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Posaconazole

別名: SCH 56592, POS 中文名稱：泊沙康唑

Posaconazole是CYP3A4的抑制劑，但不抑制其他CYP酶的活性；同時(shí)是sterol C14ɑ demethylase的抑制劑，IC50為0.25 μM。其平均的消除半衰期為15-35小時(shí)。

Posaconazole Chemical Structure

Posaconazole Chemical Structure

CAS: 171228-49-2

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1570 現(xiàn)貨
5mg 1136.26 現(xiàn)貨
25mg 4673.74 現(xiàn)貨
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Posaconazole相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

P450 (e.g. CYP17) Signaling Pathways

P450 (e.g. CYP17)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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
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生物活性

產(chǎn)品描述 Posaconazole是CYP3A4的抑制劑，但不抑制其他CYP酶的活性；同時(shí)是sterol C14ɑ demethylase的抑制劑，IC50為0.25 μM。其平均的消除半衰期為15-35小時(shí)。
特性 目前治療南美洲錐蟲病的最好候選藥。
靶點(diǎn)
lanosterol 14α-demethylase [1] CYP3A4 [6]
體外研究(In Vitro)
體外研究活性

Posaconazole具有有效的殺椎蟲活性。Amiodarone與Posaconazole產(chǎn)生協(xié)同作用。Posaconazole也會(huì)影響并打亂T. cruzi 中Ca2+內(nèi)穩(wěn)態(tài)。Posaconazole阻斷寄生蟲存活必需的麥角固醇生物合成。Posaconazole對(duì)前鞭體(細(xì)胞外)階段的增殖具有明顯的劑量依賴性作用，最低抑菌濃度為20 nM，IC50為14 nM。對(duì)臨床相關(guān)的細(xì)胞內(nèi)無鞭毛體寄生蟲形式，Posaconazole具有更好的效能。Posaconazole的最低抑菌濃度和IC50值分別為3 nM和0.25 nM。[1]Posaconazole對(duì)耐Fluconazole，Voriconazole，和Amphotericin B的念珠菌和曲霉菌株具有活性，并且比其它三唑類抗接合菌藥更有效。[2]
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 T. cruzi 無鞭毛體的短膜型
濃度 0 nM -4 nM
孵育時(shí)間 96小時(shí)
方法

寄生蟲的上鞭毛體型在肝臟灌注胰蛋白培養(yǎng)基中，用10%新生小牛血清增補(bǔ)，28 °C下強(qiáng)烈(120 rpm)攪拌培養(yǎng)。培養(yǎng)開始時(shí)，細(xì)胞密度為2×106短膜型/mL，Posaconazole在細(xì)胞密度為0.5−1.0×107短膜型/mL時(shí)加入。細(xì)胞密度使用電子粒子計(jì)數(shù)器測量，并通過血細(xì)胞計(jì)數(shù)器直接計(jì)數(shù)。細(xì)胞活性在臺(tái)盼藍(lán)排除法后，使用光學(xué)顯微鏡測定。無鞭毛體在維持最低必需培養(yǎng)液的Vero細(xì)胞中，用1%胎牛血清增補(bǔ)，在濕潤的大氣(95%空氣−5% CO2)中于37℃下培養(yǎng)。細(xì)胞以10個(gè)組織培養(yǎng)衍生的錐鞭毛體/細(xì)胞感染2小時(shí)，然后用磷酸鹽緩沖鹽水(PBS)洗滌3次以除去非粘附寄生蟲。加入包含或不包含Posaconazole的新鮮培養(yǎng)基，細(xì)胞培養(yǎng)96小時(shí)，第48小時(shí)更換培養(yǎng)基。感染細(xì)胞的百分比和每個(gè)細(xì)胞中寄生蟲數(shù)量使用光學(xué)顯微鏡直接測定，并對(duì)結(jié)果進(jìn)行統(tǒng)計(jì)分析。IC50值使用GraFit程序通過非線性回歸計(jì)算。并計(jì)算抑菌濃度指數(shù)(FIC)。對(duì)照組和藥物處理的細(xì)胞外短膜型組中，細(xì)胞質(zhì)的游離Ca2+濃度使用Fura-2通過熒光測定。亞細(xì)胞的Ca2+水平和線粒體膜電位在感染T. cruzi無鞭毛體的單個(gè)Vero細(xì)胞中通過使用時(shí)間掃描共聚焦顯微鏡監(jiān)測。簡而言之，嚴(yán)重感染(72 小時(shí))T. cruzi無鞭毛體的Vero細(xì)胞接種在22×40 mm玻片上(0.15 mm 厚)，同時(shí)與10 μM細(xì)胞滲透性Rhod-2和10 μg/mL 羅丹明-123于37℃下在培養(yǎng)基中培養(yǎng)50分鐘，然后清洗，并與包含或不包含amiodarone 的林格氏溶液一起培養(yǎng)。該條件下的Rhod-2熒光主要來自細(xì)胞內(nèi)Ca2+富集區(qū)，如線粒體中，這是由于Rhod-2對(duì)Ca2+的低親和力限制了其在Ca2+缺乏的Vero細(xì)胞或無鞭毛體細(xì)胞質(zhì)中的熒光性。羅丹明-123是線粒體特異性陽離子染料，能夠嚴(yán)格按照膜電位穿過線粒體膜分布。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot Wee1 / c-Myc / Cyclin B1 / Cdc25C / Bcl-2 / Bax / p21 / Survivin 28383032
Growth inhibition assay Cell proliferation 28383032
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

Amiodarone單獨(dú)治療感染的動(dòng)物能夠減少寄生蟲血癥，增加60天生存期(未處理的對(duì)照組為0%，amiodarone 處理的動(dòng)物為40%)，與Posaconazole聯(lián)合用藥時(shí)，能夠延緩寄生蟲血癥的發(fā)展。[1]與Posaconazole在禁食狀態(tài)單獨(dú)給藥相比，Posaconazole與Boost Plus同時(shí)服用增加藥物暴露。食物，特別是高脂肪含量的膳食，顯著增加Posaconazole的生物利用度。與高脂和脫脂食物一起消耗時(shí)，全身接觸Posaconazole分別增加其4倍和2.6倍的消耗。[3] Posaconazole 和 Amiodarone可能產(chǎn)生有效的抗T. cruzi治療，并且副作用低。[4] Posaconazole(≥15 mg/kg，每天兩次)延長小鼠生存，并減少組織負(fù)擔(dān)。[5]
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 S?o Paulo
 June 27 2023 Not Applicable

化學(xué)信息&溶解度

分子量 700.78 分子式

C37H42F2N8O4
CAS號(hào) 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
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (142.69 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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