Home Microbiology SARS-CoV inhibitor Bemnifosbuvir Hemisulfate (AT-527) For research use only.

Bemnifosbuvir Hemisulfate (AT-527)

Synonyms: RG-6422, RO 7496998

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.

Bemnifosbuvir Hemisulfate (AT-527) Chemical Structure

Bemnifosbuvir Hemisulfate (AT-527) Chemical Structure

CAS No. 2241337-84-6

Purity & Quality Control

Batch: E101301 DMSO]100 mg/mL]false]Water]100 mg/mL]false]Ethanol]100 mg/mL]false Purity: 99.37%
99.37

Bemnifosbuvir Hemisulfate (AT-527) Related Products

Biological Activity

Description

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.
Targets
SARS-CoV-2 [1]
0.47 μM(EC90)
In vitro
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]
Cell Research 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

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.
In Vivo
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]
Animal Research Animal Models Male nonnaive cynomolgus monkeys
Dosages 60 mg/kg, 30mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05618314 Recruiting
Healthy Volunteer|Renal Impairment
Atea Pharmaceuticals Inc.
 October 17 2022 Phase 1
NCT05137626 Completed
Healthy Volunteers Study
Atea Pharmaceuticals Inc.|Hoffmann-La Roche
 November 3 2021 Phase 1
NCT04309734 Withdrawn
Hepatitis C|Hepatitis C Chronic|Chronic Hepatitis C|Hepatitis C Virus Infection|HCV Infection
Atea Pharmaceuticals Inc.
 October 2021 Phase 1|Phase 2
NCT04877769 Completed
Healthy Volunteer Study
Atea Pharmaceuticals Inc.|Hoffmann-La Roche
 April 25 2021 Phase 1

Chemical Information & Solubility

Molecular Weight 630.55 Formula

C24H33FN7O7P.1/2H2O4S
CAS No. 2241337-84-6 SDF --
Smiles CNC1=C2N=C[N](C3OC(CO[P](=O)(NC(C)C(=O)OC(C)C)OC4=CC=CC=C4)C(O)C3(C)F)C2=NC(=N1)N.O[S](O)(=O)=O
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 100 mg/mL ( (158.59 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : 100 mg/mL

Ethanol : 100 mg/mL


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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