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Potent and high affinity histamine H2 receptor biased inverse agonist (Kd = 14 nM, IC50 = 33 nM). Reduces basal receptor activity by 75%. Inhibits Gs-mediated pathways but acts as a partial agonist of β-arrestin recruitment (EC50 = 105 nM). Inhibits gastric acid secretion and histamine-induced mast cell activation. Also inhibits HIV replication in vitro.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 337.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.96 mL||14.82 mL||29.63 mL|
|5 mM||0.59 mL||2.96 mL||5.93 mL|
|10 mM||0.3 mL||1.48 mL||2.96 mL|
|50 mM||0.06 mL||0.3 mL||0.59 mL|
References are publications that support the biological activity of the product.
Takagi et al (1982) Effect of a new potent H2-blocker, 3-[[[2-[(diaminomethylene)amino]-4-thiazolyl]methyl]-thio]-N2-sulfamoylpropionamidine (YM-11170) on gastric secretion induced by histamine and food in conscious dogs. Arch.Int.Pharmacodyn.Ther. 256 49 PMID: 6124219
Pendleton et al (1985) Effects of H2-receptor antagonists upon physiological acid secretory states in animals. J.Pharmacol.Exp.Ther. 233 64 PMID: 2858583
Bourinbaiar & Fruhstorfer (1996) The effect of histamine type 2 receptor antagonists on human immunodeficiency virus (HIV) replication: identification of a new class of antiviral agents. Life Sci. 59 365 PMID: 8950301
Malone et al (2020) COVID-19: Famotidine, histamine, mast cells, and mechanisms. Res.Sq. - Paper not yet peer reviewed PMID: 32702719
If you know of a relevant reference for Famotidine, please let us know.
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Keywords: Famotidine, Famotidine supplier, YM, 11170, MK, 208, histamine, h2, receptor, inverse, agonists, antagonists, biased, signaling, antiviral, COVID-19, mast, cell, activation, Histamine, H2, Receptors, Antivirals, HIV, 7290, Tocris Bioscience
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