1. Membrane Transporter/Ion Channel
    Anti-infection
  2. Potassium Channel
    Parasite
  3. GSK369796 Dihydrochloride

GSK369796 Dihydrochloride 

Cat. No.: HY-12082A Purity: 99.94%
Handling Instructions

GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM.

For research use only. We do not sell to patients.

GSK369796 Dihydrochloride Chemical Structure

GSK369796 Dihydrochloride Chemical Structure

CAS No. : 1010411-21-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 181 In-stock
Estimated Time of Arrival: December 31
2 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 192 In-stock
Estimated Time of Arrival: December 31
10 mg USD 264 In-stock
Estimated Time of Arrival: December 31
50 mg USD 792 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1320 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products
  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM.

IC50 & Target

IC50: 7.5 μM (hERG potassium ion channel)[1]

In Vitro

In vitro, GSK369796 Dihydrochloride can inhibit the growth of Plasmodium falciparum strains 3D7c, HB3c and K1d, with IC50s of 11.2±2.2, 12.6±5.3 and 13.2±3.2 nM, respectively. Protein binding is higher for GSK369796 Dihydrochloride (compound 4) compare to desethyl amodiaquine in the mouse (93 vs 74%) but similar in human (88 vs 86%). GSK369796 Dihydrochloride can also inhibit hERG potassium ion channel repolarization with an IC50 of 7.5±0.8 μM[1].

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

In Vivo

In vivo, GSK369796 Dihydrochloride can inhibit the growth of Plasmodium berghei ANKA with ED50 and ED90 of 2.8 and 4.7 mg/kg, respectively[1].

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

Clinical Trial
Molecular Weight

428.78

Formula

C₂₀H₂₄Cl₃N₃O

CAS No.

1010411-21-8

SMILES

OC1=CC(NC2=CC=NC3=CC(Cl)=CC=C23)=CC=C1CNC(C)(C)C.[H]Cl.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (233.22 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3322 mL 11.6610 mL 23.3220 mL
5 mM 0.4664 mL 2.3322 mL 4.6644 mL
10 mM 0.2332 mL 1.1661 mL 2.3322 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (5.83 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

Assays are performed in sterile 96-well microtiter plates, each plate contains 200 mL of parasite culture (2% parasitemia, 0.5% hematocrit) with or without 10 mL drug dilutions (including GSK369796 Dihydrochloride). Each drug is tested in triplicate and parasite growth is compared to control wells (which constitutes 100% parasite growth). Cultures are incubated for a further 24 h before they are harvested onto filter mats, dried for 1 h at 55 °C, and counted. IC50 values are calculated[1].

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

Animal Administration
[1]

The efficacy of selected 4-aminoquinolines (including GSK369796 Dihydrochloride) is measured against P. yoelii or P. berghei in a 4-day test. 28 Cohorts of age-matched female mice are infected iv with 6.4×106 or 10.0×106 parasites obtained from infected donors, and the mice are randomly distributed in groups of n=5 mice/group (day 0). Treatments are administered from day 0 (one hour after infection) until day 3. The therapeutic efficacy of compounds (including GSK369796 Dihydrochloride) is expressed as the effective dose that reduces parasitemia by 50% (ED50) and 90% (ED90) with respect to vehicle treated groups (ED90) and the dose that achieved eradication of parasitemia until day 23 after infection (NRL). All compounds (including GSK369796 Dihydrochloride) and corresponding vehicles are administered orally at 20 mg/kg or subcutaneously at 10 mg/kg, as appropriate[1].

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

GSK369796GSK 369796GSK-369796Potassium ChannelParasiteKcsAInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

 

Salutation

Applicant Name *

 

Email address *

Phone number *

 

Organization name *

Department *

 

Requested quantity *

Country or Region *

     

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
GSK369796 Dihydrochloride
Cat. No.:
HY-12082A
Quantity:
MCE Japan Authorized Agent: