2. Anti-infection Membrane Transporter/Ion Channel Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. Parasite Fungal Potassium Channel Reactive Oxygen Species (ROS)
  4. Halofantrine

Halofantrine  (Synonyms: SKF-102886 free base; WR-171669)

Cat. No.: HY-A0148
Handling Instructions Technical Support

Halofantrine (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 inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria.

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Halofantrine

Halofantrine Chemical Structure

CAS No. : 69756-53-2

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Halofantrine Related Antibodies

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Description

Halofantrine (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 inhibits the Cap1-dependent oxidative stress response of Candida albicans, suppresses ROS responses, and enhances the antifungal (Fungal) activity of oxidative damage agents. Halofantrine exhibits antifungal activity in the Galleria mellonella model, and shows antimalarial activity against Plasmodium strains both in vitro and in animal models. Halofantrine can be used in studies related to invasive candidiasis, falciparum malaria, and vivax malaria[1][2].

IC50 & Target

Plasmodium

 

Cellular Effect
Cell Line Type Value Description References
CHO IC50
1.9 μM
Compound: halofantrine
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
[PMID: 23812503]
In Vitro

Halofantrine (24-48 h) 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) 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 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) inhibits chloroquine-resistant Plasmodium falciparum in vitro, with an IC50 value of 1.3-3.9 μg/L[2].
Halofantrine (10 μM) 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.

Halofantrine Related Antibodies

Cell Viability Assay[3]

Cell Line: MDA-MB-231 TNBC
Concentration: 0, 2.50, 5.00, 10.00, 20.00, 40.00, and 80.00 μM
Incubation Time: 3 days
Result: IC50 was 7.73±0.23 μM.
In Vivo

Halofantrine (0-2 mg/kg; injection; single dose) 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) 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) 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
Molecular Weight

500.42

Formula

C26H30Cl2F3NO
CAS No.
SMILES

OC(CCN(CCCC)CCCC)C1=CC2=C(Cl)C=C(Cl)C=C2C3=CC(C(F)(F)F)=CC=C31
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Halofantrine Related Classifications

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

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Halofantrine69756-53-2SKF-102886 WR-171669SKF102886SKF 102886WR171669WR 171669WR-171669ParasiteFungalPotassium ChannelReactive Oxygen Species (ROS)KcsAantimalarial agentCandida albicansGalleria mellonellainvasive candidiasisfalciparum malariaand vivax malariaInhibitorinhibitorinhibit

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