ML-7 hydrochloride
(Synonyms: 1-(5-碘萘-1-磺酰基)-1H-六氢-1,4-二氮杂卓盐酸盐,ML 7 hydrochloride) 目录号 : GC11411
A smooth muscle myosin light chain kinase inhibitor
Cas No.:110448-33-4
Sample solution is provided at 25 µL, 10mM.
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Ki = 300 nM
ML-7 is a myosin light chain kinase inhibitor.
Great attention has been gained to the role of myosin light chain kinase (MLCK) pathway in the development of cardiovascular disease and I/R injury. MLCK pathway has been reported to be involved in the pathology of cardiovascular disorders, and the MLCK inhibition could protect heart from I/R injury by regulation of phosphorylation of MLC.
In vitro: Rats with myocardial infarction were intravenously infused with rhNRG-1. The cMLCK expression and phosphorylated MLC-2v were up-regulated in rat treated with rhNRG-1 significantly. Moreover, the restoration of rhNRG-1-induced sarcomeric organization in serum-free cultured neonatal rat cardiomyocytes with rhNRG-1 was inhibited by ML-7 [1].
In vivo: Administration of ML-7 from 10 min before ischemia to the first 10 min of reperfusion led to a significant recovery of heart contractility. Gel analyses of two-dimensional electrophoresis revealed eight proteins with decreased levels in I/R hearts. Six proteins involved in energy metabolism, which were cytochrome b-c1 complex subunit 1, ATP synthase beta subunit, cytochrome c oxidase subunit, mitochondrial NADHdehydrogenase, NADHdehydrogenase iron-sulfur protein 8, and succinyl-CoA ligase subunit. The other two protein levels decreased in I/R hearts, which were peroxiredoxin-2 and tubulin. In addition, ML-7 treatment increased the level of succinyl-CoA ligase, which was a key enzyme involved in the citric acid cycle [2].
Clinical trial: N/A
References:
[1] Gu X,Liu X,Xu D,Li X,Yan M,Qi Y,Yan W,Wang W,Pan J,Xu Y,Xi B,Cheng L,Jia J,Wang K,Ge J,Zhou M. Cardiac functional improvement in rats with myocardial infarction by up-regulating cardiac myosin light chain kinase with neuregulin. Cardiovasc Res.2010 Nov 1;88(2):334-43.
[2] Lin HB,Cadete VJ,Sawicka J,Wozniak M,Sawicki G. Effect of the myosin light chain kinase inhibitor ML-7 on the proteome of hearts subjected to ischemia-reperfusion injury. J Proteomics.2012 Sep 18;75(17):5386-95.
| Cell experiment [1]: | |
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Cell lines |
Primary neonatal cardiomyocytes |
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Preparation method |
Soluble in DMSO >15.95mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
10 μM, 24h |
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Applications |
The restoration of rhNRG-1(Recombinant human neuregulin-1)-induced sarcomeric organization in serum-free cultured neonatal rat cardiomyocytes with rhNRG-1 was inhibited by ML-7. RhNRG-1 could improve cardiac function in experimental heart failure models. |
| Animal experiment [2]: | |
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Animal models |
two-month-old male New Zealand white rabbits |
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Dosage form |
1 mg/kg/day, 12 weeks, oral administration |
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Application |
ML7 might ameliorate VED(Vascular endothelial dysfunction) and AS(atherosclerosis) by regulating the TJ(tight junction) proteins ZO1(zona occludens) and occludin in a rabbit model of atherosclerosis via mechanisms involving MLCK(myosin light chain kinase) and MLC phosphorylation. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Gu X1, Liu X, et al, Cardiac functional improvement in rats with myocardial infarction by up-regulating cardiac myosin light chain kinase with neuregulin. Cardiovasc Res. 2010 Nov 1;88(2):334-43. doi: 10.1093/cvr/cvq223. Epub 2010 Jul 8. [2]. Cheng X1, Wang X2, et al, Myosin light chain kinase inhibitor ML7 improves vascular endothelial dysfunction via tight junction regulation in a rabbit model of atherosclerosis. Mol Med Rep. 2015 Sep;12(3):4109-16. doi: 10.3892/mmr.2015.3973. Epub 2015 Jun 22. |
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| Cas No. | 110448-33-4 | SDF | |
| 别名 | 1-(5-碘萘-1-磺酰基)-1H-六氢-1,4-二氮杂卓盐酸盐,ML 7 hydrochloride | ||
| 化学名 | 1-((5-iodonaphthalen-1-yl)sulfonyl)-1,4-diazepane hydrochloride | ||
| Canonical SMILES | IC1=CC=CC2=C1C=CC=C2S(N3CCCNCC3)(=O)=O.Cl | ||
| 分子式 | C15H18ClIN2O2S | 分子量 | 452.74 |
| 溶解度 | ≥ 15.95 mg/mL in DMSO, ≥ 8.82 mg/mL in Water with ultrasonic and warming | 储存条件 | Store at 2-8°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet