product name Cimetidine
Description: Cimetidine (also known as SKF-92334) is a histamine congener that competitively inhibits histamine binding to histamine H2 receptors. Specifically, Cimetidine inhibits histamine H2-receptor and prevent stomach acid production. It is mainly used in the treatment of heartburn and peptic ulcers. Enhancing anti-tumor cell-mediated responses, cimetidine blocks histamines ability to stimulate suppressor T lymphocyte activity and to inhibit natural killer cell activity and interleukin-2 production.
References: J Pharm Biomed Anal. 2015 Mar 25;107:419-25; Hepatogastroenterology. 2013 Mar-Apr;60(122):244-7.
252.34
Formula
C10H16N6S
CAS No.
51481-61-9
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 51 mg/mL (202.1 mM)
Water: <1 mg/mL
Ethanol: 3 mg/mL (11.9 mM)
Solubility (In vivo)
Synonyms
SKF-92334
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19427197
| In Vitro |
In vitro activity: Cimetidine, a partial agonist for H2R, has a pharmacological profile different from ranitidine and famotidine, possibly contributing to its antitumor activity on gastrointestinal cancers. Cimetidine had no effect on the uptake and cytotoxicity of cisplatin in ovarian cancer cells with high OCT2 mRNA levels (IGROV-1 cells). Cimetidine showed no effect on proliferation, survival, migration and invasion of 3LL cells. Cimetidine reversed MDSC-mediated T-cell suppression, and improved IFN-γ production. Cimetidine-mediated down-regulation of NCAM involved suppression of the nuclear translocation of NF-kappaB, a transcriptional activator of NCAM gene expression. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | the antitumor efficacy of cisplatin in mice bearing luciferase-tagged IGROV-1 xenografts was unaffected by cimetidine (P = 0.39). Data obtained in 18 patients receiving cisplatin (100 mg/m(2)) in a randomized crossover fashion with or without cimetidine (800 mg × 2) revealed that cimetidine did not alter exposure to unbound cisplatin. cimetidine reduced CD11b(+)Gr-1(+) myeloid derived-suppressive cell (MDSC) accumulation in spleen, blood and tumor tissue of tumor-bearing mice. Cimetidine exerts a beneficial effect on periodontal disease in rats, decreasing the RANKL/OPG ratio in gingival connective tissue and reducing alveolar bone resorption. |
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| Formulation & Dosage | |
| References | Mol Pharmacol. 2006 Aug;70(2):450-3; Clin Pharmacol Ther. 2013 Nov;94(5):585-92; Mol Immunol. 2013 May;54(1):74-83; BMC Cancer. 2008 Dec 18;8:376. |
