Metoprolol-d6 (tartrate)
目录号 : GC47669
A neuropeptide with diverse biological activities
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Metoprolol-d6 is intended for use as an internal standard for the quantification of metoprolol by GC- or LC-MS. Metoprolol is a potent and selective β1-adrenergic receptor (β1-AR) antagonist (Ki = 47 nM).1 It is selective for β1- over β2- and β3-ARs (Kis = 2.96 and 10.1 μM, respectively). In vivo, metoprolol (2.5 mg/kg per hour) reduces aortic atherosclerotic plaque area, serum levels of TNF-α and CXCL1, and plaque macrophage content in an ApoE-/- mouse model of atherosclerosis.2 Metoprolol (1 mg/kg per day) reduces biventricular cavity expansion and myocardial necrosis in a mouse model of encephalomyocarditis-induced congestive heart failure when administered in combination with captopril .3 Formulations containing metoprolol have been used in the treatment of high blood pressure and heart failure.
1.Hoffmann, C., Leitz, M.R., Oberdorf-Maass, S., et al.Comparative pharmacology of human β-adrenergic receptor subtypes - characterization of stably transfected receptors in CHO cellsNaunyn Schmiedebergs Arch. Pharmacol.369(2)151-159(2004) 2.Ulleryd, M.A., Bernberg, E., Yang, L.J., et al.Metoprolol reduces proinflammatory cytokines and atherosclerosis in ApoE-/- mice.Biomed. Res. Int.548783(2014) 3.Kanda, T., Inoue, M., Suzuki, T., et al.Low-dose combination therapy with metoprolol and captopril for congestive heart failure in mice.Cardiovasc. Drugs Ther.7(5)795-800(1993)
| Cas No. | N/A | SDF | |
| Canonical SMILES | COCCC1=CC=C(C=C1)OCC(CNC(C([2H])([2H])[2H])C([2H])([2H])[2H])O.OC(C(C(C(O)=O)O)O)=O.COCCC2=CC=C(C=C2)OCC(CNC(C([2H])([2H])[2H])C([2H])([2H])[2H])O | ||
| 分子式 | C15H19D6NO3.1/2C4H6O6 | 分子量 | 348.5 |
| 溶解度 | DMSO: soluble,Methanol: soluble,Water: soluble | 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8694 mL | 14.3472 mL | 28.6944 mL |
| 5 mM | 0.5739 mL | 2.8694 mL | 5.7389 mL |
| 10 mM | 0.2869 mL | 1.4347 mL | 2.8694 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。
Characterisation of quaternary polymethacrylate films containing tartaric acid, metoprolol free base or metoprolol tartrate
Eur J Pharm Biopharm 2009 Nov;73(3):366-72.PMID:19651209DOI:10.1016/j.ejpb.2009.07.010.
The aim of this study was to better understand the interactions between metoprolol tartrate and quaternary polymethacrylate (Eudragit RL and Eudragit RS) films. For reasons of comparison, polymeric films containing the free base metoprolol or free tartaric acid were also prepared. Systems containing various amounts of the free base, free acid and the salt were characterised using polarising light microscopy, X-ray powder diffraction, differential scanning calorimetry and mechanical analysis (puncture test). The free base is the most efficient plasticiser of the three species for Eudragit RL and Eudragit RS, but with limited solubility in the polymers. Due to its hydrophobicity, it can interact with the hydrophobic polymer backbones. In contrast, in salt containing films, ionic interactions between the positively charged quaternary ammonium groups and the negatively charged tartrate anions apparently occur, this being suggested by the different effects on Eudragit RL versus RS, which have different contents of quaternary ammonium groups. Importantly, the combination of acid and base as a salt avoids drug precipitation at higher metoprolol contents. The obtained new insight into the occurring drug-polymer interactions can help to facilitate the development/optimisation of this type of dosage forms.
Calcium tartrate gel
Anal Biochem 1989 May 15;179(1):86-9.PMID:2757203DOI:10.1016/0003-2697(89)90205-4.
A method for preparation of a gel for chromatography has been developed. The adsorbent is calcium tartrate treated with potassium phosphate. By changing the temperature of synthesis (10-65 degrees C) and concentration of the salts (calcium chloride and sodium potassium tartrate) from 0.3 to 3.0 M, we have been able to prepare adsorbent crystals of definite sizes in the range 35-200 microns. In all cases, for synthesis of adsorbent, the Ca2+/K+Na+ ratio was greater than 1. After treatment of calcium tartrate crystals with 0.075-1.5 M potassium phosphate at 80-100 degrees C and pH 8.5-9.0, an appropriate chromatographic adsorbent was prepared. The chromatographic properties of calcium tartrate gel have been studied. The adsorbent permits flow rates of 25-150 ml/h, depending on the particle size. The capacity of calcium tartrate gel for binding BSA, RNA, and DNA was similar to that of Tiselius' hydroxyapatite (A. Tiselius, S. Hjerten, O. Levin (1956) Arch. Biochem. Biophys. 65, 132-155). The spheric shape of gel particles permits uniform and compact packing of adsorbent under the conditions of column chromatography.
Investigation of radiation sensitivity of some tartrate compounds
Radiat Prot Dosimetry 2014 Jun;159(1-4):199-202.PMID:24736299DOI:10.1093/rpd/ncu119.
Potential electron spin resonance (ESR) dosimetric application of different compounds of sodium tartrate, such as sodium tartrate dihydrate, sodium bitartrate monohydrate and potassium sodium tartrate tetrahydrate, was investigated in the range of 0.74-25 Gy. While the radiation-induced intermediates produced in these compounds are similar, their radiation yields are different. It is found that the radiation yield of sodium tartrate dihydrate is higher than other compounds of sodium tartrates. Comparison of the radiation yields were also made between well-known samples of ammonium tartrate, alanine and lithium formate. It is found that the radiation yields of sodium tartrate dihydrate, sodium bitartrate monohydrate and potassium sodium tartrate tetrahydrate have the values of 1.22, 0.18 and 0.13, respectively.
Deeper insight into the drug release mechanisms in Eudragit RL-based delivery systems
Int J Pharm 2010 Apr 15;389(1-2):139-46.PMID:20105459DOI:10.1016/j.ijpharm.2010.01.031.
Tartaric acid, metoprolol free base and metoprolol tartrate act as plasticisers for Eudragit RL, in the dry but also in the wet state. Fitting analytical solutions of Fick's second law of diffusion allowed for the determination of the apparent diffusivities of water and of tartaric acid, metoprolol free base and metoprolol tartrate upon exposure of thin films to 0.1M HCl, phosphate buffer pH 7.4 and distilled water. Based on these calculations, it could be shown that water penetration into the systems is predominantly controlled by pure diffusion, irrespective of the type of bulk fluid. Interestingly, the plasticising effect of metoprolol tartrate was much more pronounced than that of tartaric acid, resulting in monotonically increasing diffusion coefficients with increasing initial drug content. In contrast, the plasticising activity of metoprolol free base was very limited in the wet state, due to drug precipitation in aqueous environments. Partially observed film shrinking (after an initial system swelling) could be attributed to the leaching of the plasticising compound into the release medium, resulting in less flexible polymeric networks and squeezing out of water. Also the release of tartaric acid, metoprolol free base and metoprolol tartrate into the investigated bulk fluids was predominantly diffusion controlled. However, the precipitation of the free base in wet films rendered the mass transport mechanisms more complex, at moderate and high initial drug loadings. The obtained new insight into the underlying drug release mechanisms in Eudragit RL networks can help to facilitate the optimisation of this type of dosage forms.
Inhibitory effect of tartrate against phosphate-induced DJ-1 aggregation
Int J Biol Macromol 2018 Feb;107(Pt B):1650-1658.PMID:29030185DOI:10.1016/j.ijbiomac.2017.10.022.
The DJ-1 protein engages in diverse cellular and pathological processes, including tumorigenesis, apoptosis, sperm fertilization, and the progression of Parkinson's disease (PD). The functional dimeric form of DJ-1 transforms into non-functional filamentous aggregates in an inorganic phosphate (Pi)-dependent manner in vitro. Here, we demonstrated that Pi and reactive oxygen species (ROS) induce DJ-1 aggregation in Neuro2A and SH-SY5Y cells. Remarkably, tartrate treatment significantly reduced Pi- and ROS-induced DJ-1 aggregation and restored Pi- and ROS-provoked cell death using quantitative data as mean±standard deviation, and statistics. Mechanistically, tartrate prevented DJ-1 aggregation via occupying the Pi-binding site. These findings revealed an unexpected physiological role of tartrate in the maintenance of DJ-1 function, and thus, a potential use as an inhibitor of DJ-1 aggregation.