E6 Berbamine
(Synonyms: Berbamine p-nitrobenzoate,O-(4-Nitrobenzoyl)berbamine) 目录号 : GC16287A calmodulin inhibitor
Cas No.:114784-59-7
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
E6 Berbamine is a calmodulin inhibitor.
Calmodulin, the ubiquitous and multifunctional Ca2+-binding protein, can mediate various regulatory effects of Ca2+, such as the contractile state of smooth muscle. In smooth muscle, the main function of calmodulin is to activate crossbridge cycling and the development of force in response to Ca2+ transient through the activation of myosin light-chain kinase and myosin phosphorylation.
In vitro: The results from a previous study showed that the inhibition of MLCK activity could be increased with increasing levels of E6 Berbamine and was completely overcome by the addition of excessive Ca2+. In addition, the stimulatory activity of MLCK induced by Ca2+ was gradually inhibited by the increasing concentrations of E6 Berbamine suggesting that the inhibition of MLCK activity by E6 Berbamine was concentration dependent. In addition, E6 Berbamine could diminish the fluorescence intensity of dansyl-labeled Ca2+. E6 Berbamine showed no effect on the activity of MLCK fragments produced by limited trypsinization, a novel and considerably potent calmodulin antagonist [1].
In vivo: So far, there is no animal in vivo data reported.
Clinical trial: Up to now, E6 Berbamine is still in the preclinical development stage.
Reference:
[1] Z. Y. Hu, Y. S. Gong and W. L. Huang. Interaction of berbamine compound E6 and calmodulin-dependent myosin light chain kinase. Biochemical Pharmacology44(8), 1543-1547 (1992).
Cas No. | 114784-59-7 | SDF | |
别名 | Berbamine p-nitrobenzoate,O-(4-Nitrobenzoyl)berbamine | ||
化学名 | 3,4,4aS,5,16aR,17,18,19-octahydro-21,22,26-trimethoxy-4,17-dimethyl-16H-1,24:6,9-dietheno-11,15-metheno-2H-pyrido[2’,3’:17,18][1,11]dioxacycloeicosino[2,3,4-ij]isoquinolin-12-ol-4-nitrobenzoate | ||
Canonical SMILES | COC1=C(C2=C(CCN([C@]2([H])CC3=CC=C(OC(C4=CC=C([N+]([O-])=O)C=C4)=O)C(OC5=CC=C(C[C@@]67[H])C=C5)=C3)C)C=C1OC)OC8=CC6=C(CCN7C)C=C8OC | ||
分子式 | C44H43N3O9 | 分子量 | 757.8 |
溶解度 | ≤25mg/ml in ethanol;25mg/ml in DMSO | 储存条件 | Store at -20°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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 1.3196 mL | 6.598 mL | 13.1961 mL |
5 mM | 0.2639 mL | 1.3196 mL | 2.6392 mL |
10 mM | 0.132 mL | 0.6598 mL | 1.3196 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。