PC945|1931946-73-4|-陌孚医药/Medlife

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PC945

目录号: PL14604 纯度: ≥99%

CAS No. :1931946-73-4

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中文名称	PC945
英文名称	PC945
英文别名	PC945;45LU8Q6ASU;Opelconazole;Opelconazole(inn);D-Threo-pentitol, 2,5-anhydro-1,3,4-trideoxy-2-C-(2,4-difluorophenyl)-4-((4-(4-(4-(((4-fluorophenyl)amino)carbonyl)phenyl)-1-piperazinyl)-2-methylphenoxy)methyl)-1-(1H-1,2,4-triazol-1-yl)-;Unii-45LU8Q6asu
Cas No.	1931946-73-4
分子式	C₃₈H₃₇F₃N₆O₃
分子量	682.73
包装储存	Powder -20°C 3 years；4°C 2 years

产品详情

PC945 是一种有效的抗真菌 (antifungal) 三唑类药物，对多种敏感和耐药的烟曲霉菌株都具有抗药性。PC945 是烟曲霉甾醇 14α-去甲基酶 (CYP51A/CYP51B) 活性的有效、紧密结合的抑制剂，IC₅₀s 分别为 0.23 μM 和 0.22 μM。

生物活性

PC945, a potent, long-acting antifungal triazole, possesses activity against a broad range of both azole-susceptible and azole-resistant strains of Aspergillus fumigatus. PC945 is also a potent, tightly binding inhibitor of A. fumigatus sterol 14α-demethylase activity, CYP51A and CYP51B, with IC 50 s of 0.23 μM and 0.22 μM, respectively.

性状

Solid

IC50 & Target[1][2]

fungal CYP51A 0.23 μM (IC50)

体外研究(In Vitro)

PC945 is a triazole antifungal designed for administration via inhalation.
PC945 exhibits the most potent antifungal activity on azole-susceptible strain NCPF2010 with the MIC value of 0.063?μg/mL. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

PC945 (0.56-14 μg/mouse; intranasal; daily for 7 days) substantially inhibits the incidence of rolling behavior. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Specific-pathogen-free

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[1]. Colley T, et al. In Vitro and In Vivo Antifungal Profile of a Novel and Long-Acting Inhaled Azole, PC945, on Aspergillus fumigatus Infection. Antimicrob Agents Chemother. 2017 Apr 24;61(5). pii: e02280-16.
[2]. Colley T, et al. Antifungal synergy of a topical triazole, PC945, with a systemic triazole against respiratory Aspergillus fumigatus infection. Sci Rep. 2019 Jul 1;9(1):9482.

溶解度数据	In Vitro: DMSO : 100 mg/mL (146.47 mM; Need ultrasonic)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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