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1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEIsavuconazoleCat. No.: HY-14273CAS No.: 241479-67-4Synonyms: BAL-4815; RO-0094815分式: CHFNOS分量: 437.47作靶点: Fungal; Cytochrome P450作通路: Anti-infection; Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 m

2、onths-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (114.29 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.2859 mL 11.4294 mL 22.8587 mL5 mM 0.4572 mL 2.2859 mL 4.5717 mL10 mM 0.2286 mL 1.1429 mL 2.2859 mL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,并请注意储备液的保存式和期限。体内实验请根据您的实验

3、动物和给药式选择适当的溶解案,配制前请先配制澄清的储备液,再依次添加助溶剂(为保证实验结果的可靠性,体内实验的作液,建议您现现配,当天使;澄清的储备液可以根据储存条件,适当保存;以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占):1. 请依序添加每种溶剂: 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 3 mg/mL (6.86 mM); Clear solution2. 请依序添加每种溶剂: 10% DMSO 90% (20% SBE-CD in saline)Solubility: 3 mg/mL (6.86 mM); Cle

4、ar solution1/2 Master of Small Molecules 您边的抑制剂师www.MedChemE3. 请依序添加每种溶剂: 10% DMSO 90% corn oilSolubility: 3 mg/mL (6.86 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 Isavuconazole种溶的苯三唑,具有抗真 作,同时也是CYP3A4 的温和抑制剂。体外研究 Isavuconazole shows good activity against all Candida spp., with active MIC50 of 0.004

5、mg/L. TheMIC50s/MIC90s range from 0.002/0.004 mg/L for C. albicans to 0.25/0.5 mg/L for C. glabrata 1.Isavuconazole has potent in vitro activity against most common Aspergillus species, Purpureocilliumlilacinum, and Scedosporium apiospermum 2. Isavuconazole shows potent activity against molds, yeast

6、s,and dimorphic fungi. Rhizopus isolates have MIC values to isavuconazole as low as 0.12 g/mL with othersas high as 32 g/mL 3. In the study of pharmacokinetics and pharmacodynamics of isavuconazole againstthe GFP transformant, F/11628, NIH 4215, and F/16216, the modal MICs of isavuconazole are 1, 8,

7、 1, 4mg/L, respectively 4.户使本产品发表的科研献 Drug Metab Dispos. 2019 May 8. pii: dmd.118.085993.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Seifert H, et al. In vitro activities of isavuconazole and other antifungal agents against Candida bloodstream isolates. Antimicrob AgentsChe

8、mother. 2007 May;51(5):1818-21.2. Steinmann J, et al. In Vitro Activity of Isavuconazole against Rasamsonia Species. Antimicrob Agents Chemother. 2016 Oct21;60(11):6890-6891.3. Donnelley MA, et al. Isavuconazole in the treatment of invasive aspergillosis and mucormycosis infections. Infect Drug Resist. 2016 Jun2;9:79-86.4. Box H, et al. Pharmacodynamics of Isavuconazole in a Dynamic In Vitro Model of Invasive Pulmonary Aspergillosis. Antimicrob AgentsChemother. 2015 Oct 26;60(1):278-87.McePdfHeightCaution: Product has not been fully validated for medical ap

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