- 抑制劑
- 化合物庫
- 抗體
- 生物試劑
- 新產(chǎn)品
- 聯(lián)系我們
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。
Posaconazole Chemical Structure
CAS: 171228-49-2
產(chǎn)品質(zhì)控
批次：
純度：
99.97%
99.97
Posaconazole相關(guān)產(chǎn)品
| 相關(guān)靶點 | P450 CYP2 CYP51 CYP3 CYP735 CYP11 CYP26 CYP2C9 CYP1 CYP17 | 點擊展開 |
|---|---|---|
| 相關(guān)產(chǎn)品 | Apigenin Baicalein Avasimibe Naringenin Diosmetin Alizarin Sodium Danshensu Orteronel Amentoflavone Tetrahydrocurcumin Uniconazole (S 3307D) Naringin Ellipticine hydrochloride Tanshinone IIA sulfonate sodium Benzbromarone Piperine | 點擊展開 |
| 相關(guān)化合物庫 | 代謝化合物庫 抗癌代謝化合物庫 谷氨酰胺代謝化合物庫 糖代謝化合物庫 脂代謝化合物庫 | 點擊展開 |
相關(guān)信號通路圖
細胞實驗數(shù)據(jù)示例
| 細胞系 | 實驗類型 | 給藥濃度 | 孵育時間 | 活性描述 | 文獻信息 |
|---|---|---|---|---|---|
| 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 | ||
| 點擊查看更多細胞系數(shù)據(jù) | |||||
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。 | ||
|---|---|---|---|
| 特性 | 目前治療南美洲錐蟲病的最好候選藥。 | ||
| 靶點 |
|
| 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對前鞭體(細胞外)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。對臨床相關(guān)的細胞內(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] |
|||
|---|---|---|---|---|
| 細胞實驗 | 細胞系 | T. cruzi 無鞭毛體的短膜型 | ||
| 濃度 | 0 nM -4 nM | |||
| 孵育時間 | 96小時 | |||
| 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，28 °C下強烈(120 rpm)攪拌培養(yǎng)。培養(yǎng)開始時，細胞密度為2×106短膜型/mL，Posaconazole在細胞密度為0.5−1.0×107短膜型/mL時加入。細胞密度使用電子粒子計數(shù)器測量，并通過血細胞計數(shù)器直接計數(shù)。細胞活性在臺盼藍排除法后，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細胞中，用1%胎牛血清增補，在濕潤的大氣(95%空氣−5% CO2)中于37℃下培養(yǎng)。細胞以10個組織培養(yǎng)衍生的錐鞭毛體/細胞感染2小時，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，細胞培養(yǎng)96小時，第48小時更換培養(yǎng)基。感染細胞的百分比和每個細胞中寄生蟲數(shù)量使用光學(xué)顯微鏡直接測定，并對結(jié)果進行統(tǒng)計分析。IC50值使用GraFit程序通過非線性回歸計算。并計算抑菌濃度指數(shù)(FIC)。對照組和藥物處理的細胞外短膜型組中，細胞質(zhì)的游離Ca2+濃度使用Fura-2通過熒光測定。亞細胞的Ca2+水平和線粒體膜電位在感染T. cruzi無鞭毛體的單個Vero細胞中通過使用時間掃描共聚焦顯微鏡監(jiān)測。簡而言之，嚴重感染(72 小時)T. cruzi無鞭毛體的Vero細胞接種在22×40 mm玻片上(0.15 mm 厚)，同時與10 μM細胞滲透性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熒光主要來自細胞內(nèi)Ca2+富集區(qū)，如線粒體中，這是由于Rhod-2對Ca2+的低親和力限制了其在Ca2+缺乏的Vero細胞或無鞭毛體細胞質(zhì)中的熒光性。羅丹明-123是線粒體特異性陽離子染料，能夠嚴格按照膜電位穿過線粒體膜分布。 |
|||
| 實驗圖片 | 檢測方法 | 檢測指標 | 實驗圖片 | 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單獨治療感染的動物能夠減少寄生蟲血癥，增加60天生存期(未處理的對照組為0%，amiodarone 處理的動物為40%)，與Posaconazole聯(lián)合用藥時，能夠延緩寄生蟲血癥的發(fā)展。[1]與Posaconazole在禁食狀態(tài)單獨給藥相比，Posaconazole與Boost Plus同時服用增加藥物暴露。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，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 | 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 | ||
| 儲存條件(自收到貨起) | |||
|
體外溶解度 |
DMSO : 100 mg/mL ( (142.69 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO) Water : Insoluble Ethanol : Insoluble |
摩爾濃度計算器 |
|
體內(nèi)溶解度 現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑 |
動物體內(nèi)配方計算器 | ||||
實驗計算
動物體內(nèi)配方計算器（澄清溶液）
第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）
mg/kg
g
μL
只
第二步：請輸入動物體內(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，請聯(lián)系Selleck為您提供正確的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
計算結(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。
技術(shù)支持
在訂購、運輸、儲存和使用我們的產(chǎn)品的任何階段，您遇到的任何問題，均可以通過撥打我們的熱線電話400-668-6834，或者技術(shù)支持郵箱tech@selleck.cn，直接聯(lián)系到我們。我們會在24小時內(nèi)盡快聯(lián)系您。
如果有其他問題，請給我們留言。
* 必填項
Tags: buy Posaconazole | Posaconazole supplier | purchase Posaconazole | Posaconazole cost | Posaconazole manufacturer | order Posaconazole | Posaconazole distributor
