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Submit ReviewIsradipine
Description: CaV1.x blocker
Alternative Names: PN 200-110
Chemical Name: 4-(2,1,3-Benzoxadiazol-4-yl)-1,4-dihydro-2,6-dimethyl-3,5-pyridinecarboxylic acid methyl 1-methylethyl ester
Purity: ≥98% (HPLC)
Biological Activity for Isradipine
Isradipine is a potent and selective L-type voltage-gated Ca2+ channel blocker. EC50 and pA2 values are 1.4 nM and 10.3 for relaxation of depolarization- and Ca2+-induced contractions of rabbit aorta respectively; EC25 = 0.45 nM for reduction in rate of spontaneously beating guinea pig right atria. Long-acting antihypertensive agent in vivo, exerting primary effects on vascular tissue with secondary negative chronotropic action.
Compound Libraries for Isradipine
Isradipine is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Isradipine
| M. Wt | 371.39 |
| Formula | C19H21N3O5 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 75695-93-1 |
| PubChem ID | 3784 |
| InChI Key | HMJIYCCIJYRONP-UHFFFAOYSA-N |
| Smiles | COC(=O)C1=C(C)NC(C)=C(C1C1=CC=CC2=NON=C12)C(=O)OC(C)C |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Isradipine
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 18.57 | 50 | |
| ethanol | 7.43 | 20 |
Preparing Stock Solutions for Isradipine
The following data is based on the product molecular weight 371.39. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.5 mM | 5.39 mL | 26.93 mL | 53.85 mL |
| 2.5 mM | 1.08 mL | 5.39 mL | 10.77 mL |
| 5 mM | 0.54 mL | 2.69 mL | 5.39 mL |
| 25 mM | 0.11 mL | 0.54 mL | 1.08 mL |
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Product Datasheets for Isradipine
References for Isradipine
References are publications that support the biological activity of the product.
Hof et al (1984) PN 200-110, a new calcium antagonist: electrophysiological, inotropic, and chronotropic effects on guinea pig myocardial tissue and effects on contraction and calcium uptake of rabbit aorta. J.Cardiovasc.Pharmacol. 6 399 PMID: 6202964
Wada et al (1985) Separation of the coronary vasodilator from the cardiac effects of PN 200-110, a new dihydropyridine calcium antagonist, in the dog heart. J.Cardiovasc.Pharmacol. 7 190 PMID: 2580142
Ruegg and Hof (1990) Pharmacology of the calcium antagonist israd. Drugs 40 3
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Keywords: Isradipine, Isradipine supplier, Ca2+, channel, blockers, L-type, Calcium, CaV, Channels, voltage-gated, voltage-dependent, PN200110, PN, 200-110, Cav1.x, 2004, Tocris Bioscience
6 Citations for Isradipine
Citations are publications that use Tocris products. Selected citations for Isradipine include:
Pourbadie et al (2015) Preventing effect of L-type calcium channel blockade on electrophysiological alterations in dentate gyrus granule cells induced by entorhinal amyloid pathology. J Neurosci 10 e0117555 PMID: 25689857
McKeithan et al (2017) An Automated Platform for Assessment of Congenital and Drug-Induced Arrhythmia with hiPSC-Derived Cardiomyocytes. Front Physiol 8 766 PMID: 29075196
Dragicevic et al (2014) Cav1.3 channels control D2-autoreceptor responses via NCS-1 in substantia nigra DA neurons. PLoS One 137 2287 PMID: 24934288
Winland et al (2017) Inflammation alters AMPA-stimulated calcium responses in dorsal striatal D2 but not D1 spiny projection neurons. Eur J Neurosci 46 2519 PMID: 28921719
Murray et al (2011) Polysynaptic excitatory postsynaptic potentials that trigger spasms after spinal cord injury in rats are inhibited by 5-HT1B and 5-HT1F receptors. J Neurophysiol 106 925 PMID: 21653728
Saszik and DeVries (2012) A mammalian retinal bipolar cell uses both graded changes in membrane voltage and all-or-nothing Na+ spikes to encode light. J Neurosci 32 297 PMID: 22219291
Do you know of a great paper that uses Isradipine from Tocris? Please let us know.
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