ML-7 hydrochloride

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

ML-7 hydrochloride  纯度: 99.75%

ML-7 hydrochloride 是一种萘磺酰胺衍生物,有效抑制 MLCK (IC50=300 nM)。ML-7 hydrochloride 也是一种 YAP/TAZ 抑制剂。

ML-7 hydrochloride

ML-7 hydrochloride Chemical Structure

CAS No. : 110448-33-4

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥675 In-stock
10 mg ¥614 In-stock
50 mg ¥2864 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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生物活性

ML-7 hydrochloride is a naphthalene sulphonamide derivative, potently inhibits MLCK (IC50=300 nM). ML-7 hydrochloride also inhibits YAP/TAZ.

IC50 & Target

IC50: 300 nM (MLCK)[1]

体外研究
(In Vitro)

ML-7 hydrochloride inhibits rabbit portal vein α1-adrenoceptor NSCC with IC50 of 0.8 μM[1]. The myosin light chain kinase (MLCK) inhibitor ML-7 hydrochloride (3 μ M and 10 μM) also attenuates the Dexmedetomidine (DMT)-induced contraction (p<0.05 versus control)[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

In sham operated animals Evans Blue extravasation is not different between ML-7 hydrochloride and vehicle group (sham+vehicle: 0.26±0.02 OD/g; sham+ML-7: 0.26±0.02 OD/g). After CCI inhibition of MLCK with ML-7 results in a significant lower amount of intracerebral Evans Blue compared to vehicle treated animals (CCI+vehicle: 0.42±0.04 OD/g; CCI+ML-7: 0.35±0.05 OD/g, p=0.048)[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

452.74

Formula

C15H18ClIN2O2S

CAS 号

110448-33-4

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据
In Vitro: 

DMSO : ≥ 43 mg/mL (94.98 mM)

H2O : 1.43 mg/mL (3.16 mM; Need ultrasonic)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2088 mL 11.0439 mL 22.0877 mL
5 mM 0.4418 mL 2.2088 mL 4.4175 mL
10 mM 0.2209 mL 1.1044 mL 2.2088 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 (sealed storage, away from moisture)。-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: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 1.67 mg/mL (3.69 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.69 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 16.7 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。

    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
  • 2.

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

    Solubility: ≥ 1.67 mg/mL (3.69 mM); Clear solution

    此方案可获得 ≥ 1.67 mg/mL (3.69 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 16.7 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Shi J, et al. Myosin light chain kinase-independent inhibition by ML-9 of murine TRPC6 channels expressed in HEK293cells. Br J Pharmacol. 2007 Sep;152(1):122-31.

    [2]. Yu J, et al. Dexmedetomidine-Induced Contraction in the Isolated Endothelium-Denuded Rat Aorta Involves PKC-δ-mediated JNK Phosphorylation. Int J Med Sci. 2015 Sep 4;12(9):727-36

    [3]. Luh C, et al. Inhibition of myosin light chain kinase reduces brain edema formation after traumatic brain injury. J Neurochem. 2010 Feb;112(4):1015-25.

    [4]. Pobbati AV, et, al. A combat with the YAP/TAZ-TEAD oncoproteins for cancer therapy. Theranostics. 2020 Feb 18;10(8):3622-3635.

Animal Administration
[3]

Mice[3]
Mice are treated with intraperitoneal injection of the selective MLCK inhibitor ML-7 (1 mg/kg) or vehicle solution (0.9% NaCl, control group) 1 h prior to and 6 h after trauma. Hemispheric brain water content and neurological function are measured 24 h after controlled cortical impact (CCI) in animals randomized to: (i) vehicle+sham surgery, (ii) vehicle+CCI, (iii) ML-7+sham surgery or (iv) ML-7+CCI (n=8 per group) and 15 min after CCI in animals randomized to: (i) vehicle+sham surgery, (ii) vehicle+CCI, (iii) ML-7+sham surgery or (iv) ML-7+CCI (n=6 per group). Mice are treated with intraperitoneal injection of the selective MLCK inhibitor ML-7 (1 mg/kg) or vehicle solution (0.9% NaCl, control group) 1 h prior to and 6 h after trauma. Evans Blue extravasation is determined 24 h after surgery in animals randomized to: (i) vehicle + CCI or (ii) ML-7+CCI (n=5 per group) and in animals randomized to (iii) vehicle + sham surgery or (iv) ML-7+sham surgery (n=6 per group). ICP is measured 24 h CCI and sham surgery.

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Shi J, et al. Myosin light chain kinase-independent inhibition by ML-9 of murine TRPC6 channels expressed in HEK293cells. Br J Pharmacol. 2007 Sep;152(1):122-31.

    [2]. Yu J, et al. Dexmedetomidine-Induced Contraction in the Isolated Endothelium-Denuded Rat Aorta Involves PKC-δ-mediated JNK Phosphorylation. Int J Med Sci. 2015 Sep 4;12(9):727-36

    [3]. Luh C, et al. Inhibition of myosin light chain kinase reduces brain edema formation after traumatic brain injury. J Neurochem. 2010 Feb;112(4):1015-25.

    [4]. Pobbati AV, et, al. A combat with the YAP/TAZ-TEAD oncoproteins for cancer therapy. Theranostics. 2020 Feb 18;10(8):3622-3635.

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