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(R)(+)-Bay K8644

A Blocker of L-Type CaV Channels

Cat #: B-352
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 356.3
    Purity: >99% (HPLC)
    Form Lyophilized powder.
    Effective concentration 1-100 µM.
    Structure
    Chemical name (4R)-1,4-Dihydro-2,6-dimethyl-5-nitro-4-[2-trifluoromethyl)phenyl]-3-pyridinecarboxylic acid methyl ester.
    Molecular formula C16H15 F3N2O4.
    CAS No.: 98791-67-4
    Activity (R)(+)-Bay K8644 is an L-type Ca2+-channel blocker1.
    References-Activity
    1. Franckowiak, G. et al. (1985) Eur. J. Pharmacol. 114, 223.
    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 100 mM 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 (R)(+)-Bay K8644 inhibits L-type CaV channels heterologously expressed in Xenopus oocytes.
      Alomone Labs (R)(+)-Bay K8644 inhibits L-type CaV channels heterologously expressed in Xenopus oocytes.
      A. Time course of CaV1.2 (co-expressed with α2δ1 and β1 auxiliary subunits) peak current amplitude, elicited by 100 ms voltage ramp from holding potential of -100 mV to +50 mV, delivered every 10 seconds. Application of 1, 10 and 100 µM (R)(+)-Bay K8644 (#B-352) inhibits the CaV1.2 current (indicated by the horizontal bar). B. Representative current traces before and during application of 1, 10 and 100 µM (R)(+)-Bay K8644 as indicated.
    References - Scientific background
    1. Wei, X.Y. et al.  (1986) J. Pharmacol. Exp. Ther. 239, 144.
    Scientific background

    L-type Ca2+ channels possess binding sites for at least three distinct organic drug types: dihydropyridines (DHP), phenylalkylamines (PAA), and benzothiazepines (BTZ). These binding sites are known to reside in the α1 subunit of the channel.

    (R)(+)-Bay K8644 is a DHP L-type Ca2+-channel blocker with negative inotropic and vasodilatatory effects in vivo. (R)(+)-Bay K8644 shows opposite effects to (S)(-)-Bay K8644. The action of the of (R)(+)-Bay K8644 was studied in rat tail artery and guinea pig ileal longitudinal smooth muscle using pharmacologic and radioligand binding assays. (R)(+)-Bay K8644 inhibited the responses to KCI-induced depolarization with IC50 values of 16.1-25.6 nM1.

    Target L-type Ca2+ channels
    Lyophilized Powder
    Last update: 08/06/2021

    (R)(+)-Bay K8644 (#B-352) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use
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