Art. -Nr.: HY-B0280

Ranolazine

(Synonyms: CVT 303; RS 43285-003)

5 Cited Publications

Kundenbewertung

Based on 5 publication(s) in Google Scholar

Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (I_Na and I_Kr with IC₅₀ values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP). Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor. Antianginal agent.

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Reinheit: 99.57%
CAS. Nr.: 95635-55-5
Formel: C₂₄H₃₃N₃O₄
Molecular Weight:427.54

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ranolazine Chemical Structure

CAS. Nr.: 95635-55-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

Ranolazine (CVT 303) is an anti-angina drug that achieves its effects by inhibiting the late phase of inward sodium current (I_Na and I_Kr with IC₅₀ values of 6 μM and 12 μM, respectively) without affecting heart rate or blood pressure (BP)^[1]^[2]. Ranolazine is also a partial fatty acid oxidation (FAO) inhibitor^[3]. Antianginal agent.

IC₅₀ & Target

IC50: 6 μM (I_Na), 12 μM (I_Kr)^[1]

Alle Sodium Channel Isoform-spezifische Produkte anzeigen :

Alle Calcium Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Ventricular myocyte	IC₅₀	6.9 μM Compound: 1	Inhibition of Nav1.5 in canine ventricular myocytes assessed as inhibition of ATX2-induced late sodium current by single cell manual patch clamp assay Inhibition of Nav1.5 in canine ventricular myocytes assessed as inhibition of ATX2-induced late sodium current by single cell manual patch clamp assay	[PMID: 27038498]
Ventricular myocyte	IC₅₀	6.9 μM Compound: 1	Inhibition of canine ventricular myocytes Nav 1.5 assessed as reduction in ATX-2 induced late channel current by manual single-patch clamp assay Inhibition of canine ventricular myocytes Nav 1.5 assessed as reduction in ATX-2 induced late channel current by manual single-patch clamp assay	[PMID: 27080178]
Vero C1008	EC₅₀	>40 μM Compound: Ranolazine	Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days	10.1101/2020.04.03.023846

In Vivo

Ranolazine (Bolus injection 10 mg/kg and infusion 9.6 mg/kg/h; bolus injection; for 145 minutes; male Wistar rats) treatment significantly reduces infarct size and cardiac troponin T release in rats subjected to left anterior descending coronary artery occlusion-reperfusion^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male Wistar rats (240-350 g)^[3]
Dosage:

Bolus injection 10 mg/kg and infusion (9.6 mg/kg/h)
Administration:

Bolus injection; for 145 minutes
Result:

Significantly reduced infarct size and cardiac troponin T release in rats subjected to left anterior descending coronary artery occlusion-reperfusion.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 95635-55-5
Appearance Solid
Molecular Weight 427.54
Formel C₂₄H₃₃N₃O₄
Color White to off-white
SMILES

O=C(NC1=C(C)C=CC=C1C)CN2CCN(CC(O)COC3=CC=CC=C3OC)CC2
Synonyms

CVT 303; RS 43285-003
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (5)

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Journal Impact Factor

Cancer Res

KRAS Signaling Inhibition Induces a Targetable Metabolic Dependency on Lipophagy-Dependent Fatty Acid Oxidation in Pancreatic Cancer. [Abstract]

2026 Apr 29:10.1158/0008-5472.CAN-24-1984. PMID: 42054558
Theranostics

Adipocytes fuel gastric cancer omental metastasis via PITPNC1-mediated fatty acid metabolic reprogramming. [Abstract]

2018 Oct 29;8(19):5452-5468. PMID: 30555557

Ranolazine purchased from MedChemExpress. Usage Cited in: Theranostics. 2018 Oct 29;8(19):5452-5468. [Abstract]

Western Blot analysis of vector or PITPNC1 overexpressing BGC823 and AGS which are seeded and treated with Ranolazine.
J Invest Dermatol

The regulators of peroxisomal acyl-carnitine shuttle CROT and CRAT promote metastasis in melanoma. [Abstract]

2023 Feb;143(2):305-316.e5. PMID: 36058299
Pharmaceutics

Drug-Induced Reorganisation of Lipid Metabolism Limits the Therapeutic Efficacy of Ponatinib in Glioma Stem Cells. [Abstract]

2024 May 29;16(6):728. PMID: 38931850
Philos Trans R Soc Lond B Biol Sci

Late sodium current in synergism with Ca2+/calmodulin-dependent protein kinase II contributes to β-adrenergic activation-induced atrial fibrillation. [Abstract]

2023 Jun 19;378(1879):20220163. PMID: 37122215

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (233.90 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3390 mL

11.6948 mL

23.3896 mL

5 mM

0.4678 mL

2.3390 mL

4.6779 mL

10 mM

0.2339 mL

1.1695 mL

2.3390 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (4.87 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

[2]. Wang WQ, et al. 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. [Content Brief]

[3]. Zacharowski K, et al. 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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3390 mL	11.6948 mL	23.3896 mL	58.4741 mL
	5 mM	0.4678 mL	2.3390 mL	4.6779 mL	11.6948 mL
	10 mM	0.2339 mL	1.1695 mL	2.3390 mL	5.8474 mL
	15 mM	0.1559 mL	0.7797 mL	1.5593 mL	3.8983 mL
	20 mM	0.1169 mL	0.5847 mL	1.1695 mL	2.9237 mL
	25 mM	0.0936 mL	0.4678 mL	0.9356 mL	2.3390 mL
	30 mM	0.0780 mL	0.3898 mL	0.7797 mL	1.9491 mL
	40 mM	0.0585 mL	0.2924 mL	0.5847 mL	1.4619 mL
	50 mM	0.0468 mL	0.2339 mL	0.4678 mL	1.1695 mL
	60 mM	0.0390 mL	0.1949 mL	0.3898 mL	0.9746 mL
	80 mM	0.0292 mL	0.1462 mL	0.2924 mL	0.7309 mL
	100 mM	0.0234 mL	0.1169 mL	0.2339 mL	0.5847 mL

Keywords

Ranolazine

5 Cited Publications

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Ranolazine

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Publications Citing Use of MedChemExpress (MCE) Ranolazine

Alle Sodium Channel Isoform-spezifische Produkte anzeigen

Alle Calcium Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (5)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ranolazine Related Classifications

Art. -Nr.: HY-B0280