Amlodipine besylate

Norvasc®
A Potent Blocker of L-Type and T-Type CaV Channels
    Cat #: A-120
    Alternative Name Norvasc®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 567.1
    Purity: >99%
    Effective concentration 1-100 μM.
      • Amlodipine besylate
    Chemical name 2-[(2-Aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester benzenesulfonate.
    Molecular formula C20H25ClN2O5*C6H6O3S.
    CAS No.: 111470-99-6.
    Activity Amlodipine besylate is a dihydropyridine that acts as an L-type voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension1,2. Amlodipine besylate inhibits L- and T-type CaV channels with similar potency3.
      • Burges, R.A. et al. (1987) J. Cardiovasc. Pharmacol. 9, 110.
      • Julius, S. et al. (2004) Lancet 363, 2022.
      • Furukawa, T. et al. (2005) J. Cardiovasc. Pharmacol. 45, 241.
    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 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.
      • Amlodipine besylate
        Alomone Labs Amlodipine besylate blocks L-type Ca2+ currents in Xenopus oocytes.
        A. Time course of L-type channel (CaV1.2+α2δ1+β1a) activity before and during applications of 100 μM Amlodipine besylate (#A-120) (green) and upon wash. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms steps to 0 mV. B. Example current traces before (black) and during application of 100 μM Amlodipine besylate (taken from the experiment described in A).
    References - Scientific background
    • 1. Hockerman, G.H. et al. (1997) Annu. Rev. Pharmacol. Toxicol. 37, 361.
    • 2. Haller, H. (2008) Int. J. Clin. Pract. 62, 781.
    • 3. Julius, S. et al. (2004) Lancet 363, 2022.
    • 4. Burges, R.A. et al. (1987) J. Cardiovasc. Pharmacol. 9, 110.
    • 5. Furukawa, T. et al. (2005) J. Cardiovasc. Pharmacol. 45, 241.
      • L-type (CaV1) voltage-gated Ca2+ channels are plasma membrane protein complexes which allow the passage of Ca2+ ions into cells following depolarization of the membrane potential. L-type channels are widely expressed in cardiac and smooth muscle where they control contraction. Consequently, these channels were recognized as a therapeutic target for cardiovascular diseases1,2.

        Dihydropyridines (DHP) are molecules that act as allosteric modulators of L-type channels. Many are used in the clinic to treat hypertension2,3. Amlodipine besylate is a DHP that acts as an L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension3,4. Amlodipine inhibits Ca2+-induced contractions in depolarised rat aorta (IC50 1.9 nM) but displays a very slow action onset. Contractions induced by depolarising steps with 45 mM K+ are far less potently blocked by amlodipine (IC50 19.4 nM) and guinea pig papillary muscle single-cell slow action potentials are blocked at a concentration of 5 mM4. Amlodipine besylate inhibits L- and T-type CaV channels with similar potency5.

    Target L-type and T-type Ca2+ channels
    Last update: 22/09/2019

    Amlodipine besylate (#A-120) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Citations
    Related Products