Bemnifosbuvir Hemisulfate (AT-527)

製品コードE1013 バッチE101301

印刷

化学情報

Chemical Structure Synonyms RG-6422, RO 7496998 Storage
(From the date of receipt)		 3 years -20°C powder
化学式

C24H33FN7O7P.1/2H2O4S
分子量 630.55 CAS No. 2241337-84-6
Solubility (25°C)* 体外 DMSO 100 mg/mL (158.59 mM)
Water 100 mg/mL (158.59 mM)
Ethanol 100 mg/mL (158.59 mM)
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Bemnifosbuvir Hemisulfate (AT-527, RG-6422, RO 7496998) is a hemi-sulfate salt of AT-511. AT-511 is a potent inhibitor of SARS-CoV-2 with an EC90 of 0.47 μM.
in vitro

AT-511 is the free base of AT-527. AT-511 inhibits replication of several human coronaviruses, such as HCoV-229E, HCoV-OC43, SARS-CoV in Huh-7 cells and HCoV-229E in BHK-21 cells. AT-511 can also inhibits SARS-CoV-2 replication in primary human airway epithelial (HAE) cells. In HBE and HNE cells, AT-511 can promote the host cells to form the pharmacologically active TP, AT-9010, to inhibit virus replication.[1]
in vivo

In nonhuman primates (NHPs), after oral administration of AT-527, T-273 has the longest MRT at all dose levels, which indicate the long half-life of the active TP formed intracellularly. AT-527 is preferentially delivered to the liver, the target organ for HCV infection.[1]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 Huh-7, BHK-21, HBE, HNE cells
濃度 100 μM, 20 μM, 4 μM, 0.8 μM
反応時間 2h, 8 h, 3 days
実験の流れ

AT-511 dilution is added to 5 wells of a 96-well plate with 80 to 100% confluent cells. Three wells of each dilution are infected with virus, and two wells remain uninfected as toxicity controls. Six untreated wells are infected as virus controls, and six untreated wells are left uninfected to use as virus controls. Viruses are diluted to achieve MOIs of 0.003, 0.002, 0.001, and 0.03 CCID50 (50% cell culture infectious dose) per cell for 229E, OC43, MERS, and SARS coronaviruses, respectively.Plates are incubated at 37°C in a humidified atmosphere containing 5% CO2.The plates are stained with neutral red dye for approximately 2 h (±15 min). Supernatant dye was removed, wells are rinsed with phosphate-buffered saline (PBS), and the incorporated dye is extracted in 50:50 Sorensen citrate buffer-ethanol for >30 min. The optical density is read on a spectrophotometer at 540 nm and converts to percentage of controls.
動物実験 動物モデル Male nonnaive cynomolgus monkeys
投薬量 60 mg/kg, 30mg/kg
投与方法 p.o.

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。