Bemnifosbuvir Hemisulfate (AT-527)

Catalog No.E1013 Batch:E101301

Technical Data

Formula

C₂₄H₃₃FN₇O₇P._1/2H₂O₄S

Molecular Weight

630.55

CAS No.

2241337-84-6

Solubility (25°C)*

In vitro

DMSO

100 mg/mL (158.59 mM)

Water

100 mg/mL (158.59 mM)

Ethanol

100 mg/mL (158.59 mM)

In Vivo (Add solvents to the product individually and in order.)

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

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

Targets

SARS-CoV-2

0.47 μM(EC90)

In vitro

Bemnifosbuvir Hemisulfate (AT-527) is the free base of AT-511. This compound 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. It can also inhibits SARS-CoV-2 replication in primary human airway epithelial (HAE) cells. In HBE and HNE cells, it can promote the host cells to form the pharmacologically active TP, AT-9010, to inhibit virus replication.

In Vivo

After oral administration of Bemnifosbuvir Hemisulfate (AT-527) in nonhuman primates (NHPs), T-273 has the longest MRT at all dose levels, which indicate the long half-life of the active TP formed intracellularly. This compound is preferentially delivered to the liver, the target organ for HCV infection.

Protocol (from reference)

Cell Assay:^{^[1]}	Cell Lines Huh-7, BHK-21, HBE, HNE cells Concentrations 100 μM, 20 μM, 4 μM, 0.8 μM Incubation Time 2h, 8 h, 3 days Method 将Bemnifosbuvir Hemisulfate (AT-527)稀释液加入96孔板中5个孔，细胞汇合度为80-100%。每个稀释度设三个感染病毒的孔和两个未感染的毒性对照孔。另设六个未经处理的感染孔作为病毒对照，以及六个未经处理的未感染孔作为细胞对照。病毒分别稀释至229E、OC43、MERS和SARS冠状病毒的感染复数（MOI）为0.003、0.002、0.001和0.03 CCID50（50%细胞培养感染剂量）。将培养板置于37°C、含5% CO2的湿润气氛中培养。用中性红染料染色约2小时（±15分钟）。弃去上清染料，用磷酸盐缓冲盐水（PBS）冲洗孔，并在50:50 Sorensen柠檬酸盐缓冲液-乙醇中提取结合的染料，时间超过30分钟。用分光光度计在540 nm波长下读取光密度，并转换为对照百分比。
Animal Study:^{^[1]}	Animal Models Male nonnaive cynomolgus monkeys Dosages 60 mg/kg, 30mg/kg Administration p.o.

Cell Assay:^{^[1]}

Cell Lines
Huh-7, BHK-21, HBE, HNE cells
Concentrations
100 μM, 20 μM, 4 μM, 0.8 μM
Incubation Time
2h, 8 h, 3 days
Method
将Bemnifosbuvir Hemisulfate (AT-527)稀释液加入96孔板中5个孔，细胞汇合度为80-100%。每个稀释度设三个感染病毒的孔和两个未感染的毒性对照孔。另设六个未经处理的感染孔作为病毒对照，以及六个未经处理的未感染孔作为细胞对照。病毒分别稀释至229E、OC43、MERS和SARS冠状病毒的感染复数（MOI）为0.003、0.002、0.001和0.03 CCID50（50%细胞培养感染剂量）。将培养板置于37°C、含5% CO2的湿润气氛中培养。用中性红染料染色约2小时（±15分钟）。弃去上清染料，用磷酸盐缓冲盐水（PBS）冲洗孔，并在50:50 Sorensen柠檬酸盐缓冲液-乙醇中提取结合的染料，时间超过30分钟。用分光光度计在540 nm波长下读取光密度，并转换为对照百分比。

Animal Study:^{^[1]}

Animal Models
Male nonnaive cynomolgus monkeys
Dosages
60 mg/kg, 30mg/kg
Administration
p.o.

References

https://pubmed.ncbi.nlm.nih.gov/33558299/
https://pubmed.ncbi.nlm.nih.gov/34725982/

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SHIPPING AND STORAGE
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