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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Purity: ≥98%
Isradipine (formerly known as PN-200-110, PN-205-033, PN-205-034; DynaCirc, Prescal, Lomir) is a potent and selective L-type voltage-gated CBB/calcium channel blocker of the dihydropyridine class with antihypertensive effects. It is commonly prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and heart attack. More recent research in animal models suggests that isradipine may have potential uses for treating Parkinson's disease.
ln Vitro |
Isradipine has good brain bioavailability and a substantially higher (>40 fold) affinity for Cav1.3 channels. The efficacy of isradipine at Cav1.2 and Cav1.3 channels is almost equal[1].
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ln Vivo |
In a dose-dependent manner, isradipine (0.1~3 mg/kg; po) increases sodium excretion[3]. The striatal level of 6-hydroxydopamine-induced neurotoxicity is lessened by isradipine pretreatment. Based on data from six mice, isradipine has a dose-dependent protective effect at the striatal level. After 6-hydroxydopamine-induced degeneration, isradipine pre-treatment increases the number of surviving SNc DA cells. When intrastriatal injection of 6-hydroxydopamine is used as a slow, progressive insult, isradipine can shield SNc dopaminergic cell bodies and striatal dopaminergic terminals from it[1].
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Animal Protocol |
Animal/Disease Models: Rats[3]
Doses: 0.1~3 mg/kg Route of Administration: Po Experimental Results: Sodium excretion increased in a dose-dependent manner. |
References |
[1]. Ilijic E, et al. The L-type channel antagonist isradipine is neuroprotective in a mouse model of Parkinson's disease. Neurobiol Dis. 2011;43(2):364-371.
[2]. Campbell CA, et al. Effects of isradipine, an L-type calcium channel blocker on permanent and transient focal cerebral ischemia in spontaneously hypertensive rats. Exp Neurol. 1997;148(1):45-50. [3]. Hof RP, et al. Selective effects of PN 200-110 (isradipine) on the peripheral circulation and the heart. Am J Cardiol. 1987;59(3):30B-36B. |
Molecular Formula |
C19H21N3O5
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Molecular Weight |
371.39
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CAS # |
75695-93-1
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Related CAS # |
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Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
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SMILES |
O(C([H])(C([H])([H])[H])C([H])([H])[H])C(C1=C(C([H])([H])[H])N([H])C(C([H])([H])[H])=C(C(=O)OC([H])([H])[H])C1([H])C1=C([H])C([H])=C([H])C2C1=NON=2)=O
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO +Corn oil : 10mg/mL |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.6926 mL | 13.4629 mL | 26.9259 mL | |
5 mM | 0.5385 mL | 2.6926 mL | 5.3852 mL | |
10 mM | 0.2693 mL | 1.3463 mL | 2.6926 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.