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

GSK-1482160 是一種可口服的 P2X7 受體負變構(gòu)調(diào)節(jié)劑。P2X7 受體參與中樞和外周免疫細胞產(chǎn)生促炎細胞因子,例如 Il-1β。GSK-1482160 具有研究炎癥性疾病的潛力。

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GSK-1482160 Chemical Structure

GSK-1482160 Chemical Structure

CAS No. : 1001389-72-5

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2.  同一機構(gòu)(單位)同一產(chǎn)品試用裝僅限申領(lǐng)一次,同一機構(gòu)(單位)一年內(nèi)

     可免費申領(lǐng)三個不同產(chǎn)品的試用裝。

3.  試用裝只面向終端客戶。

規(guī)格 價格 是否有貨 數(shù)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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100 mg 現(xiàn)貨 詢價
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Customer Review

Other Forms of GSK-1482160:

  • 生物活性

  • 純度 & 產(chǎn)品資料

  • 參考文獻

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].

細胞效力
(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 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性數(shù)據(jù)
細胞實驗: 

DMSO 中的溶解度 : 100 mg/mL (298.76 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響,請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)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
查看完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物溶解方案計算器
請輸入動物實驗的基本信息:

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

由于實驗過程有損耗,建議您多配一只動物的量
計算結(jié)果
工作液所需濃度 : mg/mL
純度 & 產(chǎn)品資料
參考文獻

完整儲備液配制表

* 請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液;一旦配成溶液,請分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C儲存時,請在6個月內(nèi)使用,-20°C儲存時,請在1個月內(nèi)使用。

可選溶劑 濃度 溶劑體積 質(zhì)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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產(chǎn)品名稱:
GSK-1482160
目錄號:
HY-19888
需求量: