Ranolazine 2HCl (RS-43285; CVT-303)

Alias: RS-43285; RS43285; RS 43285; CVT 303; CVT303; CVT-303; Ranolazine; Ranexa; Latixa; Ranolazine Dihydrochloride; Ranolazine Hydrochloride; Ranolazine HCl; .
Cat No.:V0368 Purity: ≥98%
Ranolazine 2HCl (known also as Ranolazine diHydrochloride), the diHCl salt of ranolzaine (RS43285; CVT303),is aan anti-angina drug which acts as a potent calcium uptake inhibitor via the sodium/calcium channel, it isused to treat chronic angina.
Ranolazine 2HCl (RS-43285; CVT-303) Chemical Structure CAS No.: 95635-56-6
Product category: Calcium Channel
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
250mg
500mg
1g
2g
5g
Other Sizes

Other Forms of Ranolazine 2HCl (RS-43285; CVT-303):

  • Ranolazine-d8 dihydrochloride (CVT 303-dd8 dihydrochloride; RS 43285-d8)
  • Ranolazine (CVT303, RS43285-003; Ranexa)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ranolazine 2HCl (known also as Ranolazine diHydrochloride), the diHCl salt of ranolzaine (RS43285; CVT303), is a an anti-angina drug which acts as a potent calcium uptake inhibitor via the sodium/calcium channel, it is used to treat chronic angina. Ranolazine is an anti-ischemic agent that inhibits late sodium current that results in a reduction of Na+ dependent Ca2+ overload. Ranolazine can cause the shift of ATP production towards glucose oxidation, which is due to the fact that more oxygen is required to phosphorylate the same amount of ATP during fatty acid oxidation than carbohydrate oxidation. These studies indicate that Ranolazine also inhibits oxygen consumption and ketogenesis by fatty acids in liver cells.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: Ranolazine selectively inhibits late I(Na), reduces [Na(+)](i)-dependent calcium overload and attenuates the abnormalities of ventricular repolarisation and contractility that are associated with ischaemia/reperfusion and heart failure in myocardial cells. Ranolazine significantly and reversibly shortens the action potential duration (APD) of myocytes stimulated at either 0.5 Hz or 0.25 Hz in a concentration-dependent manner in left ventricular myocytes of dogs. Ranolazine at 5 and 10 mM reversibly shortens the duration of twitch contractions (TC) and abolished the after contraction. Ranolazine is found to bind more tightly to the inactivated state than the resting state of the sodium channel underlying I(NaL).

ln Vivo
In rats undergoing left anterior descending coronary artery occlusion-reperfusion, ranolazine (bolus injection 10 mg/kg and infusion 9.6 mg/kg/h; bolus injection; for 145 minutes; male Wistar rats) therapy dramatically lowers infarct size and cardiac troponin T release [3].
Animal Protocol
Animal/Disease Models: Male Wistar rats (240-350 g)[3]
Doses: Bolus injection 10 mg/kg and infusion (9.6 mg/kg/h)
Route of Administration: Bolus injection; for 145 minutes
Experimental Results: Dramatically decreased infarct size and cardiac troponin T release in rats subjected to left anterior descending coronary artery occlusion-reperfusion.
References
[1]. Keating GM. Ranolazine: A Review of Its Use as Add-On Therapy in Patients with Chronic Stable Angina Pectoris. Drugs. 2013 Jan;73(1):55-73.
[2]. Wang WQ, Robertson C, Dhalla AK, Belardinelli L. 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. 2008 Jun;325(3):875-81. doi: 10.1124/jpet.108.137729. Epub 2008 Mar 5.
[3]. Zacharowski K, Blackburn B, Thiemermann C. Ranolazine, a partial fatty acid oxidation inhibitor, reduces myocardial infarct size and cardiac troponin T release in the rat. Eur J Pharmacol. 2001 Apr 20;418(1-2):105-10.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C24H33N3O4.2HCL
Molecular Weight
500.46
CAS #
95635-56-6
SMILES
Cl[H].Cl[H].O([H])C([H])(C([H])([H])OC1=C([H])C([H])=C([H])C([H])=C1OC([H])([H])[H])C([H])([H])N1C([H])([H])C([H])([H])N(C([H])([H])C(N([H])C2C(C([H])([H])[H])=C([H])C([H])=C([H])C=2C([H])([H])[H])=O)C([H])([H])C1([H])[H]
Synonyms
RS-43285; RS43285; RS 43285; CVT 303; CVT303; CVT-303; Ranolazine; Ranexa; Latixa; Ranolazine Dihydrochloride; Ranolazine Hydrochloride; Ranolazine HCl; .
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO:100 mg/mL (199.8 mM)
Water:100 mg/mL (199.8 mM)
Ethanol:<1 mg/mL
Solubility (In Vivo)

Chemical Name:N-(2,6-dimethylphenyl)-2-[4-[2-hydroxy-3-(2-methoxyphenoxy)propyl]piperazin-1-yl]acetamide dihydrochloride

InChi Key:RJNSNFZXAZXOFX-UHFFFAOYSA-N

InChi Code:InChI=1S/C24H33N3O4.2ClH/c1-18-7-6-8-19(2)24(18)25-23(29)16-27-13-11-26(12-14-27)15-20(28)17-31-22-10-5-4-9-21(22)30-3;;/h4-10,20,28H,11-17H2,1-3H3,(H,25,29);2*1H

SMILES Code:O=C(NC1=C(C)C=CC=C1C)CN2CCN(CC(O)COC3=CC=CC=C3OC)CC2.[H]Cl.[H]Cl

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.9982 mL 9.9908 mL 19.9816 mL
5 mM 0.3996 mL 1.9982 mL 3.9963 mL
10 mM 0.1998 mL 0.9991 mL 1.9982 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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