2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation Anti-infection
  3. Histamine Receptor SARS-CoV Bacterial
  4. Ranitidine bismuth citrate

Ranitidine bismuth citrate is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine bismuth citrate antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine bismuth citrate has selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate also has anti-Helicobacter pylori infection. Ranitidine bismuth citrate inhibits breast tumor development and spread in mice.

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Ranitidine bismuth citrate Chemical Structure

Ranitidine bismuth citrate Chemical Structure

CAS No. : 128345-62-0

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Ranitidine bismuth citrate Related Antibodies

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Description

Ranitidine bismuth citrate is a potent, selective and orally active histamine H2-receptor antagonist that inhibits gastric secretion. Ranitidine bismuth citrate antagonizes Histamine (HY-B1204)-induced increases of the guinea-pig isolated rat atrium and Histamine-induced relaxations of the rat isolated uterine horn, with pA2 values of 7.2 and 6.95, respectively. Ranitidine bismuth citrate has selectivity for SARS-CoV-2-infected cells. Ranitidine bismuth citrate also has anti-Helicobacter pylori infection. Ranitidine bismuth citrate inhibits breast tumor development and spread in mice[1][2][3][4].

IC50 & Target

H2 Receptor

 

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 EC50 value of 2.3 μM in Vero E6 cells[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Ranitidine bismuth citrate Related Antibodies

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.
In Vivo

Ranitidine (0.03-3 mg/kg; i.v.; once) bismuth citrate inhibits Histamine (HY-B1204)- and Pentagastrin (HY-A0261)-induced gastric acid secretion in the perfused stomach preparation of the anaesthetized rat[1].
Ranitidine bismuth citrate (150 mg/kg; i.p.; once daily; 4 days) suppresses SARS-CoV-2 replication, and relieves virus-associated pneumonia in a golden Syrian hamster model[2].
In the rat, Ranitidine bismuth citrate (3-30 mg/kg p.o.) prevents gastric mucosal damage induced by ethanol (fundic damage) and indomethacin (antral damage)[3].
In ferrets naturally colonized with H. mustelae, Ranitidine bismuth citrate (po; 12-24 mg/kg; twice daily; for 4 weeks) causes a dose related clearance of H. mustelae[3].
Ranitidine (8 mg/kg; oral administration; administered every other day; treatment for 8 days) bismuth citrate reduces the number of CD11b+Ly6Chi cells in the spleen and bone marrow of BALB/c mice[4].
Ranitidine (8 mg/kg; oral administration; administered every other day; treatment for 8 days) bismuth citrate inhibits lung metastasis in BALB/c mice bearing 4T1 breast cancer[4].
Ranitidine (8 mg/kg; oral administration; administered every other day; for 14 days) bismuth citrate inhibits primary tumor growth in the E0771 breast cancer model of C57BL/6 mice[4].
Ranitidine (dose enabling mice to ingest 6-8 mg/kg per day; added to drinking water; changed every 3 days; treatment starting from weaning (~4 weeks) until the end of the experiment (23-26 weeks))bismuth citrate increases the latency of breast tumorigenesis and reduces the number of tumors in LKB1-/-NIC mice[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female Wistar rats (100 to 120 g) were anaesthetized with sodium pentobarbitone (50 mg/kg i.p.), and intravenous with Histamine (100 μg/kg/min) or Pentagastrin (1 μg/kg/min)[1].
Dosage: 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 0.6 mg/kg, 1 mg/kg, 3 mg/kg
Administration: i.v.; once
Result: Inhibited Histamine- and Pentagastrin-induced gastric acid secretion in the perfused stomach preparation of the anaesthetized rat.
Animal Model: Male and female Syrian hamsters (6-10 weeks)[2]
Dosage: 150 mg/kg
Administration: 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: BALB/c female mice (5-6-8 week old), orthotopic breast cancer model by injecting 100,000 4T1 cells subcutaneously into the mammary fat pad near the fourth nipple[4].
Dosage: 8 mg/kg
Administration: Oral administration, every other day, 8 days
Result: Decreased the proportion of CD11b+Ly6Chi monocytic cells in the spleen and inhibited lung metastasis.
Animal Model: C57BL/6 female mice (6-8 week old), orthotopic breast cancer model by injecting 200,000 E0771 cells in 100 μL of Matrigel subcutaneously into the mammary fat pad near the fourth nipple[4].
Dosage: 8 mg/kg
Administration: Oral administration, every other day, 8 days
Result: Decreased primary tumor growth starting from approximately day 13 post-tumor cell injection.
Animal Model: LKB1-/-/NIC female mice (weaned at about 4 weeks old), spontaneous tumor development model starting from weaning[4].
Dosage: 6-8 mg/kg
Administration: Oral administration, every 3 days, from weaning until the end of the experiment
Result: Increased the latency of tumorigenesis by an additional 24 days and reduced the average number of tumors per mouse.
Molecular Weight

712.48

Formula

C19H27BiN4O10S
CAS No.
SMILES

O=[N+](/C=C(NC)/NCCSCC1=CC=C(CN(C)C)O1)[O-].O=C(CC(C([O-])=O)(O)CC([O-])=O)[O-].[Bi+3]
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Ranitidine bismuth citrate Related Classifications

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Ranitidine bismuth128345-62-0Histamine ReceptorSARS-CoVBacterialSARS coronavirusranitidine bismuth citrateRBCorally activeHelicobacter PyloriHelicobacter mustelaeSARS-CoV-2histamine H2Inhibitorinhibitorinhibit

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