Free shipping starts now, no minimum, no coupons required!

Nicardipine HCl

Cardene®

A Potent Dihydropyridine Blocker of Ca2+ Channels

Cat #: N-125
Alternative Name Cardene®
Lyophilized Powder yes
  • Bioassay Tested
  • Source Synthetic
    MW: 515.9
    Purity: >99%
    Effective concentration 0.1-100 μM.
    Structure
    Chemical name 5-O-[2-[benzyl(methyl)amino]ethyl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate hydrochloride.
    Molecular formula C26H29N3O6*HCl.
    CAS No.: 54527-84-3
    Activity Nicardipine HCl is a dihydropyridine that acts as an L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension1,2. Nicardipine inhibits L- and T-type CaV channels with similar potency3.
    References-Activity
    1. Ishikawa, T. et al. (1993) Circ. Res. 73, 1128.
    2. Sorkin, E.M. and Clissold, S. P. (1987) Drugs 33, 296.
    3. Furukawa, T. et al. (2005) J. Cardiovasc. Pharmacol45, 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
    • Alomone Labs Nicardipine HCl blocks L-type Ca2+ currents in Xenopus oocytes.
      Alomone Labs Nicardipine HCl blocks L-type Ca2+ currents in Xenopus oocytes.
      Superimposed current traces of L-type channels (CaV1.2+α2δ1+β1a), before and during applications of 1, 10 and 100 μM Nicardipine HCl (#N-125) as indicated on the left. Holding potential was -100 mV and currents were elicited every 10 seconds by 100 ms steps to +10 mV.
    References - Scientific background
    1. Haller, H. (2008) Int. J. Clin. Practice 62, 781.
    2. Hockerman, G.H. et al. (1997) Ann. Rev. Pharmacol. Toxicol. 37, 361.
    3. Ishikawa, T. et al. (1993) Circ. Res. 73, 1128.
    4. Sorkin, E.M. and Clissold, S. P. (1987) Drugs 33, 296.
    5. Furukawa, T. et al. (2005) J. Cardiovasc. Pharmacol45, 241.
    6. Quignard, J.F. et al. (1997) J. Clin. Invest. 99, 185.
    7. Goto, K. et al. (1989) Proc. Natl. Acad. Sci. U.S.A. 86, 3915.
    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 in which they control contraction and therefore were recognized as a therapeutic target for cardiovascular diseases1,2. Dihydropyridines (DHP) are molecules that act as allosteric modulators of L-type channels and many are used in the clinic to treat hypertension2.

    Nicardipine HCl is a dihydropyridine that acts as L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension3,4. Nicardipine inhibits L- and T-type CaV channels with similar potency5. In human coronary myocytes, nicardipine inhibited the Ca2+ currents with an IC50 of ~2 µM6, While in porcine coronary artery strips 2 nM nicardipine were effective in inhibiting the constrictive response to of this muscle to endothelin7.

    Target L-type and T-type Ca2+ channels
    Last update: 24/12/2020

    Nicardipine HCl (#N-125) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use
    Shipping and Ordering information