GSK369796 HCL - CAS:1010411-21-8 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	GSK369796 HCL
英文名称:	GSK369796 HCL
别名:	GSK369796;2-[(tert-Butylamino)methyl]-5-[(7-chloroquinolin-4-yl)amino]phenol Dihydrochloride
CAS No:	1010411-21-8	分子式:	C₂₀H₂₄Cl₃N₃O	分子量:	428.78
CAS No:	1010411-21-8
分子式:	C₂₀H₂₄Cl₃N₃O
分子量:	428.78

安全技术说明书(PDF) MSDS(PDF) 点击下载产品说明书(PDF)

G10288 GSK369796 HCL ≥98% (psaitong)

相关产品

CBIQ
CAS No：32081-28-0
Cibenzoline succinate
CAS No：100678-32-8
克罗吗宁
CAS No：94470-67-4
XE991
CAS No：122955-42-4
KCNQ1 activator-1
CAS No：1008671-38-2
SKA-111
CAS No：1369170-24-0

包装规格：

5mg 10mg 25mg 100mg in glass bottle

溶解性：

溶于DMSO

产品描述：

基本信息

产品编号：	G10288
产品名称：	GSK369796 HCL
CAS:	1010411-21-8	储存条件	粉末	-20℃	四年

分子式：	C20H24Cl3N3O		溶于液体	-80℃	6个月
分子量：	428.78			-20℃	1个月
化学名：	2-[(tert-Butylamino)methyl]-5-[(7-chloroquinolin-4-yl)amino]phenol Dihydrochloride
Solubility (25°C)：
体外:	DMSO	86mg/mL (200.56mM)
	Ethanol	10mg/mL (23.32mM)
	Water	40mg/mL (93.28mM)
体内(现配现用):
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	2.3322mL	11.6610mL	23.3220mL
5mM	0.4664mL	2.3322mL	4.6644mL
10mM	0.2332mL	1.1661mL	2.3322mL

生物活性

产品描述	一种可抑制hERG钾离子通道(hERG potassium ion channel)复极化的化合物。
靶点	IC50:7.5μM (hERG potassium ion channel)
体外研究	In vitro,GSK369796 Dihydrochloride can inhibit the growth of Plasmodium falciparum strains 3D7c,HB3c and K1d,with IC50 s of 11.2±2.2,12.6±5.3 and 13.2±3.2nM,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±0.8μM.
体内研究	In vivo,GSK369796 Dihydrochloride can inhibit the growth of Plasmodium berghei ANKA with ED50 and ED90 of 2.8 and 4.7mg/kg,respectively.

推荐实验方法(仅供参考)

细胞实验:

Assays are performed in sterile 96-well microtiter plates,each plate contains 200mL of parasite culture (2% parasitemia,0.5% hematocrit) with or without 10mL 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 24h before they are harvested onto filter mats, dried for 1 h at 55℃,and counted.IC50 values are calculated.

动物实验:

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 20mg/kg or subcutaneously at 10mg/kg,as appropriate.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

搜索质检报告(COA)

参考文献 & 客户发表文献