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  1. Apoptosis
  2. TNF Receptor
  3. C 87

C 87 是一種新型小分子 TNFα 抑制劑; 高效抑制 TNFα 誘導(dǎo)的細(xì)胞毒性,IC50 值為 8.73 μM。

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C 87 Chemical Structure

C 87 Chemical Structure

CAS No. : 332420-90-3

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10 mM * 1 mL in DMSO ¥885
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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 2 篇科研文獻(xiàn)

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

C 87 is a novel small-molecule TNFα inhibitor; potently inhibits TNFα-induced cytotoxicity with an IC50 of 8.73 μM.

IC50 & Target

IC50: 8.73 μM (TNFα-induced cytotoxicity)[1]

細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
THP-1 IC50
0.11 μM
Compound: C87
Inhibition of LPS-induced TNFalpha production in human THP-1 cells incubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA
Inhibition of LPS-induced TNFalpha production in human THP-1 cells incubated for 2 hrs followed by LPS stimulation and measured after 12 hrs by ELISA
[PMID: 33479624]
THP-1 CC50
10.81 μM
Compound: C87
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
Cytotoxicity against human THP-1 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
[PMID: 33479624]
體外研究
(In Vitro)

C 87 (C87) 直接結(jié)合 TNFα,有效抑制 TNFα 誘導(dǎo)的細(xì)胞毒性 (IC50=8.73 μM) 并有效阻斷 TNFα 觸發(fā)的信號傳導(dǎo)活動。C 87 在體外表現(xiàn)出良好的溶解性和一致的劑量依賴性功能。C 87 完全阻斷 TNFα 誘導(dǎo)的 caspase-3caspase-8 激活。在 L929 細(xì)胞中,c-Jun 氨基末端激酶 (JNK) 的活性會被 C 87 顯著降低。C 87 還可以防止用 TNFα 處理的細(xì)胞中 IκBα 的降解。C 87 有效阻斷由 TNFα 觸發(fā)的多個信號轉(zhuǎn)導(dǎo)通路和下游靶基因激活[1]

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

體內(nèi)研究
(In Vivo)

C 87 (C87) 可減輕 TNFα 誘導(dǎo)的炎癥,從而顯著減少肝臟損傷并提高動物存活率[1]。
與載體對照相比,C 87 注射延遲了死亡發(fā)生率并將存活率提高了兩倍。在接受 C 87 處理的小鼠中,丙氨酸轉(zhuǎn)氨酶和天冬氨酸轉(zhuǎn)氨酶的水平持續(xù)降低[1]

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

分子量

502.93

Formula

C24H15ClN6O3S

CAS 號
性狀

固體

顏色

Yellow to orange

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 2 years
-20°C 1 year
溶解性數(shù)據(jù)
細(xì)胞實驗: 

DMSO 中的溶解度 : 5.05 mg/mL (10.04 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 1.9883 mL 9.9417 mL 19.8835 mL
5 mM 0.3977 mL 1.9883 mL 3.9767 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, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(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

動物實驗:

以下溶解方案,請直接配制工作液。建議現(xiàn)用現(xiàn)配,在短期內(nèi)盡快用完。 以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比; 如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過加熱和/或超聲的方式助溶。

  • 方案 一

    請依序添加每種溶劑: 15% Solutol HS 15    10% Cremophor EL    35% PEG400    40% Water

    Solubility: 2 mg/mL (3.98 mM); 懸濁液; 超聲助溶

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(xiàn)
Cell Assay
[1]

The inhibition of the cytotoxic effect of human TNFα by compounds (C 87) is measured in L929 cell line. L929 cells are seeded at a density of 104 cells/well in a 96-well plate and incubated for 24 h in RPMI 1640 with 10% FBS at 37°C. Compounds (C 87) are added to the cells with 1 μg/mL actinomycin D and 1 ng/mL TNFα and then incubated at 37 °C for 20 h before analysis. Cell survival is measured using the MTT method[1].

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

Animal Administration
[1]

BALB/c mice are used in the study. Before LPS/GalN challenge (LPS (50 μg/kg) and D-GalN (1.2g/kg)), mice are injected intraperitoneally with C 87 (12.5 mg/kg), Enbrel (4 mg/kg), or vehicle, respectively, at 1, 8, and 16 h. Blood is collected with retro-orbital sampling. Activities of alanine transaminase and aspartate transaminase are detected. Liver tissues are collected and fixed in 10% formalin, and sections are stained with hematoxylin and eosin[1].

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

參考文獻(xiàn)

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, 2 years; -20°C, 1 year。-80°C儲存時,請在2年內(nèi)使用, -20°C儲存時,請在1年內(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 1.9883 mL 9.9417 mL 19.8835 mL 49.7087 mL
5 mM 0.3977 mL 1.9883 mL 3.9767 mL 9.9417 mL
10 mM 0.1988 mL 0.9942 mL 1.9883 mL 4.9709 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:
C 87
目錄號:
HY-100735
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