For research use only.
Catalog No.S1799 Synonyms: CVT 303, RS 43285-003
CAS No. 95635-55-5
Ranolazine (CVT 303, RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.
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Choose Selective Calcium Channel Inhibitors
|Description||Ranolazine (CVT 303, RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina.|
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. 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. 
|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.  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. |
|In vitro||DMSO||86 mg/mL (201.15 mM)|
* 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.
|Synonyms||CVT 303, RS 43285-003|
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|Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)|
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Method for preparing DMSO master liquid: ： mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL，)
Method for preparing in vivo formulation：Take DMSO master liquid, next addμL PEG300， mix and clarify, next addμL Tween 80，mix and clarify, next add μL ddH2O，mix and clarify.
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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|
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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