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3,4-Dehydro Cilostazol Sale

(Synonyms: 西洛他唑杂质B,OPC-13015) 目录号 : GC39841

An active metabolite of cilostazol

3,4-Dehydro Cilostazol Chemical Structure

Cas No.:73963-62-9

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10mM (in 1mL DMSO)
¥1,287.00
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5mg
¥1,170.00
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10mg
¥2,205.00
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50mg
¥4,860.00
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100mg
¥8,280.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

3,4-dehydro Cilostazol is an active metabolite of the PDE3A inhibitor cilostazol .1,2 It is formed from cilostazol by the cytochrome P450 (CYP) isoforms CYP3A4 and CYP2C19.

1.Suri, A., Forbes, W.P., and Bramer, S.L.Effects of CYP3A inhibition on the metabolism of cilostazolClin. Pharmacokinet.37(Suppl 2)61-68(1999) 2.Liu, Y., Shakur, Y., Yoshitake, M., et al.Cilostazol (pletal): A dual inhibitor of cyclic nucleotide phosphodiesterase type 3 and adenosine uptakeCardiovasc. Drug Rev.19(4)369-386(2001)

Chemical Properties

Cas No. 73963-62-9 SDF
别名 西洛他唑杂质B,OPC-13015
Canonical SMILES O=C1NC2=C(C=C(OCCCCC3=NN=NN3C4CCCCC4)C=C2)C=C1
分子式 C20H25N5O2 分子量 367.44
溶解度 DMSO: 5 mg/mL (13.61 mM) 储存条件 Store at -20°C
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1 mM 2.7215 mL 13.6077 mL 27.2153 mL
5 mM 0.5443 mL 2.7215 mL 5.4431 mL
10 mM 0.2722 mL 1.3608 mL 2.7215 mL
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Research Update

Determination of cilostazol and its active metabolite 3,4-Dehydro Cilostazol from small plasma volume by UPLC-MS/MS

J Pharm Anal 2015 Feb;5(1):1-11.PMID:29403909DOI:10.1016/j.jpha.2014.08.001.

A simple, rapid and sensitive ultra performance liquid chromatography-tandem mass spectrometry (UPLC-MS/MS) method has been developed for the simultaneous determination of cilostazol and its pharmacologically active metabolite 3,4-Dehydro Cilostazol in human plasma using deuterated analogs as internal standards (ISs). Plasma samples were prepared using solid phase extraction and chromatographic separation was performed on UPLC BEH C18 (50 mm×2.1 mm, 1.7 µm) column. The method was established over a concentration range of 0.5-1000 ng/mL for cilostazol and 0.5-500 ng/mL for 3,4-Dehydro Cilostazol. Intra- and inter-batch precision (% CV) and accuracy for the analytes were found within 0.93-1.88 and 98.8-101.7% for cilostazol and 0.91-2.79 and 98.0-102.7% for the metabolite respectively. The assay recovery was within 95-97% for both the analytes and internal standards. The method was successfully applied to support a bioequivalence study of 100 mg cilostazol in 30 healthy subjects.

Effect of Baicalein on the Pharmacokinetics of Cilostazol and Its Two Metabolites in Rat Plasma Using UPLC-MS/MS Method

Front Pharmacol 2022 Apr 27;13:888054.PMID:35571101DOI:10.3389/fphar.2022.888054.

This study aimed to explore the effect of baicalein on the pharmacokinetics of cilostazol (CLZ) and its two metabolites 3,4-Dehydro Cilostazol (3,4-CLZ) and 4'-trans-hydroxy cilostazol (4'-CLZ) in rats using a newly established ultra performance liquid chromatography tandem mass spectrometry (UPLC-MS/MS) method. Ticagrelor was used as an internal standard (IS), then cilostazol and its two metabolites were separated by means of a UPLC BEH C18 column (2.1 mm × 50 mm, 1.7 μm) using gradient elution method with 0.4 ml/min of flow rate. Acetonitrile as organic phase and water with 0.1% formic acid as aqueous phase constructed the mobile phase. Selective reaction monitoring (SRM) mode and positive ion mode were preferentially chosen to detect the analytes. Twelve SD rats were divided into two groups (n = 6) when CLZ was administered orally (10 mg/kg) with or without oral baicalein (80 mg/kg). The selectivity, linearity, recovery, accuracy, precision, matrix effect and stability of UPLC-MS/MS assay were satisfied with the standards of United States Food and Drug Administration guidelines. In control group, AUC0-∞ and Cmax of CLZ were 2,169.5 ± 363.1 ng/ml*h and 258.9 ± 82.6 ng/ml, respectively. The corresponding results were 3,767.6 ± 1,049.8 ng/ml*h and 308.6 ± 87.9 ng/ml for 3, 4-CLZ, 728.8 ± 189.9 ng/ml*h and 100.3 ± 51.3 ng/ml for 4'-CLZ, respectively. After combination with baicalein, AUC0-∞ and Cmax of CLZ were 1.48, 1.38 times higher than the controls. Additionally, AUC0-∞ and Cmax were separately decreased by 36.12 and 19.54% for 3,4-CLZ, 13.11 and 44.37% for 4'-CLZ. Baicalein obviously alters the pharmacokinetic parameters of CLZ, 3,4-CLZ and 4'-CLZ in rats. These results suggested that there was a potential drug-drug interaction between baicalein and CLZ. Therefore, it must raise the awareness when concomitant use of CLZ with baicalein, the dosage regimen of CLZ should be taken into consideration, if this result is confirmed in clinical studies.

A new simple method for quantification of cilostazol and its active metabolite in human plasma by LC-MS/MS: Application to pharmacokinetics of cilostazol associated with CYP genotypes in healthy Chinese population

Biomed Chromatogr 2021 Oct;35(10):e5150.PMID:33894005DOI:10.1002/bmc.5150.

A simple, sensitive, and fully automated liquid chromatography-tandem mass spectrometry (LC-MS/MS) method was developed and validated for the simultaneous quantification of cilostazol (CIL) and its active metabolite, 3,4-Dehydro Cilostazol (CIL-M), in human plasma. Plasma samples were processed by protein precipitation in 2 mL 96-deep-well plates, and all liquid transfer steps were performed through robotic liquid handling workstation, enabling the whole procedure fast, compared to the reported methods. Separation of analytes was successfully achieved on a UPLC BEH C18 column (2.1 × 100 mm, 1.7 μm) with mobile phase A (5 mM ammonium formate containing 0.1% formic acid) and mobile phase B (methanol) at a flow rate of 0.30 mL min-1 . The total run time was 3.5 min per sample. Mass spectrometric detection was conducted by electrospray ion source in positive ion multiple reaction monitoring mode. Calibration curves were linear over the concentration range of 1.0-800 ng·mL-1 for CIL and 0.05-400 ng·mL-1 for CIL-M. The coefficient of variation for the assay's precision was 12.3%, and the accuracy was 88.8-99.8%. It was fully validated and successfully applied to assess the influence of CYP genotypes on the pharmacokinetics of CIL after oral administration of 50 mg tablet formulations of CIL to healthy Chinese volunteers. The results suggest that, in Chinese population, the genotype of CYP3A5 affects the plasma exposure of CIL.