Name: Ranolazine
Brand: Selleck Chemicals
SKU: S1799
Availability: InStock
Rating: 5 (2 reviews)

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Quality Control

Batch: Purity: 99.75%

99.75

Related Targets	CFTR CRM1 CD markers AChR Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR
Other Calcium Channel Inhibitors	Bay K 8644 Nilvadipine Flunarizine 2HCl Cilnidipine YM-58483 (BTP2) Imperatorin Manidipine 2HCl Astragaloside A Benidipine HCl Azelnidipine

Solubility

In vitro
Batch:

DMSO : 86 mg/mL (201.15 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 20 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.300mg/ml (10.06mM)	Taking the 1 mL working solution as an example, add 50 μL of 86 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.700mg/ml (1.64mM)	Taking the 1 mL working solution as an example, add 50 μL of 14 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	427.54	Formula	C₂₄H₃₃N₃O₄	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	95635-55-5	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	CVT 303, RS 43285-003			Smiles	CC1=C(C(=CC=C1)C)NC(=O)CN2CCN(CC2)CC(COC3=CC=CC=C3OC)O

Mechanism of Action

Targets/IC₅₀/Ki	Calcium channel
In vitro	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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/16686675/ [2] https://pubmed.ncbi.nlm.nih.gov/15243300/ [3] https://pubmed.ncbi.nlm.nih.gov/8616920/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT03486561	Unknown status	Chronic Stable Angina	OBS Pakistan	April 1 2018	Phase 4
NCT03044964	Unknown status	Angina	Amit Malhotra MD\|Gilead Sciences\|Stern Cardiovascular Foundation Inc.	January 10 2017	Phase 4
NCT02252406	Completed	Stable Angina\|Metabolic Syndrome	University of Florida	September 2015	Phase 4
NCT02360397	Completed	Ventricular Premature Complexes\|Myocardial Ischemia	Kent Hospital Rhode Island\|Gilead Sciences	December 2014	Phase 2
NCT02156336	Terminated	Diabetic Peripheral Neuropathic Pain	Horizons International Peripheral Group\|Gilead Sciences	May 2014	Phase 4

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Ranolazine Calcium Channel inhibitor

Chemical Structure

Molecular Weight: 427.54