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Mebeverine acid Sale

(Synonyms: 美贝维林盐酸盐,Mebeverine metabolite Mebeverine acid) 目录号 : GC61037

A metabolite of mebeverine

Mebeverine acid Chemical Structure

Cas No.:475203-77-1

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1mg
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Sample solution is provided at 25 µL, 10mM.

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产品描述

Mebeverine acid is a metabolite of the antispasmodic agent mebeverine.1

1.Moskaleva, N.E., Baranov, P.A., Mesonzhnik, N.V., et al.HPLC-MS/MS method for the simultaneous quantification of desmethylmebeverine acid, mebeverine acid and mebeverine alcohol in human plasma along with its application to a pharmacokinetics studyJ. Pharm. Biomed. Anal.138118-125(2017)

Chemical Properties

Cas No. 475203-77-1 SDF
别名 美贝维林盐酸盐,Mebeverine metabolite Mebeverine acid
Canonical SMILES O=C(O)CCCN(CC)C(C)CC1=CC=C(OC)C=C1
分子式 C16H25NO3 分子量 279.37
溶解度 DMSO : 13.33 mg/mL (47.71 mM; Need ultrasonic) 储存条件 Store at -20°C
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1 mM 3.5795 mL 17.8974 mL 35.7948 mL
5 mM 0.7159 mL 3.5795 mL 7.159 mL
10 mM 0.3579 mL 1.7897 mL 3.5795 mL
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Research Update

Identification of Mebeverine acid as the main circulating metabolite of mebeverine in man

J Pharm Biomed Anal 2002 Jun 20;29(1-2):335-40.PMID:12062694DOI:10.1016/s0731-7085(02)00023-7.

The intestinal spasmolytic drug mebeverine is known to undergo fast in vivo enzymatic hydrolysis into mebeverine alcohol and veratric acid. A reversed-phase HPLC method with coulometric detection was developed in order to assay the hitherto unidentified secondary metabolite Mebeverine acid. After intake of a single oral dose of 405 mg mebeverine hydrochloride in four healthy human volunteers, peak plasma concentrations of Mebeverine acid were found to be 1000-fold higher than those of mebeverine alcohol, i.e. approximately 3 microg/ml versus 3 ng/ml. The appearance of Mebeverine acid in plasma (median T(max)=1.25 h) as well as its disappearance (median apparent t(1/2)=1.1 h) were rapid. The urinary excretion of Mebeverine acid within the first 4 h after dosing amounted to 67% of the mebeverine dose (median range: 23-107%). Mebeverine acid appears to be a valuable marker of oral exposure to mebeverine.

HPLC-MS/MS method for the simultaneous quantification of desmethylmebeverine acid, Mebeverine acid and mebeverine alcohol in human plasma along with its application to a pharmacokinetics study

J Pharm Biomed Anal 2017 May 10;138:118-125.PMID:28192719DOI:10.1016/j.jpba.2017.02.006.

A new simple, rapid and sensitive high pressure liquid chromatography-tandem mass spectrometry (HPLC-MS/MS) method was developed and validated for simultaneous analysis of mebeverine metabolites as: mebeverine alcohol (MAL), Mebeverine acid (MAC) and desmethylmebeverine acid (DMAC) in human plasma. Sample preparation was performed by protein precipitation following the separation of analytes using an Acquity UPLC BEN C8 column 1.7 mm 2.1×50mm (Waters, USA). 2H5-desmethylmebeverine acid (2H5-DMAC) was used as the internal standard (IS). The proposed method was validated with linear ranges of 0.1-10ng/mL; 1-100ng/mL and 5-1000ng/mL for MAL, MAC and DMAC, respectively. Accuracy for all analytes (%RE), given as deviation between nominal and measured concentration and assay variability (CV) ranged from -4.04% to 4.60% and from 0.31% to 6.43% respectively both for within- and between-run. The overall recoveries for all metabolites were above 85%. The proposed method was used successfully for analysis of real samples from a pharmacokinetics study.

Use of polarity switching for the simultaneous bioanalysis of analytes with three orders of magnitude difference in concentration by LC-MS/MS

Bioanalysis 2013 Aug;5(15):1911-8.PMID:23905864DOI:10.4155/bio.13.142.

Background: The challenge of quantifying two compounds in a single assay with drastic dynamic ranges is to obtain linearity without source or detector saturation at the mass spectrometer. Results: In positive-ionization mode, the nonlinear relationships for Desmethyl Mebeverine acid (DMAC) were demonstrated using three common strategies to overcome this issue: using offset voltage parameters, less-sensitive product ion or 13C mass SRM transitions. On the contrary, nonlinear relationships for DMAC were overcome if negative-ionization mode was used. Due to Mebeverine analytical LLOQ, dilution was not suitable for a single assay of Mebeverine and DMAC. However, polarity switching in negative mode for DMAC was successfully found to compensate for the nonlinearity at the mass spectrometer while preserving Mebeverine linear regression model in positive mode. Conclusion: The polarity switching strategy has demonstrated the advantage of improving linearity for analytes having different ionization polarities and three orders of magnitude difference in concentration.