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Purity: ≥98%
Cimetidine (Tagamet; Cimetag; SKF-92334; Eureceptor; Ulcedine), an approved drug used in the treatment of heartburn and peptic ulcers, is a potent histamine congener that competitively inhibits the binding of histamine to histamine H2 receptors. Cimetidine specifically inhibits the histamine H2-receptor and stops the production of stomach acid.
| Targets |
Histamine Receptor ( Ki = 0.6 μM ); H2 Receptor
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| References |
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| Molecular Formula |
C10H16N6S
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| Molecular Weight |
252.34
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| Exact Mass |
252.12
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| Elemental Analysis |
C, 47.60; H, 6.39; N, 33.30; S, 12.71
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| CAS # |
51481-61-9
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| Related CAS # |
Cimetidine hydrochloride; 70059-30-2; Cimetidine-d3; 1185237-29-9
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| Appearance |
White crystalline solid
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| SMILES |
CC1=C(N=CN1)CSCCNC(=NC)NC#N
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| InChi Key |
AQIXAKUUQRKLND-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C10H16N6S/c1-8-9(16-7-15-8)5-17-4-3-13-10(12-2)14-6-11/h7H,3-5H2,1-2H3,(H,15,16)(H2,12,13,14)
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| Chemical Name |
1-cyano-2-methyl-3-[2-[(5-methyl-1H-imidazol-4-yl)methylsulfanyl]ethyl]guanidine
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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 Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 3 mg/mL (11.89 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 3 mg/mL (11.89 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 3 mg/mL (11.89 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 3.12 mg/mL (12.36 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication (<60°C). |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9629 mL | 19.8145 mL | 39.6291 mL | |
| 5 mM | 0.7926 mL | 3.9629 mL | 7.9258 mL | |
| 10 mM | 0.3963 mL | 1.9815 mL | 3.9629 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT05020184 | Recruiting | Drug: Cimetidine Drug: Placebo |
Erythropoietic Protoporphyria X-linked Protoporphyria |
Amy K. Dickey, M.D. | June 14, 2022 | Phase 2 |
| NCT06056583 | Recruiting | Drug: Cimetidine 200 MG | Lactation | University of Washington | January 15, 2024 | Phase 4 |
| NCT04862585 | Recruiting | Drug: Cimetidine Drug: Dexamethasone Drug: Famotidine Drug: Paclitaxel |
Breast Carcinoma Anatomic Stage 0 Breast Cancer AJCC v8 |
Ohio State University Comprehensive Cancer Center |
October 7, 2021 | Phase 2 Phase 3 |
| NCT01256879 | Completed | Drug: cimetidine | Healthy | University of Maryland, Baltimore | March 2011 | Phase 4 |
| NCT03618316 | Completed | Drug: Imeglimin Drug: Cimetidine |
Healthy | Poxel SA | June 19, 2018 | Phase 1 |
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