| 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% |
| ALogP | 4.6 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC[C@@H]([C@H](C)O)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OC[C@H]5C[C@](OC5)(CN6C=NC=N6)C7=C(C=C(C=C7)F)F |
| 分子量 | 700.78 |
| Reaxy-Rn | 13602110 |
| Reaxys-RN link address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=13602110&ln= |
| 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); |
|---|---|
| 比旋光度 | -26° (C=1,CHCl3) |
| 熔点 | 169 °C |
| 象形图 | GHS08, GHS09, GHS07 |
|---|---|
| 信号词 | Danger |
| 危险声明 |
H319: 引起严重眼睛刺激 H351: 怀疑引起遗传缺陷 H400: 对水生生物有剧毒 H410: 对水生生物有剧毒并具有长期持续影响 H372: 通过长时间或反复暴露对器官造成损害 H361: 怀疑破坏生育力或未出生的孩子 |
| 预防措施声明 |
P305+P351+P338: 如进入眼睛：用水小心冲洗几分钟。如戴隐形眼镜并可方便地取出，取出隐形眼镜。继续冲洗。 P273: 避免释放到环境中。 P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。 P405: 密闭存放 P501: 将内容物/容器处理到。。。 P264: 处理后要彻底洗手。 P260: 不要吸入灰尘/烟雾/气体/雾/蒸汽/喷雾。 P270: 使用本产品时，请勿进食、饮水或吸烟。 P391: 收集溢出物 P203: 使用前，获取、阅读并遵守所有安全说明。 P264+P265: 处理后彻底洗手[和…]。不要触摸眼睛。 P318: 如果暴露或担心，请就医。 P337+P317: 如果眼睛刺激持续：寻求医疗帮助。 P319: 如果你感到不适，请寻求医疗帮助。 |
| Merck Index | 7602 |
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