Ranolazine 2HCl

Catalog No.S1425 Synonyms: RS-43285

Ranolazine 2HCl Chemical Structure

Molecular Weight(MW): 500.46

Ranolazine 2HCl is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 120 In stock
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Biological Activity

Description Ranolazine 2HCl is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.
Targets
Calcium channel [1]
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]

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
in solvent
Synonyms RS-43285

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03162120 Withdrawn Atrial Fibrillation|Recurrence Elpen Pharmaceutical Co. Inc. September 1 2018 Phase 2|Phase 3
NCT03162120 Withdrawn Atrial Fibrillation|Recurrence Elpen Pharmaceutical Co. Inc. September 1 2018 Phase 2|Phase 3
NCT03472950 Recruiting ALS University of Kansas Medical Center|Gilead Sciences June 11 2018 Phase 2
NCT03401502 Not yet recruiting Angina TSH Biopharm Corporation Limited June 2018 Not Applicable
NCT03472950 Recruiting ALS University of Kansas Medical Center|Gilead Sciences June 11 2018 Phase 2
NCT03401502 Not yet recruiting Angina TSH Biopharm Corporation Limited June 2018 Not Applicable

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID