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.
    Structure
    • 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.
    References-Activity
    1. Burges, R.A. et al. (1987) J. Cardiovasc. Pharmacol. 9, 110.
    2. Julius, S. et al. (2004) Lancet 363, 2022.
    3. 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.
    Our bioassay
    • 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.
    Scientific background

    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: 24/01/2020

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

    For research purposes only, not for human use

    Applications

    Specifications

    Scientific Background

    Citations

    Citations
    Shipping and Ordering information