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Ranolazine

Catalog No. T6633 CAS 95635-55-5

Synonyms: CVT 303, Ranexa, RS 43285-003

Ranolazine (RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina. It affects the sodium-dependent calcium channels during myocardial ischemia in rabbits by altering the intracellular sodium level.

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Ranolazine, CAS 95635-55-5

Pack Size	Availability	Price/USD
50 mg	In stock	$ 57.00
100 mg	In stock	$ 81.00
200 mg	In stock	$ 125.00
500 mg	In stock	$ 212.00
1 mL * 10 mM (in DMSO)	In stock	$ 50.00

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Purity: 98.2%

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Description	Ranolazine (RS 43285-003) is a calcium uptake inhibitor via the sodium/calcium channel, used to treat chronic angina. It affects the sodium-dependent calcium channels during myocardial ischemia in rabbits by altering the intracellular sodium level.
Targets&IC50	INa:6 μM (IC50), IKr:12 μM (IC50)
In vitro	In the absence and presence of IK-blocking drugs, when late INa is increased, Ranolazine inhibits the late component of INa and attenuates prolongation of action potential duration. Ranolazine (10 mM) reduces by 89% of the 13.6-fold increase in variability of APD caused by 10 nM ATX-II. 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（5 mM and 10 mM） reversibly shortens the duration of TCs and abolishes the after contraction.
In vivo	In dog left ventricular myocytes, Ranolazine significantly and reversibly stimulate the action potential duration (APD) of shortened myocytes at 0.5 or 0.25 Hz in a concentration-dependent manner. In rat hearts, Ranolazine (10 mM) significantly increased 1.5-fold to 3-fold under glucose oxidation conditions. Ranolazine (10 mM) also increased glucose oxidation (high calcium, low FA; 15 ml/min) in Langendorff hearts in normoxic rats. Ranolazine significantly improves the function of the reperfused ischemic working heart, which is associated with a significant increase in glucose oxidation function.
Kinase Assay	In vitro kinase assay for CDK1 and Aurora kinases:CDK1 kinase activity is tested by the CDK1/cyclin B complex purified from baculovirus to phosphorylate a biotinylated peptide substrate containing the consensus phosphorylation site for histone H1, which is phosphorylated in vivo by CDK1. Inhibition of CDK1 activity is measured by observing a decreased amount of 33P-γ-ATP incorporation into the immobilized substrate in streptavidin-coated 96-well scintillating microplates. CDK1 enzyme is diluted in 50 mM Tris-HCl (pH 8), 10 mM MgCl2, 0.1 mM Na3VO4, 1 mM DTT, 1% DMSO, 0.25 μM peptide, 0.1 μCi per well 33P-γ-ATP, and 5 μM ATP in the presence or absence of various concentrations of JNJ-7706621 and incubated at 30 °C for 1 hour. The reaction is terminated by washing with PBS containing 100 mM EDTA and plates are counted in a scintillation counter. IC50 is determined by Linear regression analysis of the percent inhibition by JNJ-7706621.The Aurora kinase activity is measured with 10 μM ATP and a peptide containing a dual repeat of the kemptide phosphorylation motif.

Synonyms	CVT 303, Ranexa, RS 43285-003
Molecular Weight	427.54
Formula	C24H33N3O4
CAS No.	95635-55-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 16 mg/mL (37.4 mM)

DMSO: 80 mg/mL (187.1 mM)

References and Literature

1. Undrovinas AI, et al. J Cardiovasc Electrophysiol,2006, 17 Suppl 1, S169-S177. 2. Song Y, et al. J Cardiovasc Pharmacol,2004, 44(2), 192-199. 3. Baptista T, et al. Circulation,1996, 93(1), 135-142.

Citations

1. Lenaeus M, Gamal El-Din T M, Tonggu L, et al.Structural basis for inhibition of the cardiac sodium channel by the atypical antiarrhythmic drug ranolazine.Nature Cardiovascular Research.2023: 1-8.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library EMA Approved Drug Library Anti-Diabetic Compound Library Bioactive Compounds Library Max Anti-COVID-19 Compound Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Ranolazine 95635-55-5 Membrane transporter/Ion channel Metabolism Sodium Channel Calcium Channel CVT303 Na+ channels Ca2+ channels inhibit CVT-303 CVT 303 Inhibitor Ranexa RS 43285-003 Na channels Ca channels inhibitor

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