Ranolazine

Catalog No.S1799 Synonyms: CVT 303, RS 43285-003

Ranolazine  Chemical Structure

Molecular Weight(MW): 427.54

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

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 120 In stock
USD 210 In stock
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Biological Activity

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

Protocol

Solubility (25°C)

In vitro DMSO 86 mg/mL (201.15 mM)
Ethanol 20 mg/mL (46.77 mM)
Water 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 427.54
Formula

C24H33N3O4

CAS No. 95635-55-5
Storage powder
Synonyms CVT 303, RS 43285-003

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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

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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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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID