2. Membrane Transporter/Ion Channel Anti-infection
  3. Potassium Channel Parasite
  4. GSK369796 Dihydrochloride

GSK369796 Dihydrochloride 

目录号: HY-12082A 纯度: 99.56%
COA 产品使用指南

摩尔计算器

GSK369796 Dihydrochloride 是一种经济有效的抗疟药，可抑制 hERG 钾离子通道 (hERG potassium ion channel) 复极化，IC50 值为 7.5 μM。

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GSK369796 Dihydrochloride Chemical Structure

GSK369796 Dihydrochloride Chemical Structure

CAS No. : 1010411-21-8

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2.  同一机构（单位）同一产品试用装仅限申领一次，同一机构（单位）一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户。

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1509
In-stock
2 mg ￥1100
In-stock
5 mg ￥1600
In-stock
10 mg ￥2200
In-stock
50 mg ￥6600
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

Customer Review

GSK369796 Dihydrochloride 相关抗体

Top Publications Citing Use of Products

查看 Parasite 亚型特异性产品:

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Amebae Coccidia Leishmania Mite Plasmodium Toxoplasma Trypanosoma Schistosome

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK369796 Dihydrochloride is an affordable and effective antimalarial and inhibits hERG potassium ion channel repolarization with an IC50 of 7.5 μM.

IC50 & Target

IC50: 7.5 μM (hERG potassium ion channel)[1]
体外研究
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GSK369796 Dihydrochloride 相关抗体:
体内研究
(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[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
分子量

428.78

Formula

C20H24Cl3N3O
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO 中的溶解度 : 100 mg/mL (233.22 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : 50 mg/mL (116.61 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3322 mL 11.6610 mL 23.3220 mL
5 mM 0.4664 mL 2.3322 mL 4.6644 mL
查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

In Vivo:

请根据您的 实验动物和给药方式 选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.83 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (5.83 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

    20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献
Cell Assay
[1]

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

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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 20 mg/kg or subcutaneously at 10 mg/kg, as appropriate[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

GSK369796 Dihydrochloride 相关分类

完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.3322 mL 11.6610 mL 23.3220 mL 58.3050 mL
5 mM 0.4664 mL 2.3322 mL 4.6644 mL 11.6610 mL
10 mM 0.2332 mL 1.1661 mL 2.3322 mL 5.8305 mL
15 mM 0.1555 mL 0.7774 mL 1.5548 mL 3.8870 mL
20 mM 0.1166 mL 0.5830 mL 1.1661 mL 2.9152 mL
25 mM 0.0933 mL 0.4664 mL 0.9329 mL 2.3322 mL
30 mM 0.0777 mL 0.3887 mL 0.7774 mL 1.9435 mL
40 mM 0.0583 mL 0.2915 mL 0.5830 mL 1.4576 mL
50 mM 0.0466 mL 0.2332 mL 0.4664 mL 1.1661 mL
60 mM 0.0389 mL 0.1943 mL 0.3887 mL 0.9717 mL
80 mM 0.0292 mL 0.1458 mL 0.2915 mL 0.7288 mL
100 mM 0.0233 mL 0.1166 mL 0.2332 mL 0.5830 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK3697961010411-21-8GSK 369796GSK-369796Potassium ChannelParasiteKcsAInhibitorinhibitorinhibit

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