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编 号:F144457
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生物活性:
Astodrimer (SPL7013 free base) is a large (3-4 nm,?~?16.5 kDa), negatively charged, highly-branched dendrimer, is a potent virucidal agent. Astodrimer shows antiviral and virucidal activity against a broad spectrum of viruses, including SARS-CoV-2, HIV-1, HSV-1, HSV-2, HPV. Astodrimer also has antibacterial properties.

体内研究:
Astodrimer (3%, 8 times daily for 4 days then 4 times daily for 6 days) is non-toxic to rabbit eyes and has anti-adenoviral activity in NZW rabbits.Astodrimer (1%, intranasal administration; once daily for 5 days) reduces the severity of SARS-CoV-2 replication and pathogenesis in the highly susceptible K18-hACE2 mouse model.Animal Model:Two- to three-pound female NZW rabbits (both eyes with HAdV5 following corneal scarification).
Dosage:3% SPL7013
Administration:8 times daily for 4 days then 4 times daily for 6 days
Result:Inactivated the virus, and the resulting reduction in the exposure to the virus in vivo limits SARS-CoV-2 infection, resulting in significantly lower viral loads and infectious virus in the lung, trachea, brain and liver of K18-hACE2 mic, and significantly lower pro-inflammatory cytokine production.
Animal Model:Six-to-eight-week-old K18-hACE2 mice
Dosage:1% astodrimer sodium nasal spray
Administration:Intranasal administration; 25 μL/nostril; once daily on Days 1-6.
Result:Significantly reduced the severity of SARS-CoV-2 replication and pathogenesis in the highly susceptible K18-hACE2 mouse model.

体外研究:
Astodrimer (0-10 mg/mL; 4 days) inhibits SARS-CoV-2 (hCoV-19/Australia/VIC01/2020) replication against SARS-CoV-2 (hCoV-19/Australia/VIC01/2020) infection of Vero E6 cells.Astodrimer inhibits the 2019-nCoV/USA-WA1/2020 strain with EC50 values of 0.019–0.032 mg/mL and 0.030–0.037 mg/mL for infectious virus in Vero E6 cell and Calu-3 cells, respectively.
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