Posaconazole (SCH 56592)

For research use only. Not for use in humans.

目录号:S1257 中文名称:泊沙康唑

Posaconazole (SCH 56592) Chemical Structure

CAS No. 171228-49-2

Posaconazole (SCH56592) 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。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 3193.77 现货
RMB 1136.26 现货
RMB 2194.15 现货
RMB 4673.74 现货
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客户使用Selleck生产的Posaconazole (SCH 56592)发表文献18篇:

客户使用该产品的1个实验数据:

  • Comparative mean±SD plasma concentration versus time curves of 40mg/kg oral posaconazole (PSZ) administrated in normolipidemic (NL), intermediate hyperlipidemic (IHL) or extreme hyperlipidemic (HL) rat groups. An insert showing a clear snap of the plasma concentrations for the first 7 h.

    Eur J Pharm Sci, 2016, 91:190-195. . Posaconazole (SCH 56592) purchased from Selleck.

产品安全说明书

P450 (e.g. CYP17)抑制剂选择性比较

生物活性

产品描述 Posaconazole (SCH56592) 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
lanosterol 14α-demethylase [1]
()
CYP3A4 [6]
体外研究

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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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Ptch-CKO MUTGeY5kfGmxbjDhd5NigQ>? MnKzTY5pcWKrdHnvckBw\iCqZXTn[Yhw\yC|aXfuZYxqdmdicHH0bJdigSCrbjDo[YRo\WixZz3k[ZBmdmSnboSgcY92e2ViUITjbE1EU09iY3XscJMh[XO|ZYPz[YQh[XNiaX7obYJqfGmxbjDv[kBk\WyuIHfyc5d1cCxiR1m1NF0yNjYQvF2= NULsfWcxRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1Nlk3OzVpPkOwOVI6PjN3PD;hQi=>
Caco2 M4XwZWZ2dmO2aX;uJIF{e2G7 M2TuXHN2[nO2cnH0[UBi[3Srdnn0fUBifCCSLXfwJIlvKGi3bXHuJGNi[29{IHPlcIx{KGK7IFzDMW1UN02VIHHuZYx6e2m| NH3oc|g9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEWyPVY{PSd-M{C1Nlk3OzV:L3G+
Vero NFvJcWVCdnSrdnnyZYwh[XO|YYm= M3zPb2FvfGm4aYLhcEBi[3Srdnn0fUBi\2GrboP0JGRGVlZ{IEG2PFgyKGmwZnXjeIVlKGmwIFHmdolk[W5iZ4Ll[Y4hdW:wa3X5JHZmem9iY3XscJMh[nlicWLUMXBEWiCjbnHsfZNqeyxiRVO1NF01NjIQvF2= NYXuRolERGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{GxNlg1PDdpPkOxNVI5PDR5PD;hQi=>
Caco-2 MX3GeY5kfGmxbjDhd5NigQ>? MnzmOFghcHK| M1j1eWRmfGW{bXnuZZRqd25ib3[gTWM2OCC4YXz1[ZMh\m:{IHnubIljcXSrb36gc4YhW0GUUz3Dc3YuOiCrbnT1Z4VlKGO7dH;0c5hq[2m2eTDv[kBE[WOxLUKgZ4VtdHNiYX\0[ZIhPDhiaH;1dpMh[nliaHnnbEBkd262ZX70JIlu[WerbnesJGlEPTB;MT62Ne69VQ>? M3vtd|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE{QTdxJ{7DbGVOSkx:L3G+
Caco-2 MXrGeY5kfGmxbjDhd5NigQ>? M4G1PVQ5KGi{cx?= NEDoRVRVd3irY3n0fUBi\2GrboP0JGNi[29vMjDj[YxteyCmZYTldo1qdmWmIHH0JFQ5KGixdYLzJIJ6KGmwdILhZ4VtdHWuYYKgRXRRKGOxbnPlcpRz[XSrb36geZNqdmdidHjlJGNmdGyWaYTldk1IdG9iTIXtbY5me2OnboSgR4VtdCCYaXHibYxqfHliQYPzZZktKEOFNUC9NVQvPjUQvF2= M2rGV|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4f3e{5m[mlwYXOueYsw[2inbXLsM4NwdXCxdX7kY5JmeG:{dG;jZZJlN0OKRV3CUFE{QTdxJ{7DbGVOSkx:L3G+

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Growth inhibition assay
Cell proliferation ; 

PubMed: 28383032     


The effect of tivozanib on cell viability was estimated by MTT assay.

28383032
Western blot
Wee1 / c-Myc / Cyclin B1 / Cdc25C / Bcl-2 / Bax / p21 / Survivin ; 

PubMed: 28383032     


Protein lysates from tivozanib-treated cells were subjected to Western blotting and probed with the indicated antibodies. β-actin was used as the loading control. The concentrations of tivozanib were 5, 10 and 20 μM. The blots are representative of three independent experiments with similar outcomes. 

28383032
体内研究 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]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

细胞实验:

[1]

- 合并
  • Cell lines: T. cruzi 无鞭毛体的短膜型
  • Concentrations: 0 nM -4 nM
  • Incubation Time: 96小时
  • Method:

    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。


    (Only for Reference)
动物实验:

[1]

- 合并
  • Animal Models: 患有急性南美洲锥虫病的雌性 NMRI−IVIC 小鼠
  • Dosages: 20 mg/kg/d
  • Administration: 口服
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (142.69 mM)
Water Insoluble
Ethanol Insoluble
体内 从左到右依次将纯溶剂加入产品,现配现用(数据来自Selleck实验检测而非文献):
1% DMSO+30% polyethylene glycol+1% Tween 80
30 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 700.78
化学式

C37H42F2N8O4

CAS号 171228-49-2
储存条件 粉状
溶于溶剂
别名 N/A

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)
给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
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
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04825275 Not yet recruiting Drug: Posaconazole Pill Glioblastoma|Glioblastoma Multiforme|Glioblastoma Multiforme of Brain|Glioblastoma Multiforme Adult Milton S. Hershey Medical Center August 2021 Early Phase 1
NCT04771130 Not yet recruiting Drug: BGB-11417|Drug: Azacitidine|Drug: Posaconazole Acute Myeloid Leukemia|Myelodysplastic Syndromes|Myelodysplastic/Myeloproliferative Neoplasm BeiGene February 2021 Phase 1|Phase 2
NCT04725942 Not yet recruiting Drug: Oral Posaconazole tablets Pulmonary Fungal Infection Institute of Hematology & Blood Diseases Hospital|Shanxi Bethune Hospital|The Second Hospital of Hebei Medical University|Tianjin Medical University Cancer Institute and Hospital January 2021 --
NCT03717623 Recruiting Drug: Posaconazole pharmacokinetics Posaconazole|Pharmacokinetics|Invasive Candidiases|Invasive Aspergillosis|Invasive Mycosis|Fungal Infection|Prophylaxis Melbourne Health|Merck Sharp & Dohme Corp. August 1 2019 Phase 4

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操作手册

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID