Art. -Nr.: HY-111529

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Tafenoquine

(Synonyms: WR 238605)

4 Cited Publications

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Based on 4 publication(s) in Google Scholar

Tafenoquine (WR 238605) is an 8-aminoquinoline. Tafenoquine is an anti-malarial prophylactic agent.

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Reinheit: 99.77%
CAS. Nr.: 106635-80-7
Formel: C₂₄H₂₈F₃N₃O₃
Molecular Weight:463.49

Speicherung:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tafenoquine Chemical Structure

CAS. Nr.: 106635-80-7

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vivo
- Clinical Trial
Chemical Information
Publications (4)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Tafenoquine (WR 238605) is an 8-aminoquinoline. Tafenoquine is an anti-malarial prophylactic agent^[1].

IC₅₀ & Target

Anti-malarial^[1]

Alle Parasite Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HepG2	IC₅₀	<1 μM Compound: Tafenoquine	Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin Antimalarial activity against sporozoite stage of Plasmodium yoelii assessed as invasion of human HepG2 cells expressing CD81 incubated for 2 hrs prior to inoculation measured after 1 hr by immunofluorescence assay in presence of penicillin/streptomycin	[PMID: 23927658]
RAW264.7	IC₅₀	5.9 μg/mL Compound: 3, TQ	Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay Cytotoxicity against mouse RAW264.7 cells after 24 hrs by MTT assay	[PMID: 21141892]

In Vivo

Tafenoquine exhibits no anti-malarial activity in CYP 2D knock-out mice when dosed at their ED₁₀₀ values (3 mg/kg) established in WT mice. Tafenoquine anti-malarial activity is partially restored in humanized/CYP 2D6 knock-in mice when tested at two times its ED₁₀₀ (6 mg/kg)^[1].

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

Clinical Trial

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

Chemical Information

CAS. Nr. 106635-80-7
Appearance Solid
Molecular Weight 463.49
Formel C₂₄H₂₈F₃N₃O₃
Color Light yellow to light brown
SMILES

CC1=CC(OC)=NC2=C1C(OC3=CC=CC(C(F)(F)F)=C3)=C(OC)C=C2NC(CCCN)C
Synonyms

WR 238605
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

Publications (4)

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mSystems

Repurposing of the antimalarial agent tafenoquine to combat MRSA. [Abstract]

2023 Dec 21;8(6):e0102623. PMID: 38047647
J Appl Microbiol

Insights into the antimicrobial effects of tafenoquine against enterococcus and its biofilms. [Abstract]

2024 Jan 2;135(1):lxae001. PMID: 38178639
Cell Physiol Biochem

Stimulation of Suicidal Erythrocyte Death by Tafenoquine. [Abstract]

2016;39(6):2464-2476. PMID: 27855400
Heliyon

Proteins extracted from pearl oyster (Pinctada martensii) with efficient accelerated wound healing in vitro through promoting cell proliferation, migration, and collagen formation. [Abstract]

2024 Jan 6;10(1):e24239. PMID: 38234916

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (215.75 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

2.1575 mL

10.7877 mL

21.5754 mL

5 mM

0.4315 mL

2.1575 mL

4.3151 mL

10 mM

0.2158 mL

1.0788 mL

2.1575 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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: ≥ 2.5 mg/mL (5.39 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.

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 (271 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)
- Korean - KR (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]. Marcsisin SR, et al. Tafenoquine and NPC-1161B require CYP 2D metabolism for anti-malarial activity: implications for the 8-aminoquinoline class of anti-malarial compounds. Malar J. 2014 Jan 3;13:2. [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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1575 mL	10.7877 mL	21.5754 mL	53.9386 mL
	5 mM	0.4315 mL	2.1575 mL	4.3151 mL	10.7877 mL
	10 mM	0.2158 mL	1.0788 mL	2.1575 mL	5.3939 mL
	15 mM	0.1438 mL	0.7192 mL	1.4384 mL	3.5959 mL
	20 mM	0.1079 mL	0.5394 mL	1.0788 mL	2.6969 mL
	25 mM	0.0863 mL	0.4315 mL	0.8630 mL	2.1575 mL
	30 mM	0.0719 mL	0.3596 mL	0.7192 mL	1.7980 mL
	40 mM	0.0539 mL	0.2697 mL	0.5394 mL	1.3485 mL
	50 mM	0.0432 mL	0.2158 mL	0.4315 mL	1.0788 mL
	60 mM	0.0360 mL	0.1798 mL	0.3596 mL	0.8990 mL
	80 mM	0.0270 mL	0.1348 mL	0.2697 mL	0.6742 mL
	100 mM	0.0216 mL	0.1079 mL	0.2158 mL	0.5394 mL

Keywords

Tafenoquine

4 Cited Publications

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Tafenoquine

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Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Tafenoquine

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tafenoquine

Anti-Infection Compound Library

FDA-Approved Drug Library

Drug Repurposing Compound Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Antiparasitic Compound library

Rare Diseases Drug Library

Human Metabolite Library

Heterocyclic Compound Library

Off-patent Drug Library

Mitochondrial Toxicity Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Tafenoquine

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (4)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tafenoquine Related Classifications

HY-111529 Related Classifications