Home Transmembrane Transporters Calcium Channel inhibitor Ranolazine 2HCl For research use only.

Ranolazine 2HCl

Synonyms: RS-43285,RS 43285-193,Ranexa, renolazine,Ranolazine dihydrochloride

Ranolazine 2HCl (RS-43285,RS 43285-193,Ranexa, renolazine,Ranolazine dihydrochloride) is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.

Ranolazine 2HCl Chemical Structure

Ranolazine 2HCl Chemical Structure

CAS No. 95635-56-6

Purity & Quality Control

Ranolazine 2HCl Related Products

Signaling Pathway

Calcium Channel Signaling Pathways

Calcium Channel Signaling Pathway

Biological Activity

Description Ranolazine 2HCl (RS-43285,RS 43285-193,Ranexa, renolazine,Ranolazine dihydrochloride) is a calcium uptake inhibitor via the sodium/calcium channal, used to treat chronic angina.
Targets
Calcium channel [1]
In vitro
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
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]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03486561 Unknown status
Chronic Stable Angina
OBS Pakistan
 April 1 2018 Phase 4
NCT03044964 Unknown status
Angina
Amit Malhotra MD|Gilead Sciences|Stern Cardiovascular Foundation Inc.
 January 10 2017 Phase 4
NCT02252406 Completed
Stable Angina|Metabolic Syndrome
University of Florida
 September 2015 Phase 4
NCT02360397 Completed
Ventricular Premature Complexes|Myocardial Ischemia
Kent Hospital Rhode Island|Gilead Sciences
 December 2014 Phase 2
NCT02156336 Terminated
Diabetic Peripheral Neuropathic Pain
Horizons International Peripheral Group|Gilead Sciences
 May 2014 Phase 4

Chemical Information & Solubility

Molecular Weight 500.46 Formula

C24H33N3O4.2HCl
CAS No. 95635-56-6 SDF Download Ranolazine 2HCl SDF
Smiles CC1=C(C(=CC=C1)C)NC(=O)CN2CCN(CC2)CC(COC3=CC=CC=C3OC)O.Cl.Cl
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 100 mg/mL ( (199.81 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : Insoluble


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In vivo
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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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