Lumicitabine (Synonyms: ALS-008176; ALS-8176)
目录号: PL11092 纯度: ≥99%
CAS No. :1445385-02-3
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中文名称
Lumicitabine
中文别名
ALS-8176
英文名称
Lumicitabine
英文别名
4-chloromethyl-2-deoxy-3,5-di-O-isobutyryl-2-fluorocytidine;ALS 008176;ALS-008176;ALS8176;ALS-8176;Lumicitabine;BNW5PQ52G1;Lumicitabine [USAN];4'-Chloromethyl-2'-deoxy-3',5'-di-o-isobutyryl-2'-fluorocytidine;DB14808;SB19168;Q27274772;Cytidine, 4'-C-(chloromethyl)-2'-deoxy-2'-fluoro-, 3',5'-bis(2-methylpropanoate)
Cas No.
1445385-02-3
分子式
C18H25ClFN3O6
分子量
433.86
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
Lumicitabine (ALS-008176) 是呼吸道合胞病毒(RSV)聚合酶的抑制剂。
生物活性
Lumicitabine (ALS-008176) is an inhibitor of the respiratory syncytial virus (RSV) polymerase.
性状
Solid
体外研究(In Vitro)
Lumicitabine is an orally bioavailable prodrug of the novel RSV replication inhibitor ALS-008112, a cytidine nucleoside analogue. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
Lumicitabine demonstrates excellent anti-RSV efficacy and safety in a phase 2 clinical RSV challenge study. It exhibits good oral bioavailability and a high level of 2c-TP in vivo. Lumicitabine has excellent stability profiles in formulations (>24 h storage stability in 0.5% methylcellulose aqueous formulation at rt) and simulats gastric and intestinal fluids (half-life >2 h). Its solubility is adequate to support oral administration in solutions with relatively low percentage of organic solvent and in aqueous suspensions. High levels of NMP and NTP are obtained following oral administration of Lumicitabine to monkeys. In an adult human challenge study, Lumicitabine has shown efficacy against RSV infection. 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
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. DeVincenzo JP, et al. Activity of Oral ALS-008176 in a Respiratory Syncytial Virus Challenge Study. N Engl J Med. 2015 Nov 19;373(21):2048-58.
[2]. Wang G, et al. Discovery of 4-chloromethyl-2-deoxy-3,5-di-O-isobutyryl-2-fluorocytidine (ALS-8176), a first-in-class RSV polymerase inhibitor for treatment of human respiratory syncytial virus infection. J Med Chem. 2015 Feb 26;58(4):1862-78.
溶解度数据
In Vitro: DMSO : ≥ 50 mg/mL (115.24 mM)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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