Cimetidine hydrochloride  (Synonyms: SKF-92334 hydrochloride)

Cimetidine (SKF-92334) hydrochloride is an orally active, inverse and BBB-permeable histamine H2 receptor antagonist with a K_i of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity^[1][2][5].

Cimetidine (SKF-92334) hydrochloride, a partial agonist for H2R, has a pharmacological profile different from ranitidine and famotidine, possibly contributing to its antitumor activity on gastrointestinal cancers [1]. Cimetidine hydrochloride has no effect on the uptake and cytotoxicity of cisplatin in ovarian cancer cells with high OCT2 mRNA levels (IGROV-1 cells)^[3].
Cimetidine hydrochloride shows no effect on proliferation, survival, migration and invasion of 3LL cells. Cimetidine hydrochloride reverses MDSC-mediated T-cell suppression, and improves IFN-γ production^[4].
Cimetidine-mediated down-regulation of NCAM involved suppression of the nuclear translocation of NF-kappaB, a transcriptional activator of NCAM gene expression^[5].

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

Cimetidine (SKF-92334) hydrochloride reduces CD11b(+)Gr-1(+) myeloid derived-suppressive cell (MDSC) accumulation in spleen, blood and tumor tissue of tumor-bearing mice^[4].
Cimetidine hydrochloride exerts a beneficial effect on periodontal disease in rats, decreasing the RANKL/OPG ratio in gingival connective tissue and reducing alveolar bone resorption^[6].

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

288.80

C₁₀H₁₇ClN₆S

70059-30-2

CC1=C(CSCC/N=C(NC)/NC#N)NC=N1.[H]Cl

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. M J Smit, et al. Inverse agonism of histamine H2 antagonist accounts for upregulation of spontaneously active histamine H2 receptors. Proc Natl Acad Sci U S A. 1996 Jun 25;93(13):6802-7.  [Content Brief]

  [2]. Takahashi, H.K., et al., Cimetidine induces interleukin-18 production through H2-agonist activity in monocytes. Mol Pharmacol, 2006. 70(2): p. 450-3.  [Content Brief]

  [3]. Sprowl, J.A., et al., Conjunctive therapy of cisplatin with the OCT2 inhibitor cimetidine: influence on antitumor efficacy and systemic clearance. Clin Pharmacol Ther, 2013. 94(5): p. 585-92.  [Content Brief]

  [4]. Zheng, Y., et al., Cimetidine suppresses lung tumor growth in mice through proapoptosis of myeloid-derived suppressor cells. Mol Immunol, 2013. 54(1): p. 74-83.  [Content Brief]

  [5]. Fukuda, M., K. Kusama, and H. Sakashita, Cimetidine inhibits salivary gland tumor cell adhesion to neural cells and induces apoptosis by blocking NCAM expression. BMC Cancer, 2008. 8: p. 376.  [Content Brief]

  [6]. Longhini, R., et al., Cimetidine Reduces the Alveolar Bone Loss in Induced Periodontitis in Rat Molars. J Periodontol, 2013.  [Content Brief]