Description
GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM.
Product information
CAS Number: 1010411-21-8
Molecular Weight: 428.78
Formula: C20H24Cl3N3O
Chemical Name: 2-[(tert-butylamino)methyl]-5-[(7-chloroquinolin-4-yl)amino]phenol dihydrochloride
Smiles: Cl.Cl.CC(C)(C)NCC1=CC=C(C=C1O)NC1=CC=NC2=CC(Cl)=CC=C21
InChiKey: UDVALKJFXQVZSI-UHFFFAOYSA-N
InChi: InChI=1S/C20H22ClN3O.2ClH/c1-20(2,3)23-12-13-4-6-15(11-19(13)25)24-17-8-9-22-18-10-14(21)5-7-16(17)18;;/h4-11,23,25H,12H2,1-3H3,(H,22,24);2*1H
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: DMSO : 100 mg/mL (233.22 mM; Need ultrasonic). H2O : 50 mg/mL (116.61 mM; Need ultrasonic).
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
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.
Products are for research use only. Not for human use.
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