Ranolazine 2HCl
Catalog No.S1425 Synonyms: RS-43285
Molecular Weight(MW): 500.46
Ranolazine 2HCl is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.
Purity & Quality Control
Choose Selective Calcium Channel Inhibitors
Biological Activity
| Description | Ranolazine 2HCl is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina. | |
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| In vitro |
Ranolazine selectively inhibits late I(Na), reduces [Na(+)](i)-dependent calcium overload and attenuates the abnormalities of ventricular repolarisation and contractility that are associated with ischaemia/reperfusion and heart failure in myocardial cells. [1] Ranolazine significantly and reversibly shortens the action potential duration (APD) of myocytes stimulated at either 0.5 Hz or 0.25 Hz in a concentration-dependent manner in left ventricular myocytes of dogs. Ranolazine at 5 and 10 mM reversibly shortens the duration of twitch contractions (TC) and abolished the after contraction. Ranolazine is found to bind more tightly to the inactivated state than the resting state of the sodium channel underlying I(NaL). [2] |
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| In vivo | Ranolazine (10 mM) significantly increases glucose oxidation 1.5-fold to 3-fold under conditions in which the contribution of glucoseto overall ATP production is low (low Ca, high FA, with insulin), high (high Ca, low Fa, with pacing), or intermediate in working hearts. Ranolazine similarly increases glucose oxidation in normoxic Langendorff hearts (high Ca, low FA; 15 mL/min). Ranolazine also significantly increases it during flow reduction to 7 mL/min, 3 mL/min, and 0.5 mL/min. Ranolazine significantly improves functional outcome, which is associated with significant increases in glucoseoxidation, a reversal of the increased FA oxidation seen in control reperfusions (versus preischemic), and a smaller but significant increase in glycolysis in reperfuse dischemic working hearts. [3] |
Protocol
Solubility (25°C)
| In vitro | DMSO | 100 mg/mL (199.81 mM) |
|---|---|---|
| Water | 100 mg/mL (199.81 mM) | |
| Ethanol | Insoluble |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 500.46 |
|---|---|
| Formula | C24H33N3O4.2HCl |
| CAS No. | 95635-56-6 |
| Storage | powder |
| Synonyms | RS-43285 |
Bio Calculators
Molarity Calculator
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Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02687269 | Not yet recruiting | Myocardial Stunning | Policlinico Universitario Agostino Gemelli | October 2016 | Phase 4 |
| NCT02829034 | Recruiting | Pulmonary Hypertension | University of Pennsylvania|Brigham and Womens Hospital|University of Maryland|Gilead Sciences | July 2016 | -- |
| NCT02817932 | Recruiting | Healthy Male Individuals | A.Menarini Asia-Pacific Holdings Pte Ltd | March 2016 | Phase 1 |
| NCT02653833 | Recruiting | Muscular Dystrophy | Cedars-Sinai Medical Center | December 2015 | Early Phase 1 |
| NCT02611596 | Not yet recruiting | Silent Myocardial Ischemia|Type 2 Diabetes | Walter Reed National Military Medical Center | November 2015 | -- |
| NCT02252406 | Recruiting | Stable Angina|Metabolic Syndrome | University of Florida | September 2015 | Phase 4 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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