GSK369796 2HCl
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货号：A984981
同义名：
GSK369796 (hydrochloride);GSK369796 Dihydrochloride
GSK369796 is an anti-malaria drug candidate.
GSK369796 2HCl 化学结构
GSK369796 2HCl 3D分子结构
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GSK369796 2HCl 质控信息
Tolbutamide
✔
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Glimepiride
++++
SUR1, IC50: 5.4 nM
SUR2B, IC50: 7.3 nM
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Dronedarone Hydrochloride
✔
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Gliquidone
++
Potassium channel, IC50: 27.2 nM
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TRAM-34
+++
IKCa1 (KCa3.1), Kd: 20 nM
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Glibenclamide
✔
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Amiodarone HCl
✔
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Gliclazide
++
Potassium channel, IC50: 184 nM
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Repaglinide
✔
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Dofetilide
✔
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Nateglinide
✔
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Quinine hydrochloride dihydrate
✔
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ML133 HCl
+
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
GSK369796 2HCl 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] [2]
GSK369796 2HCl 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.
GSK369796 2HCl 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
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
GSK369796 2HCl 技术信息
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