Ranitidine bismuth citrate 是一种具有口服活性的组胺 H2 受体 (Histamine H2-receptor) 拮抗剂，IC50为 3.3 μM。Ranitidine bismuth citrate 对 SARS-CoV-2 感染的细胞具有高选择性。Ranitidine bismuth citrate 是抗幽门螺杆菌 (Helicobacter Pylori) 感染的常用试剂，MIC90为 16 ng/L。
| 生物活性 | Ranitidine bismuth citrate is an orally activeHistamine H2-receptorantagonist with anIC50of 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 pyloriinfectionwith an MIC90value of 16 ng/L[1][2][3]. |
| IC50& Target | |
体外研究
(In Vitro) | 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[2].
Ranitidine bismuth citrate (24 hours) shows potent activity against SARS-CoV-2 with an EC50value of 2.3 μM in Vero E6 cells[2].
Cell Cytotoxicity Assay[2] | Cell Line: | Monkey kidney Vero E6 cells, human colorectal Caco-2 cells | | Concentration: | 400-3,740 μM | | Incubation Time: | 48 hours | | Result: | Showed low cytotoxicity with the 50% cytotoxicity concentrations (CC50) ranging from 2.2 mM and 2.5 mM. |
|
体内研究
(In Vivo) | 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[2].
Ranitidine bismuth citrate (48 mg/kg, i.p.) is effective in eradicatingH. pyloriandH. mustelaein female ferrests with MIC values of 8 ng/L and 1-2 ng/L, respectively[3].
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[4].
| Animal Model: | Male and female Syrian hamsters (6–10 weeks)[1] | | 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)[3] | | 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)[4] | | 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. |
|
| 分子量 | |
| Formula | |
| CAS 号 | |
| 中文名称 | |
| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
