Isradipine

DynaCirc®, Prescal®
A Potent Blocker of L-Type (both CaV1.2 and CaV1.3) Ca+ Channels
    Cat #: I-100
    Alternative Name DynaCirc®, Prescal®
  • Lyophilized Powder
  • Bioassay Tested
  • Source Synthetic
    MW: 371.4
    Purity: >99%
    Effective concentration 50 nM - 5 μM.
      • Isradipine
    Chemical name 4-(2,1,3-Benzoxadiazol-4-yl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylic acid methyl 1-methylethyl ester.
    Molecular formula C19H21N3O5.
    CAS No.: 75695-93-1.
    Activity Isradipine is a dihydropyridine that acts as an L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension1,2. Isradipine inhibits L-type channels expressed in Xenopus oocytes with IC50 = 0.2 μM at a holding potential of -80 mV and the inhibition is state dependent and increases with reduced membrane hyperpolarization2. Isradipine, was also shown recently to putatively be an effective treatment for Parkinson’s disease, by affecting particularly the excitability of certain CaV1.3 expressing dopaminergic neurons3.
      • Ganz, M. et al. (2005) J. Clin. Hypertens. 7, 27.
      • Berjukow, S. et al. (2007) J. Biol. Chem. 275, 22114.
      • Chan, C.S. et al. (2007) Nature 447, 1081.
    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.
      • Isradipine
        Alomone Labs Isradipine 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 200 nM and 1 μM Isradipine (#I-100) (indicated by bars) and upon wash. Holding potential was -80 mV and currents were elicited every 10 seconds by 100 ms ramp to +40 mV. B. Superimposed example current traces (plotted against the corresponding ramp voltage) before and during application of 200 nM and 1 μM Isradipine as indicated (taken from the experiment described in A).
    References - Scientific background
    • 1. Haller, H. (2008) Int. J. Clin. Pract. 62, 781.
    • 2. Hockerman, G. H. et al. (1997) Annu. Rev. Pharmacol. Toxicol. 37, 361.
    • 3. Ganz, M. et al. (2005) J. Clin. Hypertens. 7, 27.
    • 4. Berjukow, S. et al. (2007) J. Biol. Chem. 275, 22114.
    • 5. Bonci, A. et al. (1998) J. Neurosci. 18, 6693.
    • 6. Chan, C.S. et al. (2007) Nature 447, 1081.
    • 7. Nitert, M.D. et al. (2008) J. Mol. Endocrinol. 41, 1.
      • 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 and therefore were recognized as a therapeutic target for cardiovascular diseases1,2.

        Isradipine is a dihydropyridine that acts as a L-type, voltage-gated Ca2+ channel blocker and is used in the clinic to treat hypertension3,4. Isradipine inhibits L-type channels expressed in Xenopus oocytes with IC50 = 0.2 µM at a holding potential of -80 mV and the inhibition is state dependent and increases with reduced membrane hyperpolarization4. Slow excitatory synaptic currents in dopaminergic neurons in slices of rat substantia nigra pars compacta and ventral tegmental area, which were evoked by a train of focally delivered electrical stimuli, were depressed by isradipine (30 nM-100 µM) in a concentration-dependent and reversible manner5. In addition, isradipine, was shown recently to be a putative effective treatment for Parkinson’s disease, by affecting particularly the excitability of certain CaV1.3 expressing dopaminergic neurons6. In a pancreatic cell line, insulin secretion triggered by 16.7 mM glucose, was completely abolished by 5 µM isradipine7.

    Target CaV1.2, CaV1.3 Ca2+ channels

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    Last update: 10/10/2019

    Isradipine (#I-100) is a highly pure, synthetic, and biologically active compound.

    For research purposes only, not for human use

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