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

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

Cat. No.: HY-A0148A Purity: 99.9%
COA
SDS
Handling Instructions Technical Support

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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Halofantrine hydrochloride

Halofantrine hydrochloride Chemical Structure

CAS No. : 36167-63-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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Based on 2 publication(s) in Google Scholar

Other Forms of Halofantrine hydrochloride:

Halofantrine hydrochloride Related Antibodies

Top Publications Citing Use of Products

2 Publications Citing Use of MCE Halofantrine hydrochloride

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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[1][2].

IC50 & Target

Plasmodium

 

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.

Halofantrine hydrochloride Related Antibodies
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
Molecular Weight

536.88

Formula

C26H31Cl3F3NO
CAS No.
Appearance

Solid

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

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

Solvent & Solubility
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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8626 mL 9.3131 mL 18.6261 mL
5 mM 0.3725 mL 1.8626 mL 3.7252 mL
View the Complete Stock Solution Preparation Table

* 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.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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

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

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

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

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.9%

SDS (393 KB)

COA (251 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* 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.

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
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Halofantrine hydrochloride Related Classifications

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:

Halofantrine36167-63-2SKF-102886WR-171669SKF102886SKF 102886WR171669WR 171669ParasiteFungalReactive Oxygen Species (ROS)Potassium ChannelKcsAantimalarial agentCandida albicansGalleria mellonellainvasive candidiasisfalciparum malariaand vivax malariaInhibitorinhibitorinhibit

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