Artefenomel (Synonyms: OZ439)
目录号: PL04667 纯度: ≥98%
CAS No. :1029939-86-3
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中文名称
Artefenomel
中文别名
OZ439标准品
英文名称
Artefenomel
英文别名
OZ439;Artefenomel;RIK029813G;cis-4-[2-[4-(Dispiro[cyclohexane-1,3'-[1,2,4]trioxolane-5',2''-tricyclo[3.3.1.1(3,7)]decan]-4-yl)phenoxy]ethyl]morpholine methanesulfonate;cis-4-[2-[4-(Dispiro[cyclohexane-1,3'-[1,2,4]trioxolane-5',2''-tricyclo[3.3.1.1(3,7)]decan]-4-yl)phenoxy]ethyl]morpholine methanesulfonate;Artefenomel [INN];GTPL9971;OZ 439;DB11809;SB19148;Q27288132
Cas No.
1029939-86-3
分子式
C28H39NO5
分子量
469.61
包装储存
-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
产品详情
Artefenomel (OZ439) 是一种具有口服活性的、合成的含有青蒿素药效团的抗疟疾化合物,具有类似于青蒿素的作用机制。 Artefenomel 具有 SARS-CoV-2 的抗病毒活性。
生物活性
Artefenomel (OZ439) is an orally active, synthetic anti-malarial compound containing an artemisinin pharmacophore with a mechanism of action similar to that of artemisinin. Artefenomel has antiviral activity against SARS-CoV-2.
性状
Solid
体外研究(In Vitro)
Artefenomel (OZ439) (10 μg/mL, 2 h) can alkylate Plasmodium falciparum proteins.
Artefenomel (0.3-300 μM) reduces ACE2 expression in Vero cells in a dose-dependent manner and does not induce any cytotoxicity at concentrations up to 300 μM.
Artefenomel (33-100 μM) can completely prevent the virus-induced CPE and inhibit SARS-CoV-2 in a dose-dependent manner with an IC50 of 2.9 μM.
Artefenomel (0-10 μg/mL) affects red blood cells and induces anaemia, thereby inducing histological changes (cell death) and macroscopic abnormalities in the embryo from pregnant Crl:CD(SD)BR rats.
has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
ClinicalTrial
参考文献
[1]. Jo?lle Jourdan, et al. Monoclonal Antibodies That Recognize the Alkylation Signature of Antimalarial Ozonides OZ277 (Arterolane) and OZ439 (Artefenomel). ACS Infect Dis. 2016 Jan 8;2(1):54-61.
[2]. Tania Massignan, et al. Antimalarial Artefenomel Inhibits Human SARS-CoV-2 Replication in Cells while Suppressing the Receptor ACE2.
[3]. Robert L Clark, e
溶解度数据
In Vitro: DMSO : 4.2 mg/mL (8.94 mM; Need ultrasonic)配制储备液
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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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