Chlorpheniramine-d6 (maleate)
(Synonyms: 马来酸氯苯那敏-D6,(R)-(-)-Chlorpheniramine maleate-d6; L-Chlorpheniramine maleate-d6) 目录号 : GC49652
An internal standard for the quantification of chlorpheniramine
Cas No.:1219806-45-7
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
Chlorpheniramine-d6 is intended for use as an internal standard for the quantification of chlorpheniramine by GC- or LC-MS. Chlorpheniramine is a histamine H1 receptor antagonist with an IC75 value of 0.0016 μg/ml for reversal of histamine-induced spasms in isolated guinea pig ileum.1 It protects against intravenous histamine-induced death (PD50 = 0.15 mg/kg) and delays induction of aerosolized histamine-induced coughing (ED100sec = 0.44 mg/kg) in guinea pigs. Chlorpheniramine (20 mg/kg, i.p.) prevents histamine-induced passive cutaneous anaphylaxis (PCA) in rabbits.2 It also reduces respiratory resistance and hypersecretion of tracheobronchial fluid in a dog model of histamine-induced asthma.3 Formulations containing chlorpheniramine have been used in the treatment of seasonal allergies.
1.Lish, P.M., Robbins, S.I., and Peters, E.L.Specificity of antihistamine drugs and involvement of the adrenergic system in histamine deaths in the guinea pigJ. Pharmacol. Exp. Ther.153(3)538-543(1966) 2.Henson, P.M., and Cochrane, C.G.Immunological induction of increased vascular permeability. I. A rabbit passive cutaneous anaphylactic reaction requiring complement, platelets, and neutrophilsJ. Exp. Med.129(1)153-165(1969) 3.Yamatake, Y., Sasagawa, S., Yanaura, S., et al.Involvement of histamine H1- and H2-receptors in induced asthmas in dogsJpn. J. Pharmacol.27(6)791-797(1977)
| Cas No. | 1219806-45-7 | SDF | Download SDF |
| 别名 | 马来酸氯苯那敏-D6,(R)-(-)-Chlorpheniramine maleate-d6; L-Chlorpheniramine maleate-d6 | ||
| Canonical SMILES | ClC(C=C1)=CC=C1C(CCN(C([2H])([2H])[2H])C([2H])([2H])[2H])C2=CC=CC=N2.OC(/C=C\C(O)=O)=O | ||
| 分子式 | C16H13ClD6N2 • C4H4O4 | 分子量 | 396.9 |
| 溶解度 | Methanol: slightly,Water: slightly | 储存条件 | -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 | 2.5195 mL | 12.5976 mL | 25.1953 mL |
| 5 mM | 0.5039 mL | 2.5195 mL | 5.0391 mL |
| 10 mM | 0.252 mL | 1.2598 mL | 2.5195 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。
Towards an antimicrobial 'microglove'
Sci Rep 2015 Nov 13;5:16679.PMID:26564815DOI:10.1038/srep16679.
A large proportion of hospital-related infections are acquired and spread due to the direct contacts between patients and healthcare workers. Accordingly, proper infection prevention measures, and especially hand hygiene, are key to limit the spread of infections in nosocomial settings. However, healthcare workers frequently experience difficulties in complying strictly to hand disinfection protocols. This study was therefore aimed at the development of a hand rub with antimicrobial activity that forms a protective film on the hand, a so-called microglove, in order to enhance hand hygiene. For this purpose, various co-polymer formulations consisting of different ratios of Polyvinylpyrrolidone (PVP) and a branched C20 derivatized maleate (M20) in combination with the known biocide benzalkonium chloride (BKC) were tested for their combined film-forming and antimicrobial activities. The results of a series of novel contamination and transmission assays show that a formulation of 80% PVP and 20% M20 co-polymer with 0.9% BKC fulfils the elementary requirements for an antimicrobial microglove.
Pressure-induced phase transition in Glycinium maleate crystal
Spectrochim Acta A Mol Biomol Spectrosc 2021 Dec 5;262:120076.PMID:34174678DOI:10.1016/j.saa.2021.120076.
The multicomponent glycinium maleate single crystal was grown by the slow evaporation method. The crystal was submitted to pressures ranging from 1 atm to 5.6 GPa and Raman spectroscopy was used as a spectroscopic probe. The modifications of relative intensity bands related to the lattice modes at 0.3 GPa were associated with rearrangements of hydrogen bonds. Moreover, between 1.7 and 4.8 GPa the Raman results indicate that the crystal experience a long structural phase transition, which was confirmed by PCA analysis. DFT calculations gave us more precision in the assignments of modes. The behavior of the internal modes under pressure showed that the maleic acid molecule undergoes greater modifications than glycine amino acid. All observed modifications were reversible when the pressure was released.
[Quantitative analysis of chlorpheniramine maleate in cough and cold drugs by ion-pair high-performance liquid chromatography for the simultaneous determination of chlorpheniramine and maleate]
Yakugaku Zasshi 1996 Apr;116(4):329-34.PMID:8709008DOI:10.1248/yakushi1947.116.4_329.
A simple, rapid and convenient chromatographic method, which permits the simultaneous determination of chlorpheniramine (CP) and maleate (MA), recently developed by the authors was applied to the analysis of chlorpheniramine maleate (CPM) in cough and cold drugs. In this method, a Capcell Pak C8 column and an isocratic mobile phase containing 15% methanol, 50 mM KH2PO4 and 5mM tetra-n-butylammonium phosphate as an ion-pair reagent were used. By using the mobile phase adjusted to pH 3.0 with orthophosphoric acid, fumaric acid, MA, CP, acetaminophen (paracetamol), caffeine, and m- and p-hydroxybenzoic acid as candidates for an internal standard were eluted separately within 17 min. Detection was carried out with UV detector at 215 nm. Under the same conditions, five other antihistamines analogous to CPM were also separated. The calibration graphs for CP and MA showed good linearity in the range of 0.5-10 nmol (0.195-3.9 micrograms) per 20 microliters injection, respectively. The proposed method was successfully applied to the simultaneous determination of CP and MA, i.e., CPM analysis, in commercial cough and cold drugs which pharmaceutical forms were tablet, granule and syrups.
Pharmaceutical salts of emoxypine with dicarboxylic acids
Acta Crystallogr C Struct Chem 2018 Jul 1;74(Pt 7):797-806.PMID:29973419DOI:10.1107/S2053229618007386.
New salt forms of the antioxidant drug emoxypine (EMX, 2-ethyl-6-methylpyridin-3-ol) with pharmaceutically acceptable maleic (Mlt), malonic (Mln) and adipic (Adp) acids were obtained {emoxypinium maleate, C8H12NO+·C4H3O4-, [EMX+Mlt], emoxypinium malonate, C8H12NO+·C3H3O4-, [EMX+Mln], and emoxypinium adipate, C8H12NO+·C6H9O4-, [EMX+Adp]} and their crystal structures determined. The molecular packing in the three EMX salts was studied by means of solid-state density functional theory (DFT), followed by QTAIMC (quantum theory of atoms in molecules and crystals) analysis. It was found that the major contribution to the packing energy comes from pyridine-carboxylate and hydroxy-carboxylate heterosynthons forming infinite one-dimensional ribbons, with [EMX+Adp] additionally stabilized by hydrogen-bonded C(9) chains of Adp- ions. The melting processes of the [EMX+Mlt] (1:1), [EMX+Mln] (1:1) and [EMX+Adp] (1:1) salts were studied and the fusion enthalpy was found to increase with the increase of the calculated lattice energy. The dissolution process of the EMX salts in buffer (pH 7.4) was also studied. It was found that the formation of binary crystals of EMX with dicarboxylic acids increases the EMX solubility by more than 30 times compared to its pure form.
Extending the shikimate pathway for microbial production of maleate from glycerol in engineered Escherichia coli
Biotechnol Bioeng 2021 May;118(5):1840-1850.PMID:33512000DOI:10.1002/bit.27700.
maleate is one of the most important unsaturated four-carbon dicarboxylic acids. It serves as an attractive building block in cosmetic, polymer, and pharmaceutical industries. Currently, industrial production of maleate relies mainly on chemical synthesis using benzene or butane as the starting materials under high temperature, which suffers from strict reaction conditions and low product yield. Here, we propose a novel biosynthetic pathway for maleate production in engineered Escherichia coli. We screened a superior salicylate 5-hydroxylase that can catalyze hydroxylation of salicylate into gentisate with high conversion rate. Then, introduction of salicylate biosynthetic pathway and gentisate ring cleavage pathway allowed the synthesis of maleate from glycerol. Further optimizations including enhancement of precursors supply, disruption of competing pathways, and construction of a pyruvate recycling system, boosted maleate titer to 2.4 ± 0.1 g/L in shake flask experiments. Subsequent scale-up biosynthesis of maleate in a 3-L bioreactor under fed-batch culture conditions enabled the production of 14.5 g/L of maleate, indicating a 268-fold improvement compared with the titer generated by the wildtype E. coli strain carrying the entire maleate biosynthetic pathway. This study provided a promising microbial platform for industrial level synthesis of maleate, and demonstrated the highest titer of maleate production in microorganisms so far.