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(±)-Bay K8644

An L-Type Voltage-Gated Ca2+ Channel Activator

Cat #: B-350
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 356.3
    Purity: >99% (HPLC)
    Effective concentration 1-5 μM.
    Structure
    Chemical name 1,4-Dihydro-2,6-dimethyl-5-nitro-4-[2-(trifluoromethyl) phenyl]-3-pyridinecarboxylic acid, methyl ester.
    Molecular formula C16H15F3N2O4.
    CAS No.: 71145-03-4
    Activity (±)-Bay K8644 is a dihydropyridine that acts as an L-type, voltage-gated Ca2+ channel agonist. The (-)-enantiomer has strong Ca2+ channel agonist properties, whereas the (+)-enantiomer has weak Ca2+ channel antagonist activity. The net activity of the racemic mix is L-type channel opening. In the presence of this agonist, channels tend to open for longer periods causing a large increase in the channel microscopic response1-4. (±)-Bay K8644 is also an inhibitor (by increasing the inactivation) of a Shaker KV channel5.
    References-Activity
    1. Hess, P. et al. (1984) Nature 311, 538.
    2. Nowycky, M.C. et al. (1985) Proc. Natl. Acad. Sci. U.S.A. 82, 2178.
    3. Bechem, M. and Hoffmann, H. (1993) Pflugers Arch. 424, 343.
    4. Triggle, D.J. and Rampe, D. (1989) Trends Pharmacol. Sci. 10, 507.
    5. Avdonin, V. et al. (1997) J. Gen. Physiol. 109, 169.
    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 Ethanol, methanol or DMSO. Centrifuge all product preparations before use (10000 x g 5 min).
    Storage of solutions Up to four weeks at 4°C or three months at -20°C.
    Our bioassay
    • Alomone Labs (±)-Bay K8644 increases L-type Ca2+ currents expressed in Xenopus oocytes.
      Alomone Labs (±)-Bay K8644 increases L-type Ca2+ currents expressed in Xenopus oocytes.
      Left: I-V relation before (squares) and during (circles) bath perfusion of 5 μM (±)-Bay K8644 (#B-350). Right: An example of current response to 200 ms depolarization to +20mV (from holding potential of -100 mV) before (black) and during (pink) perfusion of (±)-Bay K8644.
    • Alomone Labs (±)-Bay K8644 modulates the phosphorylation of ERK1/2 MAPK in Jurkat T cells.
      Alomone Labs (±)-Bay K8644 modulates the phosphorylation of ERK1/2 MAPK in Jurkat T cells.
      Cells were preincubated with or without EGTA or Nifedipine for 20 min then stimulated with (±)-Bay K8644 (#B-350) or with Ionomycin for 10 min. The cell proteins were blotted and probed with anti-phospho ERK1/2 (upper panel) or with anti-ERK1/2 (lower panel).
    References - Scientific background
    1. Hess, P. et al. (1984) Nature 311, 538.
    2. Nowycky, M.C. et al. (1985) Proc. Natl. Acad. Sci. U.S.A. 82, 2178.
    3. Bechem, M. and Hoffmann, H. (1993) Pflugers Arch. 424, 343.
    Scientific background

    (±)-Bay K8644 is an opener of all L-type channels (CaV1 family). In the presence of this agonist, channels tend to open for longer periods causing a large increase in the channel macroscopic response.

    The net activity of the racemic mix is that of the (-)-enantiomer agonistic activity.

    (±)-Bay K8644 is a widely used L-type Ca2+ channel activator in various neuronal, muscle, endocrine, thyroid and other cell types.1-3

    Target L-type Ca2+ channels
    Lyophilized Powder
    Last update: 25/07/2021

    (±)-Bay K8644 (#B-350) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use

    Applications

    Citations

    Citations
    Product citations
    1. Dahan, T. et al. (2017) Diabetes 66, 426.
    2. Teraoku, H. and Lenzen, S. (2017) J. Diabetes Res. 2017, 2309630.
    3. Gurgul-Convey, E. (2015) Biochem. Biophys. Res. Commun. 464, 13.
    4. He, S. et al. (2014) J. Neurosci. 34, 5261.
    5. Dominguez, B. et al. (2009) Am. J. Physiol. 296, E1148.
    6. Kaisman-Elbaz, T. et al. (2009) J. Cell. Physiol. 220, 222.
    7. Husch, A. et al. (2008) J. Neurophysiol. 99, 320.
    8. Hutchins, B.I. and Kalil, K. (2008) J. Neurosci. 28, 143.
    9. Perissinotti, P.P. et al. (2008) Eur. J. Neurosci. 27, 1333.
    10. Worrell, J.W. and Levine, R.B. (2008) J. Neurophysiol. 100, 868.

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