GSK369796 Dihydrochloride

SKU: orb1220550

Description

GSK369796 Dihydrochlorideis an anti-malaria drug candidate. is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization(IC50 of 7.5 μM)(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.(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.

Key Properties

• CAS Number: 1010411-21-8
• MW: 428.78
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₄Cl₃N₃O
• SMILES: Cl.Cl.CC(C)(C)NCc1ccc(Nc2ccnc3cc(Cl)ccc23)cc1O
• Target: Potassium Channel
• Solubility: DMSO:75 mg/mL (174.91 mM)

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

N-tert-butylisoquine

Quick Database Links

Gene Symbol

Potassium Channel