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Carvedilol is a potent β-adrenoceptor and α1-adrenoceptor antagonist (Ki values are 0.81, 0.96 and 2.2 nM for β1-, β2- and α1-adrenoceptors respectively) that displays antihypertensive and peripheral vasodilatory activity. Blocks cardiac inward-rectifier K+ (KIR) channels, voltage-dependent Ca2+ channels and exhibits antioxidant properties at higher concentrations.
Carvedilol is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
|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|
The following data is based on the product molecular weight 406.47. 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||2.46 mL||12.3 mL||24.6 mL|
|5 mM||0.49 mL||2.46 mL||4.92 mL|
|10 mM||0.25 mL||1.23 mL||2.46 mL|
|50 mM||0.05 mL||0.25 mL||0.49 mL|
References are publications that support the biological activity of the product.
Ponicke et al (2002) Differential effects of bucindolol and carve. on noradrenaline-induced hypertonic response in ventricular cardiomyocytes of adult rats. J.Pharmacol.Exp.Ther. 301 71 PMID: 11907159
Kikuta et al (2006) Carvedilol blocks cardiac KATP and KG but not IK1 channels by acting at the bundle-crossing region. Eur.J.Pharmacol. 529 47 PMID: 16325804
Ohlstein et al (1993) Carvedilol, a cardiovascular drug, prevents vascular smooth muscle cell proliferation, migration, and neointimal formation following vascular injury. Proc.Natl.Acad.Sci.USA. 90 6189 PMID: 8327499
If you know of a relevant reference for Carvedilol, please let us know.
Keywords: Carvedilol, Carvedilol supplier, β-adrenoceptor, beta-adrenoceptor, b-adrenoceptor, β-adrenergic, beta-adrenergic, b-adrenergic, α1-adrenoceptor, alpha1-adrenoceptor, a1-adrenoceptor, a1-adrenergic, antagonists, Non-Selective, Adrenoceptors, BM14190, BM, 14190, Non-selective, Adrenergic, Beta, Receptors, Alpha-1, 2685, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Carvedilol include:
Zaytseva et al (2013) Resonant waveguide grating biosensor-enabled label-free and fluorescence detection of cell adhesion. Sens Actuators B Chem 188 PMID: 24319319
Ajmo et al (2009) Blockade of adrenoreceptors inhibits the splenic response to stroke. Nat Commun 218 47 PMID: 19371742
Baker et al (2011) Predicting in vivo cardiovascular properties of β-blockers from cellular assays: a quantitative comparison of cellular and cardiovascular pharmacological responses. FASEB J 25 4486 PMID: 21865315
Do you know of a great paper that uses Carvedilol from Tocris? Please let us know.
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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.