Bemnifosbuvir

SKU: orb1940237

Description

Bemnifosbuvir is a novel phosphoramidate prodrug of 2'-fluoro-2'-C-methylguanosine-5'-monophosphate that has potent in vitro activity against HCV.(In Vitro):AT-511 is a novel phosphoramidate prodrug of 2'-fluoro-2'-C-methylguanosine-5'-monophosphate that has potent in vitro activity against HCV.In the absence of cells, AT-511 was stable when incubated in culture medium at 37°C for up to 24 h. AT-9010 was the predominant intracellular metabolite measured in all hepatocyte species and Huh-7 cell incubations with 10 μM AT-511 and, except in mouse hepatocytes,far exceeded intracellular AT-511 concentrations,demonstrating that the active TP was efficiently formed from its phosphoramidate protide in liver cells. In hepatocyte incubations, the relative levels of AT-9010 formed, and its accumulation over 24 h expressed as area under the curve or AUC0-24h; from most to least abundant, were rat>human >mouse >dog/monkey.(In Vivo):Treatment with moxifloxacin every 8 hr was accompanied by longer survival than in any other group.Tissue cultures 30 hr after bacterial challenge showed considerably less bacterial growth in the spleens and lungs of moxifloxacin-treated animals than in the other groups, but not in their livers.

Key Properties

• CAS Number: 1998705-64-8
• MW: 581.53
• Purity: >98% (HPLC)
• Formula: C₂₄H₃₃FN₇O₇P
• SMILES: CC(OC([C@@H](N[P@](OC[C@@H]1[C@H]([C@](C)([C@](N2C=NC3=C(N=C(N=C32)N)NC)(O1)[H])F)O)(OC4=CC=CC=C4)=O)C)=O)C
• Solubility: In Vitro: DMSO : 200 mg/mL (343.92 mM)

Bioactivity

• In Vivo:
  When given orally to rats (500 mg/kg) and monkeys (30 mg/kg, 100 mg/kg or 300 mg/kg), Bemnifosbuvir preferentially delivers high levels of AT-9010 in the liver In vivo.
• In Vitro:
  Bemnifosbuvir has pan-genotypic antiviral activities that inhibits HCV genotype 1a (HCV GT1a), HCV GT1b, HCV GT2a, HCV GT3a, HCV GT4a, and HCV GT5a replication with EC50 values of 12.8 nM, 12.5 nM, 9.2 nM, 10.3 nM, 14.7 nM, and 28.5 nM, respectively. In normal human airway epithelial cells, the concentration of Bemnifosbuvir required to inhibit replication of SARS-CoV-2 by EC90 is 0.47 μM, very similar to its EC90 against HCoV-229E, HCoV-OC43 and SARS-CoV in Huh-7 cells.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

AT-511