Amlodipine

Norvasc®
A Potent Blocker of L-type and T-type CaV Channels
Cat #: A-110
Alternative Name Norvasc®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 408.9
    Purity: >96%
    Effective concentration 1-100 µM.
    Chemical name 3-O-ethyl 5-O-methyl 2-(2-aminoethoxymethyl)-4-(2-chlorophenyl)-6-methyl-1,4-dihydropyridine-3,5-dicarboxylate.
    Molecular formula C20H25ClN2O5.
    CAS No.: 88150-42-9.
    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.
    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.
      • Alomone Labs Amlodipine inhibits L-type voltage-gated Ca2+ currents heterologously expressed in Xenopus oocytes.
        A. Time course of CaV1.2/α2-δ1/β2a (L-type) current inhibition by 10 µM of Amlodipine (#A-110). Currents were elicited by application of voltage steps from a holding potential of -100 mV to 0 mV (100 msec). B. Superimposed example traces of current responses before and during perfusion of 10 µM Amlodipine as indicated.
      • 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 in which they control contraction and therefore were recognized as a therapeutic target for cardiovascular diseases1,2.

        Dihydropyridines (DHP) are molecules that acts as allosteric modulators of L-type channels and many are used in the clinic to treat hypertension2,3. Amlodipine besylate is a DHP that acts as a L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension3,4. Amlodipine inhibit Ca2+ -induced contractions in depolarised rat aorta (IC50 1.9 nM) but, displays a very slow onset of action. Contractions induced by depolarising steps with 45 mM K+ are much 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: 03/03/2019

    Amlodipine (#A-110) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use