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Competitive β3-adrenoceptor antagonist that displays selectivity over β1 and β2 receptors (Ki values are 4.0, 204 and 390 nM for β3-, β2- and β1-adrenoceptors respectively). Inhibits cAMP accumulation in response to isoproterenol (IC50 = 6 nM). Reduces iNOS expression, attenuates nitric oxide-induced cell proliferation and induces apoptosis in a melanoma cell line.
|Storage||Store at +4°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 497.61. 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||2.01 mL||10.05 mL||20.1 mL|
|5 mM||0.4 mL||2.01 mL||4.02 mL|
|10 mM||0.2 mL||1 mL||2.01 mL|
|50 mM||0.04 mL||0.2 mL||0.4 mL|
References are publications that support the biological activity of the product.
Candelore et al (1999) Potent and selective human β3-adrenergic receptor antagonist. J.Pharmacol.Exp.Ther. 290 649 PMID: 10411574
Neidhold et al (2007) The function of α- and β-adrenoceptors of the saphenous artery in caveolin-1 knockout and wild-type mice. Br.J.Pharmacol. 150 261 PMID: 17179950
Dal Monte et al (2014) β3-adrenergic receptor activity modulates melanoma cell proliferation and survival through nitric oxide signaling. Naunyn Schmiedebergs Arch.Pharmacol. 387 533 PMID: 24599317
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Literature in this Area
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Major depressive disorder is characterized by depressed mood and a loss of interest and/or pleasure. Updated in 2015 this poster highlights presynaptic and postsynaptic targets for the potential treatment of major depressive disorder, as well as outlining the pharmacology of currently approved antidepressant drugs.