U0126-EtOH - CAS:1173097-76-1

您当前的位置：

U0126-EtOH

目录号 : KM6965 CAS No. : 1173097-76-1 纯度 : 98%

产品说明书产品使用指南

U0126-EtOH 是一种有效，非 ATP 竞争性的，选择性的 MEK1 和 MEK2 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。

规格	价格	是否有货
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg		In-stock
500mg		In-stock
1g	询价	In-stock
5g	询价	In-stock

查看所有商品（2）

加入购物车大包装询价

Other Forms of Rapamycin:

UH15-38 In-stock
Shegansu B In-stock
Salcomine In-stock
Cletoquine hydrochloride In-stock
3-Phenyl-N-[1-(phenylmethyl)-4-piperidinyl]-tricyclo[3.3.1.13,7]decane-1-carboxamide In-stock

KKL Med 的所有产品和服务仅用于科学研究，不能被用于人体，兽医，我们也不向个人提供产品和服务。

生物活性

U0126 (U0126-EtOH) is a potent, non-ATP competitive and selective MEK1 and MEK2 inhibitor, with IC₅₀s of 72 nM and 58 nM, respectively. U0126 is an autophagy and mitophagy inhibitor.

体外研究

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 EC₅₀ values for U0126-EtOH against H1N1v are 1.2±0.4 μM in A549 cells and 74.7±1.0 μM in MDCKII cells.
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-G₁ phase and to a lesser extent in G₂/M.

Cell Viability Assay

Cell Line:	A549 and MDCK II cells.
Concentration:	0.001-1000 μM.
Incubation Time:	48 h.
Result:	The EC₅₀ values 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

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.
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.

Animal Model:	Athymic female nude mice (SWISS, nu/nu).
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).
Dosage:	30 mg/kg.
Administration:	Intraperitoneally.
Result:	The vasoconstriction to S6c is markedly reduced.

分子式

C₂₀H₂₂N₆Os₂

分子量

426.56

CAS号

1173097-76-1

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

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 mg	5 mg	10 mg

1 mM	2.3443 mL	11.7217 mL	23.4434 mL
5 mM	0.4689 mL	2.3443 mL	4.6887 mL
10 mM	0.2344 mL	1.1722 mL	2.3443 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°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。

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。
3.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
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。