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A Blocker of KV1.5, Kir3.2 and Kir2.3 Channels and an Antagonist of Adrenoceptors

Cat #: C-180
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 406.47
    Purity: >97%
    Form Lyophilized powder.
    Effective concentration 0.1-300 µM.
    Chemical name 1-(9H-carbazol-4-yloxy)-3-[2-(2-methoxyphenoxy)ethylamino]propan-2-ol.
    Molecular formula C24H26N2O4.
    CAS No.: 72956-09-3
    Activity Carvedilol is a blocker of KV1.5 channels with IC50 ~0.5 μM1. It also blocks Kir2.3 channels2 and antagonizes adrenoceptors3.
    1. Jeong, I. et al. (2012) Biochem. Pharmacol. 83, 497.
    2. Ferrer, T. et al. (2011) Eur. J. Pharmacol. 668, 72.
    3. Beattie, K. et al. (2013) Profiles Drug Subst. Excip. Relat. Methodol. 38, 113.
    Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
    Solubility 100mM in DMSO . Centrifuge all product preparations before use (10000 x g for 1 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs Carvedilol inhibits Kir3.2 channels expressed in Xenopus oocytes.
      Alomone Labs Carvedilol inhibits Kir3.2 channels expressed in Xenopus oocytes.
      Application of 300 µM Carvedilol (#C-180, bottom bar) reversibly inhibits Kir3.2 channel currents. Kir3.2 channels were activated by continuous application of high K+ containing solution (top bar) at a holding potential of -80 mV, resulting in a downward deflection of the continuously recorded current trace.
    References - Scientific background
    1. Stafylas, P.C. and Sarafidis, P.A.  (2008) Vasc. Health Risk Manag4, 23.
    2. Yue, T.L. et al. (1992) J. Pharmacol. Exp. Ther263, 92.
    3. Beattie, K. et al. (2013) Profiles Drug Subst. Excip. Relat. Methodol. 38, 113.
    4. Dulin, B. and Abraham, W.T. (2004) Am. J. Cardiol. 93, 3B.
    5. Jeong, I. et al. (2012) Biochem. Pharmacol. 83, 497.
    6. Ferrer, T. et al. (2011) Eur. J. Pharmacol. 668, 72.
    Scientific background Carvedilol is a potent nonselective β1-, β2-, and α1-adrenoceptor antagonist1 with an IC50 of 3.8 µM2. Carvedilol is also a vasodilator with anti-oxidant, anti-inflammatory, anti-fibrotic and anti-proliferative effects. It has “atypical” effects on β-receptors mediated by an interaction with G proteins that leads to down-regulation of receptors in model systems. Experimental models demonstrate that Carvedilol blocks α1-, β1-, and β2-adrenergic receptors without exhibiting high levels of inverse agonist activity3. The lack of inverse agonist activity and intrinsic sympathomimetic activity (ISA) reduces the side-effects and makes the compound better tolerated than the older β-blockers. The pharmacologic effects of Carvedilol are related to the inhibition of multiple neurohormonal pathways. Additional studies indicate that some of the efficacy of Carvedilol may be associated with its effects on levels of inflammatory cytokines4. Carvedilol also blocks KV1.5 channels independently of its action on adrenoceptors5, as well as Kir2.3 and Kir3.2 channels6.
    Target KV1.5, Kir2.3, Kir3.2 K+ channels, adrenoceptors
    Last update: 12/08/2021

    Carvedilol (#C-180) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use



    Scientific Background

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