Ranolazine 2HCl

Catalog No.S1425 Synonyms: RS-43285

For research use only.

Ranolazine 2HCl (RS-43285) is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.

Ranolazine 2HCl Chemical Structure

CAS No. 95635-56-6

Selleck's Ranolazine 2HCl has been cited by 1 Publication

Purity & Quality Control

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Biological Activity

Description Ranolazine 2HCl (RS-43285) 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 (from reference)

Solubility (25°C)

In vitro

DMSO 100 mg/mL
(199.81 mM)
Water 100 mg/mL
(199.81 mM)
Ethanol Insoluble

Chemical Information

Molecular Weight 500.46
Formula

C24H33N3O4.2HCl

CAS No. 95635-56-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=C(C(=CC=C1)C)NC(=O)CN2CCN(CC2)CC(COC3=CC=CC=C3OC)O.Cl.Cl

In vivo Formulation Calculator (Clear solution)

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
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Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03486561 Unknown status Drug: Ranolazine Chronic Stable Angina OBS Pakistan April 1 2018 Phase 4
NCT03044964 Unknown status Drug: Ranolazine|Drug: Placebo Angina Amit Malhotra MD|Gilead Sciences|Stern Cardiovascular Foundation Inc. January 10 2017 Phase 4
NCT02252406 Completed Drug: Ranolazine|Other: Placebo Stable Angina|Metabolic Syndrome University of Florida September 2015 Phase 4
NCT02360397 Completed Drug: ranolazine Ventricular Premature Complexes|Myocardial Ischemia Kent Hospital Rhode Island|Gilead Sciences December 2014 Phase 2
NCT02156336 Terminated Drug: Ranolazine|Drug: Placebo Diabetic Peripheral Neuropathic Pain Horizons International Peripheral Group|Gilead Sciences May 2014 Phase 4

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

Handling Instructions

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