1. Membrane Transporter/Ion Channel
  2. P2X Receptor
  3. GSK-1482160

GSK-1482160 是一种可口服的 P2X7 受体负变构调节剂。P2X7 受体参与中枢和外周免疫细胞产生促炎细胞因子,例如 Il-1β。GSK-1482160 具有研究炎症性疾病的潜力。

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GSK-1482160 Chemical Structure

GSK-1482160 Chemical Structure

CAS No. : 1001389-72-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥1100
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1 mg ¥400
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5 mg ¥1000
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10 mg ¥1600
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25 mg ¥3200
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50 mg ¥5600
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Customer Review

Other Forms of GSK-1482160:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK-1482160 is an orally available negative allosteric modulator of the P2X7 receptor. P2X7 receptors are involved in the production of pro-inflammatory cytokines, such as Il-1β, by central and peripheral immune cells. GSK-1482160 has the potential for the research of inflammation diseases[1].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
HEK293 IC50
119.3 nM
Compound: 1b; GSK1482160
Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytome
Inhibition of human P2X7 expressed in human HEK293 cells assessed as reduction in BzATP-stimulated TO-PRO-3 incorporation preincubated with compound and TO-PRO-3 for 15 mins prior to BzATP addition and measured after 1 hr by Fluo-3AM dye based flow cytome
[PMID: 31525963]
HEK293 IC50
332.4 nM
Compound: 1b; GSK1482160
Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method
Displacement of [3H]-A804598 from human P2X7 expressed in human HEK293 cell membrane incubated for 1 hr by microplate scintillation counting method
[PMID: 31525963]
HEK293 IC50
8.9 nM
Compound: GSK1482160
Displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay
Displacement of [11C]GSK1482160 from human recombinant P2X7 receptor expressed in HEK293 cell membranes incubated for 30 mins by scintillation counting method based radioligand competitive binding assay
[PMID: 31005444]
Clinical Trial
分子量

334.72

Formula

C14H14ClF3N2O2

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (298.76 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)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.9876 mL 14.9379 mL 29.8757 mL
5 mM 0.5975 mL 2.9876 mL 5.9751 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。-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。

  • 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

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

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
纯度 & 产品资料
参考文献

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。-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
DMSO 1 mM 2.9876 mL 14.9379 mL 29.8757 mL 74.6893 mL
5 mM 0.5975 mL 2.9876 mL 5.9751 mL 14.9379 mL
10 mM 0.2988 mL 1.4938 mL 2.9876 mL 7.4689 mL
15 mM 0.1992 mL 0.9959 mL 1.9917 mL 4.9793 mL
20 mM 0.1494 mL 0.7469 mL 1.4938 mL 3.7345 mL
25 mM 0.1195 mL 0.5975 mL 1.1950 mL 2.9876 mL
30 mM 0.0996 mL 0.4979 mL 0.9959 mL 2.4896 mL
40 mM 0.0747 mL 0.3734 mL 0.7469 mL 1.8672 mL
50 mM 0.0598 mL 0.2988 mL 0.5975 mL 1.4938 mL
60 mM 0.0498 mL 0.2490 mL 0.4979 mL 1.2448 mL
80 mM 0.0373 mL 0.1867 mL 0.3734 mL 0.9336 mL
100 mM 0.0299 mL 0.1494 mL 0.2988 mL 0.7469 mL
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.

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Inquiry Information

产品名称:
GSK-1482160
目录号:
HY-19888
需求量: