4-Methylamino antipyrine hydrochloride
(Synonyms: 安乃近杂质C) 目录号 : GC60523An active metabolite of metamizole
Cas No.:856307-27-2
Sample solution is provided at 25 µL, 10mM.
4-Methylaminoantipyrine is a major active metabolite of the non-opioid prodrug metamizole .1 It is formed from metamizole by non-enzymatic hydrolysis in the gastrointestinal tract.2 4-Methylaminoantipyrine (0.1 mM) inhibits production of prostaglandin E2 induced by the calcium ionophore A23187 in isolated mouse peritoneal macrophages.3 It increases the paw withdrawal threshold in a rat model of carrageenan-induced hyperalgesia when administered at a dose of 160 ?g/paw.4 4-Methylaminoantipyrine (60, 90, and 120 mg/kg) reduces LPS-induced pyrexia in rats.5 It is also a potential impurity found in commercial preparations of metamizole.6
1.Rogosch, T., Sinning, C., Podlewski, A., et al.Novel bioactive metabolites of dipyrone (metamizol)Bioorg. Med. Chem.20(1)101-107(2012) 2.Nikolova, I., Tencheva, J., Voynikov, Y., et al.Metamizole: A review profile of a well-known “forgotten” drug. Part I: Pharmaceutical and nonclinical profileBiotechnol. Biotechnol. Equip.26(6)3329-3337(2012) 3.Brune, K., Aehringhaus, U., and Peskar, B.A.Pharmacological control of leukotriene and prostaglandin production from mouse peritoneal macrophagesAgents Actions14(5-6)729-734(1984) 4.Gon?alves Dos Santos, G., Vieira, W.F., Vendramini, P.H., et al.Dipyrone is locally hydrolyzed to 4-methylaminoantipyrine and its antihyperalgesic effect depends on CB2 and κ-opioid receptors activationEur. J. Pharmacol.874173005(2020) 5.Malvar, D.d.C., Aguiar, F.A., Vaz Ade, L., et al.Dipyrone metabolite 4-MAA induces hypothermia and inhibits PGE2 -dependent and -independent fever while 4-AA only blocks PGE2 -dependent feverBr. J. Pharmacol.171(15)3666-3679(2014) 6.Vieira, J.C., Sversut, R.A., Maciel, I.T., et al.HPLC–DAD method for simultaneous determination of dipyrone (metamizole) and caffeine in tablets and identification of major degradation product by direct infusion ESI–MSChromatographia80(3)489–495(2017)
Cas No. | 856307-27-2 | SDF | |
别名 | 安乃近杂质C | ||
Canonical SMILES | O=C1N(C2=CC=CC=C2)N(C)C(C)=C1NC.[H]Cl | ||
分子式 | C12H16ClN3O | 分子量 | 253.73 |
溶解度 | 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 | 3.9412 mL | 19.706 mL | 39.412 mL |
5 mM | 0.7882 mL | 3.9412 mL | 7.8824 mL |
10 mM | 0.3941 mL | 1.9706 mL | 3.9412 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet