| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| P409129-1ml |
1ml |
现货  |
|
| 英文别名 | 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-triazol-1-yl)methyl)-5-(2,4-difluorophenyl)-tetrahydrofuran-3-yl)methoxy)phenyl)piperazin-1-yl)phenyl)-2-((2S,3S)-2-hydroxypentan-3-yl)-2H-1,2,4-triazol-3(4H)-one |
|---|---|
| 规格或纯度 | Moligand™, 10mM in DMSO |
| 英文名称 | Posaconazole (SCH 56592) |
| 生化机理 | 泊沙康唑（SCH56592）主要是 CYP3A4 的抑制剂，但不抑制其他 CYP 酶的活性；也是甾醇 C14ɑ 去甲基化酶抑制剂，IC50 为 0.25 μM。泊沙康唑的中位终末消除半衰期为 15-35 小时。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 细胞色素 P450 51 抑制剂 |
| 产品介绍 |
Posaconazole 是甾醇C14ɑ去甲基化酶抑制剂，IC50为0.25 nM。A triazole anti-fungal Information Posaconazole (SCH56592) is an inhibitor primarily ofCYP3A4, but it does not inhibit the activity of other CYP enzymes; Also an inhibitor ofsterol C14ɑ demethylaseinhibitor with IC50 of 0.25 μM. Posaconazole has a median terminal elimination half-life of 1 Posaconazole has potent trypanocidal activity. Amiodarone acts synergistically with Posaconazole. Posaconazole also affects and disrupts Ca2+ homeostasis in T. cruzi. Posaconazole blocks the biosynthesis of ergosterol, which is essential for parasite survival. Posaconazole has a clear, dose-dependent effect on proliferation of the epimastigote (extracellular) stages, with a minimal inhibitory concentration of 20 nM and an IC50 of 14 nM. Against the clinically relevant intracellular amastigote form of the parasite, Posaconazole is even more potent. Posaconazole has the minimal inhibitory concentration and IC50 values of 3 nM and 0.25 nM. Posaconazole is active against isolates of Candida and Aspergillus spp. that exhibit resistance to Fluconazole, Voriconazole, and Amphotericin B and is much more active than the other triazoles against zygomycetes. In vivo Treatment of infected animals with amiodarone alone reduces parasitemia, increases survival 60 days pi (0% for untreated controls vs 40% for amiodarone-treated animals) and, when given in combination with Posaconazole, delays the development of parasitemia. Coadministration of Posaconazole and Boost Plus increases drug exposure compared to the administration of Posaconazole alone in the fasted state. Food, particularly meals high in fat content, significantly increases Posaconazole bioavailability. Systemic exposure to Posaconazole increases 4- and 2.6-fold when it is consumed with a high-fat and nonfat meal, respectively. Posaconazole and Amiodarone may constitute an effective anti-T. cruzi therapy with low side effect. At twice-daily doses of ≥15 mg/kg of body weight, Posaconazole prolongs the survival of the mice and reduces tissue burden. cell lines： Concentrations：0 nM -4 nM Incubation Time：96 hours Powder Purity:≥99% |
| 分子类型 | 小分子 |
|---|---|
| Canonical SMILES | CCC(C(C)O)N1N=CN(C1=O)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(OCC5COC(C5)(C[N]6C=NC=N6)C7=CC=C(F)C=C7F)C=C4 |
| 分子量 | 700.78 |
| 溶解性 | Solubility (25°C) In vitro DMSO: 57 mg/mL (200.48 mM); Water: 57 mg/mL (200.48 mM); Ethanol: 57 mg/mL (200.48 mM); |
|---|
| Concentration | 9-11（mmol/L） |
|---|---|
| Proton NMR spectrum | Conforms to Structure |
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