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

Ranolazine

Synonyms: CVT 303, RS 43285-003

Ranolazine (CVT 303, RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.

Ranolazine Chemical Structure

Ranolazine Chemical Structure

CAS No. 95635-55-5

Purity & Quality Control

Ranolazine Related Products

Signaling Pathway

Calcium Channel Signaling Pathways

Calcium Channel Signaling Pathway

Biological Activity

Description Ranolazine (CVT 303, RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.
Targets
Calcium channel [1]
In vitro
In vitro

Ranolazine is found to bind more tightly to the inactivated state than the resting state of the sodium channel underlying I(NaL), with apparent dissociation constants K(dr)=7.47 mM and K(di)=1.71 mM, respectively. Ranolazine at 5 mM and 10 mM reversibly shortens the duration of TCs and abolishes the after contraction.[1] Ranolazine inhibits the late component of INa and attenuates prolongation of action potential duration when late INa is increased, both in the absence and presence of IK-blocking drugs. Ranolazine (10 mM) reduces by 89% the 13.6-fold increase in variability of APD caused by 10 nM ATX-II. [2]
In Vivo
In vivo

Ranolazine significantly and reversibly shortens the action potential duration (APD) of myocytes stimulated at either 0.5 or 0.25 Hz in a concentration-dependent manner in left ventricular myocytes of dogs. [1] Ranolazine (10 mM) significantly increases glucose oxidation 1.5-fold to 3-fold under conditions in which the contribution of glucose to overall ATP production is low (low Ca, high FA, with insulin), high (high Ca, low Fa, with pacing), or intermediate in working heart of rats. Ranolazine (10 mM) similarly increases glucose oxidation in normoxic Langendorff hearts (high Ca, low FA; 15 mL/min) of rats. Ranolazine significantly improves functional outcome in reperfused ischemic working hearts, which is associated with significant increases in glucose oxidation. [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 427.54 Formula

C24H33N3O4
CAS No. 95635-55-5 SDF Download Ranolazine SDF
Smiles CC1=C(C(=CC=C1)C)NC(=O)CN2CCN(CC2)CC(COC3=CC=CC=C3OC)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 86 mg/mL ( (201.15 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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.

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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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