Catalog No.S1799 Synonyms: CVT 303, RS 43285-003
Molecular Weight(MW): 427.54
Ranolazine 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 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)|
|Ethanol||20 mg/mL (46.77 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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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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