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100mg | ||
250mg | ||
500mg |
ln Vitro |
Ranitidine bismuth citrate (0.1–1 μM, 5 minutes) is a strong and irreversible inhibitor of DNA unwinding (IC50 = 0.74 μM, Ki = 0.39 μM) Agent-CoV-2 helicase and SARS ATPase (IC50 = 0.69 μM, Ki = 0.97 μM) [2]. With an EC50 value of 2.3 μM in Vero E6 cells, ranitidine bismuth citrate (24 hours) demonstrated strong efficacy against SARS-CoV-2 [2].
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ln Vivo |
In the golden Syrian hamster model, ranitidine bismuth citrate (150 mg/kg; intranasally; thrice daily; 4 days) reduced SARS-CoV-2 replication and relieved virus-associated pneumonia [2]. Ranitidine bismuth citrate (48 mg/kg, intraperitoneally) is efficient in eliminating H. pylori in female ferrets and weasels, 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; oral) significantly suppresses stomach acid secretion and (1.0 mM) inhibits human pepsin isoenzyme activity [4].
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Cell Assay |
Cytotoxicity assay[2]
Cell Types: monkey kidney Vero E6 cells, human colorectal Caco-2 cells Tested Concentrations: 400-3,740 μM Incubation Duration: 48 hrs (hours) Experimental Results: demonstrated low cytotoxicity, 50% cytotoxic concentration (CC50) range 2.2 mM and 2.5 mm. |
Animal Protocol |
Animal/Disease Models: Female Beagle dog (14-20 kg) [3]
Doses: 0.1 mg/kg Route of Administration: Oral once hourly for 5 hrs (hrs (hours)) Experimental Results: Inhibition of gastric acid secretion. Animal/Disease Models: Female, randomly raised hooded rats (body weight range 90-120 g) [4] Doses: 0.5 mL/100 g Route of Administration: Pretreatment with indomethacin (5 mg/kg sc); oral Results of intragastric (po) (po) Route of Administration: Inhibition of gastric mucosal damage in rats. |
References |
[1]. Herling AW, et al. Inhibition of 14C-aminopyrine accumulation in isolated rabbit gastric glands by the H2-receptor antagonist HOE 760 (TZU-0460). Agents Actions. 1987 Feb. 20(1-2):35-9.
[2]. Yuan S, et al. Metallodrug ranitidine bismuth citrate suppresses SARS-CoV-2 replication and relieves virus-associated pneumonia in Syrian hamsters. Nat Microbiol. 2020 Nov. 5(11):1439-1448. [3]. Lambert JR, et al. The actions of bismuth in the treatment of Helicobacter pylori infection. Aliment Pharmacol Ther. 1997 Apr. 11(Suppl 1):27-33. [4]. Stables R, et al. Gastric anti-secretory, mucosal protective, anti-pepsin and anti-Helicobacter properties of ranitidine bismuth citrate. Aliment Pharmacol Ther. 1993 Jun. 7(3):237-46. |
Molecular Formula |
C13H22N4O3S.C6H5O7-3.BI+3
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Molecular Weight |
712.48348
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CAS # |
128345-62-0
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Related CAS # |
Ranitidine hydrochloride;66357-59-3
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SMILES |
[Bi+3].CN/C(/NCCSCC1=CC=C(CN(C)C)O1)=C\[N+]([O-])=O.O=C(CC(C([O-])=O)(O)CC([O-])=O)[O-]
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 1.4035 mL | 7.0177 mL | 14.0355 mL | |
5 mM | 0.2807 mL | 1.4035 mL | 2.8071 mL | |
10 mM | 0.1404 mL | 0.7018 mL | 1.4035 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.