Art. -Nr.: HY-A0148A

Halofantrine hydrochloride

(Synonyms: SKF-102886; WR-171669 hydrochloride)

2 Cited Publications

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Based on 2 publication(s) in Google Scholar

Halofantrine hydrochloride (SKF-102886 hydrochloride; WR-171669 hydrochloride) is a blocker that delays the delayed rectifier potassium current by inhibiting human ERG channels, and it is a potent antimalarial agent with oral activity. Halofantrine hydrochloride inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine hydrochloride exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine hydrochloride can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria.

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Reinheit: 99.9%
CAS. Nr.: 36167-63-2
Formel: C₂₆H₃₁Cl₃F₃NO
Molecular Weight:536.88

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Halofantrine hydrochloride Chemical Structure

CAS. Nr.: 36167-63-2

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (2)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

Plasmodium

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In Vitro

Halofantrine (24-48 h) hydrochloride acts synergistically with oxidative damage agents Plumbagin (HY-N1497), menadione, and H₂O₂ against Candida albicans strains SC5314 and SN152, with FICI values of 0.0938, 0.1563, and 0.2526, respectively^[1].
The combination of halofantrine (24 h) hydrochloride and H₂O₂ retains synergistic activity against Candida albicans hog1Δ/Δ and rad53Δ/Δ strains (with FICI values of 0.5 and 0.2813, respectively), but shows no synergistic activity against cap1Δ/Δ, ybp1Δ/Δ or gpx3Δ/Δ strains when combined with H₂O₂, indicating that its oxidative stress inhibitory effect depends on the Cap1-Ybp1 pathway^[1].
Halofantrine hydrochloride inhibits chloroquine (HY-17589A)-sensitive Plasmodium falciparum in vitro, with an IC₅₀ value of 1.5-2.5 μg/L^[2].
Halofantrine (1.3-3.9 μg/L) hydrochloride inhibits chloroquine-resistant Plasmodium falciparum in vitro, with an IC₅₀ value of 1.3-3.9 μg/L^[2].
Halofantrine (10 μM) hydrochloride inhibits glucose-dependent proton efflux in Plasmodium berghei-infected mouse erythrocytes at a concentration of 10 μmol/L in vitro^[2].
Halofantrine inhibits Plasmodium falciparum in vitro, with an ID₅₀ of 4.0 μg/L^[2].

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

In Vivo

Halofantrine (0-2 mg/kg; injection; single dose) hydrochloride reduces the mortality rate of Galleria mellonella larvae infected with Candida albicans to 40% during an 8-day observation period^[1].
Halofantrine (10-640 mg/kg; s.c.; p.o.; daily; single dose) hydrochloride exhibits potent in vivo antimalarial activity in mice infected with Plasmodium berghei, but shows poor oral bioavailability at doses up to 640 mg/kg^[2].
Halofantrine (35-140 mg/kg; p.o.; 7-day regimen; single dose) hydrochloride alleviates Plasmodium falciparum infection in Aotus monkeys^[2].

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

Animal Model:

larvae (average weight 300 mg; inoculated with Candida albicans SN152)^[1]
Dosage:

0.5 mg/kg; 1 mg/kg; 2 mg/kg
Administration:

injection; single dose
Result:

Reduced larval mortality to 40% at 2 mg/kg over 8 days.

Animal Model:

Mice^[2]
Dosage:

10-640 mg/kg
Administration:

s.c.; single dose; p.o.; single dose; daily
Result:

Exhibited potent in vivo antimalarial activity in mice infected with Plasmodium berghei, but showed poor oral bioavailability at doses up to 640 mg/kg

Animal Model:

Aotus monkeys^[2]
Dosage:

35-140 mg/kg
Administration:

p.o.; 7-day regimen; single dose
Result:

Alleviated Plasmodium falciparum infection in Aotus monkeys

Chemical Information

CAS. Nr. 36167-63-2
Appearance Solid
Molecular Weight 536.88
Formel C₂₆H₃₁Cl₃F₃NO
Color White to off-white
SMILES

OC(CCN(CCCC)CCCC)C1=CC2=C(Cl)C=C(Cl)C=C2C3=CC(C(F)(F)F)=CC=C31.[H]Cl
Synonyms

SKF-102886; WR-171669 hydrochloride
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Publications (2)

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Journal Impact Factor

Nat Mater

Drinkable in situ-forming tough hydrogels for gastrointestinal therapeutics. [Abstract]

2024 Sep;23(9):1292-1299. PMID: 38413810
bioRxiv

2022 Dec 19.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 30 mg/mL (55.88 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

1.8626 mL

9.3131 mL

18.6261 mL

5 mM

0.3725 mL

1.8626 mL

3.7252 mL

10 mM

0.1863 mL

0.9313 mL

1.8626 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 (sealed storage, away from moisture). 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 90% Corn Oil

Solubility: ≥ 3 mg/mL (5.59 mM); Clear solution

This protocol yields a clear solution of ≥ 3 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 (30.0 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 (280 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]. Xiong J, et al. Halofantrine Hydrochloride Acts as an Antioxidant Ability Inhibitor That Enhances Oxidative Stress Damage to Candida albicans. Antioxidants (Basel). 2024 Feb 9;13(2):223. [Content Brief]

[2]. Bryson HM, et al. Halofantrine. A review of its antimalarial activity, pharmacokinetic properties and therapeutic potential. Drugs. 1992 Feb;43(2):236-58. [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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.8626 mL	9.3131 mL	18.6261 mL	46.5653 mL
	5 mM	0.3725 mL	1.8626 mL	3.7252 mL	9.3131 mL
	10 mM	0.1863 mL	0.9313 mL	1.8626 mL	4.6565 mL
	15 mM	0.1242 mL	0.6209 mL	1.2417 mL	3.1044 mL
	20 mM	0.0931 mL	0.4657 mL	0.9313 mL	2.3283 mL
	25 mM	0.0745 mL	0.3725 mL	0.7450 mL	1.8626 mL
	30 mM	0.0621 mL	0.3104 mL	0.6209 mL	1.5522 mL
	40 mM	0.0466 mL	0.2328 mL	0.4657 mL	1.1641 mL
	50 mM	0.0373 mL	0.1863 mL	0.3725 mL	0.9313 mL

Halofantrine hydrochloride

2 Cited Publications

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Halofantrine hydrochloride

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Publications Citing Use of MedChemExpress (MCE) Halofantrine hydrochloride

Alle Parasite Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (2)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Halofantrine hydrochloride Related Classifications

Art. -Nr.: HY-A0148A