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ML-7盐酸盐

ML-7盐酸盐用途

ML-7 hydrochloride 是一种萘磺酰胺衍生物,有效抑制 MLCK (IC50=300 nM) 和 TRPC6 通道 (IC50>10 μM)。

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ML-7盐酸盐名称

[ CAS 号 ]:
110448-33-4

[ 中文名 ]:
1-(5-碘萘-1-磺酰基)-1H-六氢-1,4-二氮杂卓盐酸盐

[ 英文名 ]:
ML-7 hydrochloride

[中文别名 ]:

[英文别名 ]:

ML-7 HYDROCHLORIDE
MFCD00065524
ML-7 (hydrochloride)

ML-7盐酸盐生物活性

[ 描述 ]:

ML-7 hydrochloride 是一种萘磺酰胺衍生物,有效抑制 MLCK (IC50=300 nM) 和 TRPC6 通道 (IC50>10 μM)。

[ 相关类别 ]:

信号通路 >> 细胞骨架 >> 肌球蛋白

研究领域 >> 癌症

[ 靶点 ]

IC50: 300 nM (MLCK)[1]

[体外研究]

ML-7盐酸盐抑制兔门静脉α1-肾上腺素受体NSCC,IC50为0.8μM[1]。肌球蛋白轻链激酶(MLCK)抑制剂ML-7盐酸盐(3μM和10μM)也减弱了右美托咪定(DMT)诱导的收缩(与对照相比p <0.05)[2]。

[体内研究]

在假手术动物中,Evans Blue外渗在ML-7盐酸盐和赋形剂组之间没有差异(假+载体：0.26±0.02OD/g;假+ ML-7：0.26±0.02OD/g)。用载体处理的动物CCI抑制MLCK后,与载体处理的动物相比,导致脑内伊文思蓝的量显着降低(CCI +载体：0.42±0.04OD/g; CCI + ML-7：0.35±0.05OD/g,p = 0.048)[3]。

[动物实验]

小鼠[3]在创伤前和创伤后6小时腹膜内注射选择性MLCK抑制剂ML-7（1mg / kg）或载体溶液（0.9％NaCl，对照组）处理小鼠。控制皮质撞击（CCI）后24小时测量半球脑水含量和神经功能，随机分为：（i）载体+假手术，（ii）载体+ CCI，（iii）ML-7 + shamsurgery或（iv）随机分配至：（i）载体+假手术，（ii）载体+ CCI，（iii）ML-7 +假手术或（iv）的动物中ML-7 + CCI（每组n = 8）和CCI后15分钟ML-7 + CCI（每组n = 6）。在创伤前和创伤后6小时，通过腹膜内注射选择性MLCK抑制剂ML-7（1mg / kg）或载体溶液（0.9％NaCl，对照组）处理小鼠。埃文斯蓝外渗在手术后24小时确定为随机分配至：（i）媒介物+ CCI或（ii）ML-7 + CCI（每组n = 5）和随机分配至（iii）媒介物+假手术的动物或（ iv）ML-7 +假手术（每组n = 6）。在24小时CCI和假手术中测量ICP。

[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.

[相关活性小分子]

ML-7盐酸盐物理化学性质

[ 沸点 ]:
542.7ºC at 760 mmHg

[ 熔点 ]:
246-249ºC dec.

[ 分子式 ]:
C₁₅H₁₈ClIN₂O₂S

[ 分子量 ]:
452.738

[ 闪点 ]:
282ºC

[ 精确质量 ]:
451.982208

[ PSA ]:
57.79000

[ LogP ]:
4.57790

[ 储存条件 ]:
-20℃

ML-7盐酸盐MSDS

详细MSDS(安全技术说明书)

ML-7盐酸盐安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

ML-7盐酸盐文献

Myosin II controls cellular branching morphogenesis and migration in three dimensions by minimizing cell-surface curvature.

Nat. Cell Biol. 17(2) , 137-47, (2015)

In many cases, cell function is intimately linked to cell shape control. We used endothelial cell branching morphogenesis as a model to understand the role of myosin II in shape control of invasive ce...

Directional bleb formation in spherical cells under temperature gradient.

Biophys. J. 109 , 355-64, (2015)

Living cells sense absolute temperature and temporal changes in temperature using biological thermosensors such as ion channels. Here, we reveal, to our knowledge, a novel mechanism of sensing spatial...

MAPK3/1 (ERK1/2) and Myosin Light Chain Kinase in Mammalian Eggs Affect Myosin-II Function and Regulate the Metaphase II State in a Calcium- and Zinc-Dependent Manner.

Biol. Reprod. 92 , 146, (2015)

Vertebrate eggs are arrested at metaphase of meiosis II, a state classically known as cytostatic factor arrest. Maintenance of this arrest until the time of fertilization and then fertilization-induce...

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