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Submit ReviewRanolazine dihydrochloride is an antianginal agent with antiarrhythmic properties that acts as a partial fatty acid oxidation inhibitor. Activates pyruvate dehydrogenase in ischemic myocytes to promote glucose oxidation, switching substrate utilization from fatty acids to glucose. Also shown to inhibit late INa and IKr currents.
Ranolazine dihydrochloride is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
M. Wt | 500.46 |
Formula | C24H33N3O4.2HCl |
Storage | Desiccate at RT |
Purity | ≥98% (HPLC) |
CAS Number | 95635-56-6 |
PubChem ID | 71279 |
InChI Key | RJNSNFZXAZXOFX-UHFFFAOYSA-N |
Smiles | COC1=CC=CC=C1OCC(CN2CCN(CC(NC3=C(C)C=CC=C3C)=O)CC2)O.Cl.Cl |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
water | 50.05 | 100 | |
DMSO | 50.05 | 100 |
The following data is based on the product molecular weight 500.46. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 2 mL | 9.99 mL | 19.98 mL |
5 mM | 0.4 mL | 2 mL | 4 mL |
10 mM | 0.2 mL | 1 mL | 2 mL |
50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
References are publications that support the biological activity of the product.
Zacharowski et al (2001) Ranolazine, a partial fatty acid oxidation inhibitor, reduces myocardial infarct size and cardiac troponin T release in the rat. Eur.J.Pharmacol. 418 105 PMID: 11334871
Shryock and Belardinelli (2008) Inhibition of late sodium current to reduce electrical and mechanical dysfunction of ischaemic myocardium. Br.J.Pharmacol. 153 1128 PMID: 18071302
Wang et al (2008) Antitorsadogenic effects of (+/-)-N-(2,6-dimethyl-phenyl)-4[2-hydroxy-3-(2-methoxyphenoxy)propyl]-1-piperazine (ranolazine) in anesthetized rabbits. J.Pharmacol.Exp.Ther. 325 875 PMID: 18322148
If you know of a relevant reference for Ranolazine dihydrochloride, please let us know.
Keywords: Ranolazine dihydrochloride, Ranolazine dihydrochloride supplier, Anti-anginal, activates, pyruvate, dehydrogenase, anti-arrhythmic, agent, activators, Enzyme, Substrates, RS43285, RS, 43285, Other, Dehydrogenases, /, Activators, Miscellaneous, Compounds, 3118, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Ranolazine dihydrochloride include:
McKeithan et al (2017) An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes. Front Physiol 8 766 PMID: 29075196
Park et al (2013) Slowly inactivating component of Na+ current in peri-somatic region of hippocampal CA1 pyramidal neurons. J Neurophysiol 109 1378 PMID: 23236005
Carstensen et al (2019) Effects of UK 68798 and RS 43285 on atrial fibrillatory rate in a horse model of acutely induced atrial fibrillation. J Cardiovasc Electrophysiol 30 596 PMID: 30661267
Do you know of a great paper that uses Ranolazine dihydrochloride from Tocris? Please let us know.
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Guinea pig ventricular cardiomyocytes were treated (12-16 h) with HOCl-LDL (250 µg/ml). Cells were patched and stimulated at a frequency of 1 Hz. Representative action potentials (shown in Image) recorded in the same cell are shown before (A) and after (B) superfusion with Ranolazine (10 µM, 5 min). For comparative purpose representative APs of a control cardiomyocyte are shown (C).
Application of Ranolazine on acute brain slices to verify for fatty acid oxidation involvement in studied process. It had the same effect as etomoxir (CPT1 blocker), as expected per hypothesis.
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