Posaconazole
别名: SCH 56592, POS 中文名称：泊沙康唑
Posaconazole是CYP3A4的抑制剂，但不抑制其他CYP酶的活性；同时是sterol C14ɑ demethylase的抑制剂，IC50为0.25 μM。其平均的消除半衰期为15-35小时。
Posaconazole Chemical Structure
CAS: 171228-49-2
产品质控
批次：
纯度：
99.97%
99.97
Posaconazole相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| BESM | Function assay | 5 uM | 72 hrs | Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi epimastigotes infected in BESM cells assessed as accumulation of lanosterol and eburicol precursors at 5 uM after 72 hrs | 20385875 |
| BESM | Function assay | 5 uM | 72 hrs | Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi epimastigotes infected in BESM cells assessed as reduction in episterol content at 5 uM after 72 hrs | 20385875 |
| BESM | Function assay | 5 uM | 72 hrs | Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi epimastigotes infected in BESM cells assessed as reduction in fecosterol content at 5 uM after 72 hrs | 20385875 |
| BESM | Function assay | 5 uM | 72 hrs | Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi amastigotes infected in BESM cells assessed as accumulation of lanosterol and eburicol precursors at 5 uM after 72 hrs | 20385875 |
| BESM | Function assay | 5 uM | 72 hrs | Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi amastigotes infected in BESM cells assessed as reduction in episterol content at 5 uM after 72 hrs | 20385875 |
| BESM | Function assay | 5 uM | 72 hrs | Inhibition of sterol 14-alpha-demethylase in Trypanosoma cruzi amastigotes infected in BESM cells assessed as reduction in fecosterol content at 5 uM after 72 hrs | 20385875 |
| C2C12 | Function assay | 100 nM | 24 hrs | Inhibition of sterol biosynthesis in Trypanosoma cruzi CAI/72 amastigotes infected in mouse C2C12 cells assessed as increase in lanosterol level at 100 nM incubated for 24 hrs by GC-MS method | 25393646 |
| C2C12 | Function assay | 100 nM | 24 hrs | Inhibition of sterol biosynthesis in Trypanosoma cruzi CAI/72 amastigotes infected in mouse C2C12 cells assessed as increase in eburicol level at 100 nM incubated for 24 hrs by GC-MS method | 25393646 |
| C2C12 | Function assay | 100 nM | 24 hrs | Inhibition of sterol biosynthesis in Trypanosoma cruzi CAI/72 amastigotes infected in mouse C2C12 cells assessed as reduction in episterol level at 100 nM incubated for 24 hrs by GC-MS method | 25393646 |
| C2C12 | Function assay | 100 nM | 24 hrs | Inhibition of sterol biosynthesis in Trypanosoma cruzi CAI/72 amastigotes infected in mouse C2C12 cells assessed as reduction in fecosterol level at 100 nM incubated for 24 hrs by GC-MS method | 25393646 |
| ASZ | Function assay | 48 hrs | Inhibition of hedgehog pathway in mouse ASZ cells assessed as downregulation of Gli1 mRNA expression after 48 hrs by qPCR method, IC50=0.54μM | 27014922 | |
| MERP MB | Antiproliferative assay | 48 hrs | Antiproliferative activity against mouse MERP MB cells assessed as cell growth inhibition using methyl-[3H]thymidine after 48 hrs by liquid scintillation spectrophotometry, GI50=1.5μM | 27014922 | |
| J774 | Antileishmanial assay | 72 hrs | Antileishmanial activity against Leishmania amazonensis infected in mouse J774 cells after 72 hrs using 2 hrs parasite exposed mouse J774 cells, IC50=1.6μM | 27048943 | |
| ASZ | Function assay | 48 hrs | Inhibition of hedgehog signaling pathway in mouse ASZ cells assessed as decrease in Gli1 mRNA expression after 48 hrs by qRT-PCR analysis, IC50=0.5μM | 30529635 | |
| Caco-2 | Function assay | 48 hrs | Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging, IC50=1.61μM | ChEMBL | |
| Caco-2 | Function assay | 48 hrs | Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay, CC50=14.64μM | ChEMBL | |
| 3T3 | Antitrypanosomal assay | Antitrypanosomal activity against Trypanosoma cruzi Tulahuen infected in mouse 3T3 cells, EC50=0.0003μM | 19875282 | ||
| human hepatocytes | Function assay | Inhibition of CYP3A4 in human hepatocytes using testosterone as substrate by HPLC/MS/MS method, IC50=0.05 μM | 24948565 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 20429511 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 20547819 | ||
| SK-N-SH | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells | 20547819 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 20547819 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 23462713 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 24120539 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 24304150 | ||
| LAN-5 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells | 27014922 | ||
| Ptch-CKO | Function assay | Inhibition of hedgehog signaling pathway in hedgehog-dependent mouse Ptch-CKO cells assessed as inhibition of cell growth, GI50=1.5μM | 30529635 | ||
| Caco2 | Function assay | Substrate activity at P-gp in human Caco2 cells by LC-MS/MS analysis | 30529635 | ||
| Vero | Antiviral assay | Antiviral activity against DENV2 16881 infected in African green monkey Vero cells by qRT-PCR analysis, EC50=4.1μM | 31128447 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Posaconazole是CYP3A4的抑制剂，但不抑制其他CYP酶的活性；同时是sterol C14ɑ demethylase的抑制剂，IC50为0.25 μM。其平均的消除半衰期为15-35小时。 | ||
|---|---|---|---|
| 特性 | 目前治疗南美洲锥虫病的最好候选药。 | ||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Posaconazole具有有效的杀椎虫活性。Amiodarone与Posaconazole产生协同作用。Posaconazole也会影响并打乱T. cruzi 中Ca2+内稳态。Posaconazole阻断寄生虫存活必需的麦角固醇生物合成。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。对临床相关的细胞内无鞭毛体寄生虫形式，Posaconazole具有更好的效能。Posaconazole的最低抑菌浓度和IC50值分别为3 nM和0.25 nM。[1]Posaconazole对耐Fluconazole，Voriconazole，和Amphotericin B的念珠菌和曲霉菌株具有活性，并且比其它三唑类抗接合菌药更有效。[2] |
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|---|---|---|---|---|
| 细胞实验 | 细胞系 | T. cruzi 无鞭毛体的短膜型 | ||
| 浓度 | 0 nM -4 nM | |||
| 孵育时间 | 96小时 | |||
| 方法 | 寄生虫的上鞭毛体型在肝脏灌注胰蛋白培养基中，用10%新生小牛血清增补，28 °C下强烈(120 rpm)搅拌培养。培养开始时，细胞密度为2×106短膜型/mL，Posaconazole在细胞密度为0.5−1.0×107短膜型/mL时加入。细胞密度使用电子粒子计数器测量，并通过血细胞计数器直接计数。细胞活性在台盼蓝排除法后，使用光学显微镜测定。无鞭毛体在维持最低必需培养液的Vero细胞中，用1%胎牛血清增补，在湿润的大气(95%空气−5% CO2)中于37℃下培养。细胞以10个组织培养衍生的锥鞭毛体/细胞感染2小时，然后用磷酸盐缓冲盐水(PBS)洗涤3次以除去非粘附寄生虫。加入包含或不包含Posaconazole的新鲜培养基，细胞培养96小时，第48小时更换培养基。感染细胞的百分比和每个细胞中寄生虫数量使用光学显微镜直接测定，并对结果进行统计分析。IC50值使用GraFit程序通过非线性回归计算。并计算抑菌浓度指数(FIC)。对照组和药物处理的细胞外短膜型组中，细胞质的游离Ca2+浓度使用Fura-2通过荧光测定。亚细胞的Ca2+水平和线粒体膜电位在感染T. cruzi无鞭毛体的单个Vero细胞中通过使用时间扫描共聚焦显微镜监测。简而言之，严重感染(72 小时)T. cruzi无鞭毛体的Vero细胞接种在22×40 mm玻片上(0.15 mm 厚)，同时与10 μM细胞渗透性Rhod-2和10 μg/mL 罗丹明-123于37℃下在培养基中培养50分钟，然后清洗，并与包含或不包含amiodarone 的林格氏溶液一起培养。该条件下的Rhod-2荧光主要来自细胞内Ca2+富集区，如线粒体中，这是由于Rhod-2对Ca2+的低亲和力限制了其在Ca2+缺乏的Vero细胞或无鞭毛体细胞质中的荧光性。罗丹明-123是线粒体特异性阳离子染料，能够严格按照膜电位穿过线粒体膜分布。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | Wee1 / c-Myc / Cyclin B1 / Cdc25C / Bcl-2 / Bax / p21 / Survivin |
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28383032 | |
| Growth inhibition assay | Cell proliferation |
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28383032 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Amiodarone单独治疗感染的动物能够减少寄生虫血症，增加60天生存期(未处理的对照组为0%，amiodarone 处理的动物为40%)，与Posaconazole联合用药时，能够延缓寄生虫血症的发展。[1]与Posaconazole在禁食状态单独给药相比，Posaconazole与Boost Plus同时服用增加药物暴露。食物，特别是高脂肪含量的膳食，显著增加Posaconazole的生物利用度。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。[3] Posaconazole 和 Amiodarone可能产生有效的抗T. cruzi治疗，并且副作用低。[4] Posaconazole(≥15 mg/kg，每天两次)延长小鼠生存，并减少组织负担。[5] |
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|---|---|---|
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT06282718 | Not yet recruiting | Acute Respiratory Tract Infection |
European Clinical Research Alliance for Infectious Diseases (ECRAID)|UMC Utrecht|University of Oxford|Universiteit Antwerpen |
February 2024 | -- |
| NCT06158360 | Recruiting | Thyroid Cancer |
Ilsan Cha hospital |
January 1 2024 | -- |
| NCT05845359 | Withdrawn | Bariatric Surgery Candidate |
Montefiore Medical Center |
September 2023 | Phase 4 |
| NCT06302842 | Active not recruiting | Supportive Care |
Istituto Auxologico Italiano |
July 1 2023 | Not Applicable |
| NCT05617638 | Recruiting | Pain |
Hospital Israelita Albert Einstein|Beneficência Portuguesa de São Paulo |
June 27 2023 | Not Applicable |
化学信息&溶解度
| 分子量 | 700.78 | 分子式 | C37H42F2N8O4 |
| CAS号 | 171228-49-2 | SDF | Download Posaconazole SDF |
| Smiles | CCC(C(C)O)N1C(=O)N(C=N1)C2=CC=C(C=C2)N3CCN(CC3)C4=CC=C(C=C4)OCC5CC(OC5)(CN6C=NC=N6)C7=C(C=C(C=C7)F)F | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (142.69 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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