide - Physico-chemical Properties
| Molecular Formula | C24H33N3O4 |
| Molar Mass | 427.54 |
| Density | 1.174±0.06 g/cm3(Predicted) |
| Melting Point | 119-1200C |
| Boling Point | 624.1±55.0 °C(Predicted) |
| Flash Point | 331.2°C |
| Solubility | DMSO 86 mg/mL Water <1 mg/mL Ethanol 20 mg/mL |
| Vapor Presure | 1.94E-16mmHg at 25°C |
| Appearance | Solid |
| Color | White |
| pKa | 14.06±0.20(Predicted) |
| Storage Condition | Sealed in dry,Room Temperature |
| Refractive Index | 1.585 |
| Use | New anti-angina drug |
| In vitro study | Ranolazine was found to bind more tightly to sodium channels in the inactive rather than resting state, with apparent dissociation constants of K(DR)= 7.47 mM and K(DI)= 1.71 mM, respectively. Ranolazine at 5 mM and 10 mM reversibly shortens the duration of TC and abolishes contractions. In late sodium increases, Ranolazine inhibits the late component of the sodium current, and attenuates the prolongation of the action potential duration, both in the absence and presence of IK-blocking drugs. Ranolazine(10 mM) reduced the 13.6-fold induced increase in APD variability induced by 89% ATX-Ⅱ at 10 nM. |
| In vivo study | In dog left ventricular myocytes, Ranolazine significantly and reversibly shortened the action potential duration (APD) of myocytes stimulated at 0.5 or 0.25Hz in a concentration-dependent manner. In working rat hearts, Ranolazine(10 mM) significantly increased 1.5-fold to 3-fold under conditions of glucose oxidation, in which the contribution of the overall ATP production of glucose was low (low calcium, high FA, insulin), contribution High (high calcium, low FA, with pacing), or intermediate. In the Langendorff hearts of normoxic rats, Ranolazine(10 mM) similarly increased glucose oxidation (high calcium, low FA;15 mL/min). Ranolazine significantly improved the function of the Reperfused ischemic working heart, which was associated with a significant increase in glucose oxidation function. |
N-(2,6-dimethylphenyl)-2-(4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)piperazin-1-yl)acetamide - Risk and Safety
| HS Code | 2933595960 |
N-(2,6-dimethylphenyl)-2-(4-(2-hydroxy-3-(2-methoxyphenoxy)propyl)piperazin-1-yl)acetamide - Reference Information
| drugs for chronic angina pectoris | ranolazine is a drug for treating chronic angina pectoris, which can reduce the occurrence of arrhythmia, including ventricular arrhythmia, new-onset arterial fibrillation, bradycardia due to coronary artery disease. The mechanism of action is to partially inhibit fatty acid metabolism, and cause the induction of glucose metabolism, because glucose metabolism is more effective than fatty acid metabolism, promote the heart to use oxygen more effectively, thereby significantly improve the symptoms of patients with angina pectoris. |
| biological activity | Ranolazine (CVT 303, RS 43285-003) is an inhibitor of calcium uptake by sodium/calcium channel anti-anginal drug used in the treatment of chronic angina pectoris. |
| Target | Value |
| Use | new anti-angina drug |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 20:45:29
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