Posaconazole
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Posaconazole(SCH 56592或Noxafil)是一种新型抗真菌三唑化合物,有效抑制各种真菌中的14α去甲基化酶,包括念珠菌(C. albicans C43、C. albicans C288、C. albicans C600和C. albicans C248)和曲霉(A. fumigatus ND158和A. flavus ND134),IC50值分别为0.007 μg/ml、0.06 μg/ml、0.2 μg/ml、0.3 μg/ml、0.03 μg/ml和0.03 μg/ml[1]。
Posaconzole是伊曲康唑的衍生物,氟取代了苯环上的氯,侧链被羟基化。Posaconzole与14α去甲基化酶活性位点上的血红素辅因子结合,从而使羊毛甾醇向14α-二甲基羊毛甾醇转化,破坏了真菌细胞膜的完整性和功能,抑制真菌生长[2]。
参考文献:
[1] Hanan K. Munayyer, Paul A. Mann, Andrew S. Chau, Taisa Yarosh-Tomaine, Jonathan R. Greene, Roberta S. Hare, Larry Heimark, Robert E. Palermo, David Loebenberg and Paul M. McNicholas. Posaconazole is a potent inhibitor of sterol 14α-demethylation in yeasts and molds. ANTIMICROBIAL AGENTS AND CHEMOTHERAPY. 2004; 48(10): 3690-3696
[2] Daryl S. Schiller and Horatio B. Fung. Posaconazole: an extended-spectrum triazole antifungal agent. Clinical Therapeutics. 2007; 29(9): 1862-1886
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 700.78 |
Cas No. | 171228-49-2 |
Formula | C37H42F2N8O4 |
Solubility | ≥35.04 mg/mL in DMSO; insoluble in H2O; ≥2.55 mg/mL in EtOH with ultrasonic |
Chemical Name | 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)-5-(1,2,4-triazol-1-ylmethyl)oxolan-3-yl]methoxy]phenyl]piperazin-1-yl]phenyl]-2-[(2S,3S)-2-hydroxypentan-3-yl]-1,2,4-triazol-3-one |
SDF | Download SDF |
Canonical 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 |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
细胞实验[1]: | |
细胞系 |
25株粗球孢子菌 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月。 |
反应条件 |
MIC: 0.5 μg/ml, 48 hours |
实验结果 |
在含有L-谷氨酰胺和吗啉丙磺酸的RPMI 1640缓冲液中,Posaconazole的浓度为165 mM。药物的最终浓度为0.015至8 μg/ml。在24和48小时读取MICs。Posaconazole的MICs范围为0.25至1 μg/ml,Posaconazole MIC的几何平均值为0.5 μg/ml。Posaconazole的MIC50和MIC90分别为0.5和1 μg/ml。 |
动物实验[2]: | |
动物模型 |
雄性BALB/c小鼠 |
剂量 |
口服给药,5、15或30 mg/kg,每天两次,给药七天 |
实验结果 |
在感染前一天,使用单剂量的5-氟尿嘧啶和环磷酰胺使小鼠中性白细胞减少。这种治疗减少嗜中性粒细胞的数目。使用0.2ml的接种物静脉内感染小鼠。感染后1天开始抗真菌剂治疗。Posaconazole处理小鼠的存活以剂量依赖性方式显著增加,并显著高于对照组。使用30 mg/kg的剂量,每日两次,存活率为60至83%。剂量为15和30 mg/kg的posaconazole显著降低组织中的计数。剂量为30 mg/kg的posaconazole将计数降低至不可检测水平。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] González G M, Tijerina R, Najvar L K, et al. In vitro and in vivo activities of posaconazole against Coccidioidesimmitis. Antimicrobial agents and chemotherapy, 2002, 46(5): 1352-1356. [2] Sun Q N, Najvar L K, Bocanegra R, et al. In vivo activity of posaconazole against Mucor spp. in an immunosuppressed-mouse model. Antimicrobial agents and chemotherapy, 2002, 46(7): 2310-2312. |
描述 | Posaconazole是C14ɑ去甲基化酶的抑制剂,IC50值为0.25 nM。 | |||||
靶点 | C14ɑ demethylase | |||||
IC50 | 0.25 nM |
质量控制和MSDS
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