Cimetidine

SKU: orb1224854

Description

Cimetidine is a histamine-2 (H2) receptor antagonist.(In Vitro):Cimetidine (SKF-92334), 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.(In Vivo):Cimetidine (SKF-92334) reduceS 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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 51481-61-9
• MW: 252.34
• Purity: >98% (HPLC)
• Formula: C₁₀H₁₆N₆S
• SMILES: CN=C(NCCSCC1=C(C)NC=N1)NC#N
• Target: Histamine Receptor
• Solubility: DMSO: 51mg/ml (202.11 mM); Water: <1mg/ml; Ethanol: 3mg/ml (11.89 mM)

Bioactivity

• In Vivo:
  Cimetidine (SKF-92334) reduceS 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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• In Vitro:
  Cimetidine (SKF-92334), 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.
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

NSC 335308 | SKF 92334

Quick Database Links

Gene Symbol

Histamine Receptor