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(S)(-)-Bay K8644

An Activator of L-Type CaChannels
Cat #: B-351
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 356.3
    Purity: >98% (HPLC)
    Form Lyophilized powder.
    Effective concentration 50 nM - 5 µM.
    Structure
    Chemical name (4S)-1,4-dihydro-2,6-dimethyl-5-nitro-4-[2-trifluoromethyl)phenyl]-3-pyridinecarboxylic acid methyl ester.
    Molecular formula C16H15 F3N2O4.
    CAS No.: 98625-26-4.
    Activity (S)(-)-Bay K8644 is an L-type Ca2+-channel activator. It displays vasoconstrictive effects in vivo1.
    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 (S)(-)-Bay K8644 increases L-type CaV channel currents heterologously expressed in Xenopus oocytes.
      Alomone Labs (S)(-)-Bay K8644 increases L-type CaV channel currents 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 0.1 and 1 µM (S)(-)-Bay K8644 (#B-351) increases the CaV1.2 current (indicated by the horizontal bar). B. Representative current traces before and during application of 0.1 and 1 µM (S)(-)-Bay K8644 as indicated.
    References - Scientific background
    1. Hadley, R.W. and Hume, J.R. (1988) Circ. Res62, 97.
    2. Wei, X.Y. et al. (1986) J. Pharmacol. Exp. Ther239, 144.
    Scientific background (S)(-)-Bay K8644 is an L-type Ca2+-channel activator with positive inotropic, vasoconstrictive and behavioral effects in vivo. It is an enantiomer of (±)-Bay K8644. (S)(-)-Bay K8644 is a dihydropyridine that can, among other effects, constrict blood vessels and increase the force of contraction of the heart. The drug is thought to increase the entry of Ca2+ into cells by increasing the open-state probability of Ca2+ channels, either by prolonging the duration of individual openings or by increasing the number of openings. It was noted in early experiments with Bay K8644 that the dose-response curve is biphasic1. The action of (S)(-)-Bay K8644 was studied in rat tail artery and guinea pig ileal longitudinal smooth muscle using pharmacologic and radioligand binding assays. It induced concentration-dependent contractions in both smooth muscle preparations with EC50 values of 1.98-11 nM. With increasing concentrations, (S)(-)-Bay K8644 relaxed the tissue with IC50 values of 0.53-2.60 μM2.
    Target L-type Ca2+ channels
    Last update: 23/08/2020

    (S)(-)-Bay K8644 (#B-351) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
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