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U0126-EtOH
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
U0126-EtOH图片
CAS NO:1173097-76-1
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
10mg电议
50mg电议
100mg电议
200mg电议
500mg电议
1 g电议
5 g电议

产品介绍
U0126-EtOH 是一种有效,非 ATP 竞争性的,选择性的MEK1MEK2抑制剂,IC50分别为 72 nM 和 58 nM。U0126-EtOH 是一种自噬 (autophagy) 和线粒体自噬 (mitophagy) 抑制剂。
生物活性

U0126 (U0126-EtOH) is a potent, non-ATP competitive and selectiveMEK1andMEK2inhibitor, withIC50s of 72 nM and 58 nM, respectively. U0126 is anautophagyandmitophagyinhibitor[1][2][3][4].

IC50& Target[1]

MEK2

60 nM (IC50)

MEK1

70 nM (IC50)

体外研究
(In Vitro)

Treatment with U0126-EtOH (U0126) efficiently reduces progeny virus titers of all tested strains in A549 cells. While nM concentrations of U0126-EtOH are efficient to reduce H1N1v and H5N1 (MB1), μM concentrations of U0126-EtOH are required to reduce the virus titer of H5N1 (GSB) and H7N7. The EC50values for U0126-EtOH against H1N1v are 1.2±0.4 μM in A549 cells and 74.7±1.0 μM in MDCKII cells[2].
Rat hepatocarcinoma cells (FAO) stimulated by fetal calf serum (FCS) exhibits a significant proportion in S phase (32.62%) whereas U0126-EtOH (U0126) strongly decreases the proportion of cells in S phase (9.92%) and increases the proportion of cells in G0-G1phase and to a lesser extent in G2/M[3].

Cell Viability Assay[2]

Cell Line:A549 and MDCK II cells.
Concentration:0.001-1000 μM.
Incubation Time:48 h.
Result:The EC50values for U0126 against H1N1v were 1.2 ± 0.4 μM in A549 cells and 74.7 ± 1.0 μM in MDCKII cells
体内研究
(In Vivo)

Mice are treated daily with U0126-EtOH (U0126; i.p., 10.5 mg/kg). In control experiment, tumor sizes are constant or slightly increase all over the kinetic. At the opposite, in all U0126-EtOH experiments, engraftment and early tumor growth are significantly decreased. Furthermore, a 60-70% reduction in the volume of tumors treated with U0126-EtOH is obtained 9 days after injection and thereafter[3].
Rats are subjected to 120 minutes transient middle cerebral artery occlusion (tMCAO) and thereafter treated with the U0126-EtOH (U0126; i.p., 30 mg/kg) at 0 and 24 hours of reperfusion. After treatment with U0126-EtOH, the vasoconstriction to S6c is markedly reduced[4].

Animal Model:Athymic female nude mice (SWISS, nu/nu)[3].
Dosage:10.5 mg/kg.
Administration:Intraperitoneal injection daily.
Result:Inhibited tumor growth.
Animal Model:Twelve-week-old female Wistar rats (250 to 265 g)[4].
Dosage:30 mg/kg.
Administration:Intraperitoneally.
Result:The vasoconstriction to S6c is markedly reduced.
分子量

426.56

性状

Solid

Formula

C20H22N6OS2

CAS 号

1173097-76-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
溶解性数据
In Vitro: 

DMSO : 50 mg/mL(117.22 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.3443 mL11.7217 mL23.4434 mL
5 mM0.4689 mL2.3443 mL4.6887 mL
10 mM0.2344 mL1.1722 mL2.3443 mL
*

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℃, 6 months; -20℃, 1 month。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

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

  • 1.

    请依序添加每种溶剂: 0.5%CMC-Na/saline water

    Solubility: 5 mg/mL (11.72 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.88 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.88 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 4.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.08 mg/mL (4.88 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (4.88 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在本网站选购。