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Posaconazole

Posaconazole

产品编号 T6211   CAS 171228-49-2
别名: 泊沙康唑, SCH 56592, POS

Posaconazole (POS) 是一种甾醇 C14ɑ 去甲基化酶的三唑类广谱抑制剂,IC50值为 0.25 nM,具有抗真菌作用。

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Posaconazole Chemical Structure
Posaconazole, CAS 171228-49-2
规格 价格/CNY 货期 数量
1 mg ¥ 296 现货
2 mg ¥ 416 现货
5 mg ¥ 655 现货
10 mg ¥ 985 现货
25 mg ¥ 1,980 现货
50 mg ¥ 3,950 现货
100 mg ¥ 5,630 现货
1 mL * 10 mM (in DMSO) ¥ 896 现货
其他形式的 Posaconazole:
产品目录号及名称: Posaconazole (T6211)
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纯度: 100%
纯度: 99.93%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Posaconazole (POS) is a sterol C14ɑ demethylase inhibitor (IC50: 0.25 nM).
靶点活性 C14ɑ demethylase:0.25 nM
体外活性 Posaconazole的生物利用度可被食物,尤其是高脂肪膳食显著增加.与高脂和脱脂食物一起消耗时,全身接触Posaconazole分别增加其4倍和2.6倍的消耗.Posaconazole(≥15 mg/kg,b.i.d)可使小鼠寿命延长,并减少组织负担.在感染的动物中,胺碘酮单独使用可减少寄生虫血症,增加60天生存期(未处理的对照组为0%,胺碘酮处理的动物为40%),与Posaconazole联用可延缓寄生虫血症的进程.Posaconazole 和胺碘酮可能产生有效的抗T. cruzi治疗,且副作用低.在禁食状态,Posaconazole与Boost Plus同时服用增加药物暴露.
体内活性 Posaconazole对临床相关的细胞内无鞭毛体寄生虫形式的效能更好。Posaconazole的最低抑菌浓度和IC50值分别为3 nM和0.25 nM。Posaconazole对耐氟康唑、伏立康唑和两性霉素B的念珠菌和曲霉菌株具有活性,且效果比其它三唑类抗接合菌药更好。胺碘酮与Posaconazole可产生协同效果。Posaconazole还会影响并打乱T. cruzi 中Ca2+内稳态。Posaconazole对前鞭体(细胞外)阶段的增殖具有明显的剂量依赖性作用,最低抑菌浓度为20 nM,IC50为14 nM。
激酶实验 In vitro Aβ reduction assays : Human embryonic kidney cells (American Type Culture Collection CRL-1573), transfected with the gene for APP751 (HEK 293) are used for routine Aβ reduction assays. Cells are plated in 96-well plates and allowed to adhere overnight in Dulbecco's modified Eagle medium (DMEM) supplemented with 10% heat-inactivated fetal bovine serum. DAPT are diluted from stock solutions in dimethylsulfoxide (DMSO) to yield a final concentration equal to 0.1% DMSO in media. Cells are pre-treated for 2 hours at 37 °C with DAPT, media are aspirated off and fresh compound solutions applied. After an additional 2-hour treatment period, conditioned media is drawn off and analyzed by a sandwich ELISA (266–3D6) specific for total Aβ. Reduction of Aβ production is measured relative to control cells treated with 0.1% DMSO and expressed as a percentage inhibition. Data from at least six doses in duplicate are fitted to a four-parameter logistical model using XLfit software in order to determine potency. Human and PDAPP mouse neuronal cultures are grown in serum-free media to enhance their neuronal characteristics, and appeared to be greater than 90% neurons after maturation prior to use. Conditioned media to establish baseline Aβ values are collected by adding fresh media to each well and incubated for 24 hours at 37 °C in the absence of DAPT. Cultures are then treated with fresh media containing DAPT at the desired range of concentrations for an additional 24 hours at 37 °C, and conditioned media collected. For the measurement of total Aβ, samples are analyzed with the same ELISA (266–3D6) as used for the HEK 293 cell assays. Analyses of samples for Aβ42 production are performed by a separate ELISA (21F12–3D6) that utilizes a capture antibody specific for the Aβ42 C-terminus. Inhibition of production for both total Aβ and Aβ42 are determined by the difference between the values for the compound treatment and baseline periods.After plotting percentage inhibition versus DAPT concentration, data are analyzed with XLfit software, as above, to determine potency.
细胞实验 The epimastigote form of the parasite is cultivated in liver infusion tryptose medium,supplemented with 10% new born calf serum at 28 °C with strong (120 rpm) agitation.Cultures are initiated at a cell density of 2 × 106 epimastigotes/mL,and Posaconazole is added at a cell density of 0.5−1.0 × 107 epimastigotes/mL.Cell densities are measured by using an electronic particle counter as well as by direct counting with a hemocytometer.Cell viability is followed by Trypan blue exclusion,using light microscopy.Amastigotes are cultured in Vero cells maintained in minimal essential medium supplemented with 1% fetal calf serum in a humidified atmosphere (95% air−5% CO2) at 37 °C.Cells are infected with 10 tissue culture-derived trypomastigotes per cell for 2 hours and then washed three times with phosphate-buffered saline (PBS) to remove nonadherent parasites.Fresh medium with and without Posaconazole is added,and the cells are incubated for 96 hours with a medium change at 48 hours.The percent of infected cells and the numbers of parasites per cell are determined directly using light microscopy,and a statistical analysis of the results is carried out.IC50 values are calculated by nonlinear regression,using the program GraFit.Fractional inhibitory concentrations (FIC) are calculated.Cytoplasmic free Ca2+ concentrations in control and drug-treated extracellular epimastigotes are determined by fluorimetric methods using Fura-2.Subcellular Ca2+ levels and mitochondrial membrane potentials are monitored on individual Vero cells infected with T.cruzi amastigotes by using time-scan confocal microscopy.Briefly,Vero cells heavily infected (72 hours) with T.cruzi amastigotes are plated onto 22 × 40 mm glass coverslips (0.15 mm thickness) and incubated simultaneously with 10 μM cell-permeant Rhod-2 and 10 μg/mL Rhodamine-123 for 50 minutes at 37 °
别名 泊沙康唑, SCH 56592, POS
分子量 700.78
分子式 C37H42F2N8O4
CAS No. 171228-49-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

DMSO: 93 mg/mL (132.7 mM)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.427 mL 7.1349 mL 14.2698 mL 35.6745 mL
5 mM 0.2854 mL 1.427 mL 2.854 mL 7.1349 mL
10 mM 0.1427 mL 0.7135 mL 1.427 mL 3.5675 mL
20 mM 0.0713 mL 0.3567 mL 0.7135 mL 1.7837 mL
50 mM 0.0285 mL 0.1427 mL 0.2854 mL 0.7135 mL
100 mM 0.0143 mL 0.0713 mL 0.1427 mL 0.3567 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Benaim G, et al. J Med Chem. 2006, 49(3), 892-389. 2. Sabatelli F, et al. Antimicrob Agents Chemother. 2006, 50(6), 22009-22015. 3. Sansone-Parsons A, et al. Antimicrob Agents Chemother. 2006, 50(5), 1881-1883. 4. Veiga-Santos P, et al. Int J Antimicrob Agents. 2012, 40, 61-71. 5. Sun QN, et al. Antimicrob Agents Chemother. 2002, 46(7), 2310-2312.
Zinc pyrithione Nerol Deacylketoconazole Oenothein B Caulilexin C alpha-Mangostin Clioquinol Rapamycin

相关化合物库

该产品包含在如下化合物库中:
抗感染化合物库 含氟化合物库 抗生素库 抗真菌库 肝脏毒性化合物库 口服活性化合物库 ReFRAME 相关化合物库 共价抑制剂库 抗COVID-19化合物库 临床期小分子药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Posaconazole 171228-49-2 Microbiology/Virology Antifungal Inhibitor SCH56592 inhibit 泊沙康唑 SCH 56592 POS SCH-56592 Fungal inhibitor

 

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