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编 号:F109388
分子式:C19H27BiN4O10S
分子量:712.48
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生物活性:
Ranitidine bismuth citrate is an orally active Histamine H2-receptor antagonist with an IC50 of 3.3 μM. Ranitidine bismuth citrate has high selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate is a commonly used agent anti-Helicobacter pylori infection with an MIC90 value of 16 ng/L.

体内研究:
Ranitidine bismuth citrate (150?mg/kg; intranasally inoculation; once daily; 4 days) suppresses SARS-CoV-2 replication, and relieves virus-associated pneumonia in a golden Syrian hamster model.Ranitidine bismuth citrate (48 mg/kg, i.p.) is effective in eradicating H. pylori and H. mustelae in female ferrests with MIC values of 8 ng/L and 1-2 ng/L, respectively.Ranitidine bismuth citrate (0.1 mg/kg, 0.3 mg/kg; p.o.) is effective in inhibiting gastric acid secretion and (1.0 mM) inhibits human pepsin isoenzymes activity.Animal Model:Male and female Syrian hamsters (6–10?weeks)
Dosage:150?mg/kg
Administration:Intranasally inoculation; intraperitoneally given; once daily; 4 days
Result:Suppressed SARS-CoV-2 replication, and relieved virus-associated pneumonia in a golden Syrian hamster model.
Animal Model:Female Beagle dogs (14-20 kg)
Dosage:0.1 mg/kg
Administration:Oral dosed every hour, for 5 hours
Result:Inhibited gastric acid secretion.
Animal Model:Female, random-bred hooded rats (weight range 90-120 g)
Dosage:0.5 mL/100 g
Administration:Pre-treated with indomethacin (5 mg/kg s.c.); oral gavage
Result:Inhibited gastric mucosal damage in the rat.

体外研究:
Ranitidine bismuth citrate (0.1-1 μM, 5 min) is a potent irreversible inhibitor of both the ATPase (IC50=0.69?μM, Ki =0.97?μM ) and DNA-unwinding (IC50?=0.74?μM, Ki =0.39 ?μM) of the SARS-CoV-2 helicase.Ranitidine bismuth citrate (24 hours) shows potent activity against SARS-CoV-2 with an EC50 value of 2.3 μM in Vero E6 cells.
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