Isradipine (Dynacirc)

Calcium channel blocker CAS# 75695-93-1

Isradipine (Dynacirc)

Catalog No. BCC3797----Order now to get a substantial discount!

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Chemical structure

Isradipine (Dynacirc)

3D structure

Chemical Properties of Isradipine (Dynacirc)

Cas No. 75695-93-1 SDF Download SDF
PubChem ID 3784 Appearance Powder
Formula C19H21N3O5 M.Wt 371.39
Type of Compound N/A Storage Desiccate at -20°C
Synonyms PN 200-110
Solubility DMSO : ≥ 100 mg/mL (269.26 mM)
*"≥" means soluble, but saturation unknown.
Chemical Name 3-O-methyl 5-O-propan-2-yl 4-(2,1,3-benzoxadiazol-4-yl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylate
SMILES CC1=C(C(C(=C(N1)C)C(=O)OC(C)C)C2=CC=CC3=NON=C32)C(=O)OC
Standard InChIKey HMJIYCCIJYRONP-UHFFFAOYSA-N
Standard InChI InChI=1S/C19H21N3O5/c1-9(2)26-19(24)15-11(4)20-10(3)14(18(23)25-5)16(15)12-7-6-8-13-17(12)22-27-21-13/h6-9,16,20H,1-5H3
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months.
Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it.
About Packaging 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial.
2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial.
3. Try to avoid loss or contamination during the experiment.
Shipping Condition Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request.

Biological Activity of Isradipine (Dynacirc)

DescriptionPotent 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.

Isradipine (Dynacirc) Dilution Calculator

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Isradipine (Dynacirc) Molarity Calculator

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Preparing Stock Solutions of Isradipine (Dynacirc)

1 mg 5 mg 10 mg 20 mg 25 mg
1 mM 2.6926 mL 13.4629 mL 26.9259 mL 53.8517 mL 67.3147 mL
5 mM 0.5385 mL 2.6926 mL 5.3852 mL 10.7703 mL 13.4629 mL
10 mM 0.2693 mL 1.3463 mL 2.6926 mL 5.3852 mL 6.7315 mL
50 mM 0.0539 mL 0.2693 mL 0.5385 mL 1.077 mL 1.3463 mL
100 mM 0.0269 mL 0.1346 mL 0.2693 mL 0.5385 mL 0.6731 mL
* Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations.

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Background on Isradipine (Dynacirc)

Isradipine (tradenames DynaCirc, Prescal) is a calcium channel blocker of the dihydropyridine class. It is usually prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and heart attack.

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References on Isradipine (Dynacirc)

Separation of the coronary vasodilator from the cardiac effects of PN 200-110, a new dihydropyridine calcium antagonist, in the dog heart.[Pubmed:2580142]

J Cardiovasc Pharmacol. 1985 Jan-Feb;7(1):190-6.

Coronary vasodilator and cardiac effects of PN 200-110 were compared by use of isolated, blood-perfused sinoatrial (SA) node, atrioventricular (AV) node, and papillary muscle preparations of dogs. PN 200-110 was administered intraarterially. In all preparations PN 200-110 produced an increase in coronary blood flow. In SA node preparations, the drug produced a decrease in sinus rate and atrial standstill as well, but only in large doses. The dose that produced a 15% (nearly half-maximum) decrease in sinus rate was about three times the dose that doubled coronary blood flow. In AV node preparations, the drug produced an increase in AV conduction time and, in large doses, second- or third-degree AV block only when it was injected into the artery supplying the AV node. The dose that produced a 15% (nearly half-maximum) increase in AV conduction time was approximately 12 times the dose that doubled coronary blood flow. In paced papillary muscle preparations, the drug produced a decrease in the force of contraction. However, the dose that produced a 50% decrease in the force of contraction of the papillary muscle was approximately 14 times the dose that doubled coronary blood flow. These effects of PN 200-110 were of long duration. The drug was entirely ineffective in changing the rate of ventricular automaticity. The order of selectivity of PN 200-110 was as follows: coronary blood flow greater than SA nodal automaticity greater than AV nodal conduction greater than ventricular muscle contraction. This cardiovascular profile of PN 200-110 is slightly different from that of PY 108-068, a compound closely related to PN 200-110 in chemical structure.

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.[Pubmed:6202964]

J Cardiovasc Pharmacol. 1984 May-Jun;6(3):399-406.

The compound isopropyl 4-(2,1,3- benzoxadiazol -4-yl)-1,4-dihydro-5-methoxycarbonyl-2,6-dim ethyl-3- pyrid inecarboxylate (code name PN 200-110 [PN]) was investigated for calcium antagonistic effects in experiments in vitro. Action potentials recorded with intracellular microelectrodes in guinea pig papillary muscles were changed little by PN, 10(-7) M, except for a slight shortening of the duration of the plateau phase. Slow action potentials elicited in partially depolarized papillary muscles were gradually diminished and finally blocked by this concentration of PN. Contractile force was diminished in normal and partially depolarized muscles. The rate of spontaneously beating guinea pig right atria was decreased dose dependently, and the EC25 was 4.5 x 10(-10) M. The EC25 for the negative inotropic effects measured on paced guinea pig left atria was 1.5 x 10(-8) M. No membrane-stabilizing effects were found. Calcium-induced contraction of rabbit aorta in depolarizing bath solution was inhibited with an apparent pA2 of 10.3. Contraction elicited by graded depolarization at a constant calcium concentration was inhibited with an EC50 of 1.4 x 10(-9) M. Under resting conditions PN did not alter net uptake of 45Ca2+. KCl-stimulated uptake was inhibited with an EC50 of 3.6 x 10(-9) M. Neither noradrenaline-induced contractions nor noradrenaline-stimulated net uptake of 45Ca2+ were inhibited by a concentration of PN as high as 10(-5) M. PN thus is selective on cardiac tissue with respect to negative chronotropic versus inotropic activity and on rabbit aorta with respect to potential-operated versus receptor-operated channels.

Description

Isradipine(Dynacirc) is a calcium channel blocker with an IC50 of 34±8 μM.

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