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GSK369796 2HCl

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Chemical Structure| 1010411-21-8 同义名 : GSK369796 (hydrochloride);GSK369796 Dihydrochloride;N-tert-butylisoquine;GSK369796
CAS号 : 1010411-21-8
货号 : A984981
分子式 : C20H24Cl3N3O
纯度 : 99%+
分子量 : 428.783
MDL号 : MFCD16627991
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 105 mg/mL(244.88 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 50 mg/mL(116.61 mM),配合低频超声助溶

动物实验配方:
生物活性
描述 GSK369796 Dihydrochloride is an effective antimalarial. GSK369796 Dihydrochloride can also inhibit hERG potassium ion channel repolarization with an IC50 of 7.5±0.8 μM. 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. 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]. GSK369796 has high anti-DENV activity in the DENV2 replicon expressing cells with EC50 value of 5.06 ± 0.86 μM. The infectivity assays revealed the EC50 value of 3.03 ± 0.35 μM. Moreover, GSK369796 also showed antiviral activity against the rapidly emerging Zika virus (ZIKV) with EC50 value of 2.57 ± 0.09 μM[2].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.66mL

2.33mL

1.17mL

23.32mL

4.66mL

2.33mL

参考文献

[1]O'Neill PM, Park BK, Shone AE, Maggs JL, Roberts P, Stocks PA, Biagini GA, Bray PG, Gibbons P, Berry N, Winstanley PA, Mukhtar A, Bonar-Law R, Hindley S, Bambal RB, Davis CB, Bates M, Hart TK, Gresham SL, Lawrence RM, Brigandi RA, Gomez-delas-Heras FM, Gargallo DV, Ward SA. Candidate selection and preclinical evaluation of N-tert-butyl isoquine (GSK369796), an affordable and effective 4-aminoquinoline antimalarial for the 21st century. J Med Chem. 2009 Mar 12;52(5):1408-15. doi: 10.1021/jm8012618. PMID: 19222165.

[2]Balasubramanian A, Teramoto T, Kulkarni AA, Bhattacharjee AK, Padmanabhan R. Antiviral activities of selected antimalarials against dengue virus type 2 and Zika virus. Antiviral Res. 2017 Jan;137:141-150. doi: 10.1016/j.antiviral.2016.11.015. Epub 2016 Nov 23. PMID: 27889529.