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Voriconazole-d3

(Synonyms: VRC-d3) 目录号 : GC48254

具有多种生物活性的神经肽

Voriconazole-d3 Chemical Structure

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500 μg
¥2,381.00
现货
1 mg
¥4,283.00
现货

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产品描述

Voriconazole-d3 is intended for use as an internal standard for the quantification of voriconazole by GC- or LC-MS. Voriconazole is a triazole antifungal agent and a derivative of fluconazole .[1],[2] It is active against a variety of yeast and fungi, including clinical isolates of A. flavus, A. fumigatus, F. oxysporum, F. solani, C. albicans, and C. neoformans (MICs = 1 Voriconazole is also active against 56 clinical isolates of fluconazole-resistant C. albicans (MICs = 0.015-8 µg/ml).[2] It inhibits ergosterol biosynthesis in C. albicans, C. glabrata, A. fumigatus, and A. flavus (IC50s = 0.03-1 µg/ml).[3] Voriconazole (10 mg/kg twice per day, i.v.) decreases the number of lung colony-forming units (CFUs), reduces alveolar collapse and lung inflammatory cell infiltration and necrosis, and increases survival in a rat model of invasive pulmonary aspergillosis.[4] Formulations containing voriconazole have been used in the treatment of fungal infections.

Reference:
[1].Espinel-Ingroff, A.In vitro activity of the new triazole voriconazole (UK-109,496) against opportunistic filamentous and dimorphic fungi and common and emerging yeast pathogensJ. Clin. Microbiol.36(1)198-202(1998)
[2].Cuenca-Estrella, M., DÍaz-Guerra, T.M., Mellado, E., et al.Comparative in vitro activity of voriconazole and itraconazole against fluconazole-susceptible and fluconazole-resistant clinical isolates of Candida species from SpainEur. J. Clin. Microbiol. Infect. Dis.18(6)432-435(1999)
[3].Munayyer, H.K., Mann, P.A., Chau, A.S., et al.Posaconazole is a potent inhibitor of sterol 14α-demethylation in yeasts and moldsAntimicrob. Agents Chemother.48(10)3690-3696(2004)
[4].Zhang, M., Su, X., Sun, W.-K., et al.Efficacy of the combination of voriconazole and caspofungin in experimental pulmonary aspergillosis by different Aspergillus speciesMycopathologia177(1-2)11-18(2014)

Chemical Properties

Cas No. N/A SDF
别名 VRC-d3
化学名 (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoropyrimidin-4-yl)-1-(1H-1,2,4-triazol-1-yl)butan-4,4,4-d3-2-ol
Canonical SMILES FC1=CN=CN=C1[C@@H]([C@](O)(CN2N=CN=C2)C3=C(C=C(C=C3)F)F)C([2H])([2H])[2H]
分子式 C16H11D3F3N5O 分子量 352.3
溶解度 DMSO: 20 mg/ml,Ethanol: 20 mg/ml 储存条件 Store at -20°C
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1 mg 5 mg 10 mg
1 mM 2.8385 mL 14.1924 mL 28.3849 mL
5 mM 0.5677 mL 2.8385 mL 5.677 mL
10 mM 0.2838 mL 1.4192 mL 2.8385 mL
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Research Update

Simultaneous Determination of Voriconazole and Its Voriconazole N-Oxide Metabolite in Human Urine by Liquid Chromatography/Tandem Mass Spectrometry

J Chromatogr Sci 2022 Oct 3;60(8):800-806.PMID:34761250DOI:10.1093/chromsci/bmab126

A convenient and sensitive liquid chromatography-tandem mass spectrometry method was established to simultaneously quantify voriconazole (VRZ) and its metabolite, voriconazole N-oxide (VNO), in human urine. Voriconazole-d3 and Voriconazole-d3 N-oxide were used as isotopic internal standards. Samples were processed by protein precipitation and separated using a ZORBAX SB-Aq column (1.8 μm, 2.1 × 50 mm). Mass spectrometry was performed using an API 4000 mass spectrometry by positive electrospray ionization. The flow rate was 0.6 mL/min. Gradient elution was performed with methanol and 0.1% formic acid as the organic and water phase, respectively. The VRZ and VNO calibration curves ranged from 20.0 to 7200 ng/mL in human urine. The specificity, matrix effect, extraction recovery, intra/inter-run precision, accuracy and stability were validated for both VRZ and VNO in human urine. The developed method was used to study urinary excretion after intravenous injection of 4 mg/kg VRZ in healthy Chinese subjects.