A histamine H2 receptor antagonist (Ki = 0.6 μM); also acts as an inverse agonist

Cimetidine – 50 g

Brand:
Cayman
CAS:
51481-61-9
Storage:
-20
UN-No:
Non-Hazardous - /

Cimetidine is a histamine H2 receptor antagonist (Ki = 0.6 μM).{30325} It also acts as an inverse agonist, inhibiting basal cAMP production in CHO cells expressing recombinant H2 receptors (IC50 = 1.2 μM). Cimetidine inhibits histamine-induced acid secretion from isolated bullfrog gastric mucosa (IC50 = 16 μM).{30545} In vivo, it inhibits histamine-induced gastric acid secretion in gastric fistulae and Heidenhain pouches in dogs (ED50 = 1.88 μmol/kg, p.o.). Cimetidine (20 mg/kg per day) also reduces tumor growth and neovascularization in a CMT93 colon cancer mouse syngeneic model.{47643}  

 

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Description

A histamine H2 receptor antagonist (Ki = 0.6 μM); also acts as an inverse agonist, inhibiting basal cAMP production in CHO cells expressing recombinant H2 receptors (IC50 = 1.2 μM); inhibits histamine-induced acid secretion from isolated bullfrog gastric mucosa (IC50 = 16 μM); inhibits histamine-induced gastric acid secretion in gastric fistulae and Heidenhain pouches in dogs (ED50 = 1.88 μmol/kg, p.o.); reduces tumor growth and neovascularization in a CMT93 colon cancer mouse syngeneic model at 20 mg/kg per day

Formal name: N-cyano-N”-methyl-N’-[2-[[(4-methyl-1H-imidazol-5-yl)methyl]thio]ethyl]-guanidine

Synonyms:  NSC 335308|SKF 92334

Molecular weight: 252.3

CAS: 51481-61-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Receptor Pharmacology|Inverse Agonists||Research Area|Cancer|Angiogenesis||Research Area|Immunology & Inflammation|Gastric Disease

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