E6 Berbamine (Synonyms: Berbamine p-nitrobenzoate,O-(4-Nitrobenzoyl)berbamine) |
| Catalog No.GC16287 |
calmodulin inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 114784-59-7
Sample solution is provided at 25 µL, 10mM.
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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 | |
| Synonyms | Berbamine p-nitrobenzoate,O-(4-Nitrobenzoyl)berbamine | ||
| Chemical Name | 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 | ||
| Formula | C44H43N3O9 | M.Wt | 757.8 |
| Solubility | ≤25mg/ml in ethanol;25mg/ml in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 37 reference(s) in Google Scholar.)
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