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Nisoldipine

Sular®
A Potent and Selective Blocker of L-type CaV Channels
Cat #: N-160
Alternative Name Sular®
Lyophilized Powder yes
  • Bioassay Tested
    • Source Synthetic
    MW: 388.4
    Purity: >98%
    Effective concentration 10 nM - 1000 µM.
    Structure
    Chemical name (±)-Isobutyl methyl 1,4-dihydro-2,6-dimethyl-4-(o-nitrophenyl)-3,5-pyridinedicarboxylate.
    Molecular formula C20H24N2O6.
    CAS No.: 63675-72-9
    Activity 10 nM completely inhibited L-type currents expressed in HEK-293 cells1. The IC50 value of nisoldipine was 2.2 and 0.084 μM in oocytes injected with α1β and α1β α2, respectively2.
    References-Activity
    1. Hu, H. and Marban, E. (1998) Mol. Pharmacol. 53, 902.
    2. Wei, X. et al. (1995) J. Biol. Chem. 270, 27106.
    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 Nisoldipine inhibits CaV1.2 currents expressed in Xenopus oocytes.
      Alomone Labs Nisoldipine inhibits CaV1.2 currents expressed in Xenopus oocytes.
      A. Time course of CaV1.2/α2-δ1/β2a (L-type) current inhibition by 200 and 1000 µM of Nisoldipine (#N-160). 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 200 and 1000 µM Nisoldipine as indicated.
    References - Scientific background
    1. Furukawa, T. et al. (1999) J. Pharmacol. Exp. Ther. 291, 464.
    2. Hering, S. et al. (1998) Trends Pharmacol. Sci. 19, 439.
    3. Hockerman, G.H. et al. (1997) Ann. Rev. Pharmacol. Toxicol. 37, 361.
    4. Haller, H. (2008) Int. J. Clin. Practice 62, 781.
    Scientific background

    Native voltage-gated Ca2+ channels (VGCC, CaV) are pharmacologically classified into at least five different subclasses (L-, N-, P-, Q-, and R-type), the characteristics of which are determined by the pore-forming α1 subunit. The subunits CaV1.1-1.4 (α1S, α1C, α1D and α1F) form L-type Ca2+ channels and bind dihydropyridines (DHPs) with high affinity1,2. Nisoldipine, a DHP, is a selective L-type Ca2+ channel blocker.
    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 diseases3,4.

    10 nM of nisoldipine completely inhibited L-type currents expressed in HEK-293 cells1. The IC50 value of nisoldipine was 2.2 and 0.084 μM in oocytes injected with α1/β2a and α1/β2a/α2δ, respectively2.

    Target L-type Ca2+ channels
    Lyophilized Powder
    Last update: 24/12/2020

    Nisoldipine (#N-160) is a highly pure, synthetic, and biologically active compound.

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    For research purposes only, not for human use

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    L-Type (CaV1) Channels

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