Isradipine Calcium Channel inhibitor

Cat.No.S1662

Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure.
Isradipine Calcium Channel inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 371.39

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 371.39 Formula

C19H21N3O5

Storage (From the date of receipt)
CAS No. 75695-93-1 Download SDF Storage of Stock Solutions

Synonyms PN 200-110 Smiles CC1=C(C(C(=C(N1)C)C(=O)OC(C)C)C2=CC=CC3=NON=C32)C(=O)OC

Solubility

In vitro
Batch:

DMSO : 74 mg/mL (199.25 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 74 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
Calcium channel [1]
In vitro
Isradipine produces inhibition of both growth cultures and oxygen consumption on epimastigotes of Trypanosoma cruzi Tulahuen strain, at micromolar concentrations. This compound is found to be the most potent derivative in both, in growth cultures (I50 = 20.8 mM) and in vivo oxygen uptake (I50 = 31.1 mM). [1]
In vivo
Isradipine reduces hypoxia-induced activation of calcium dependent xanthine oxidases, monoamine oxidases, cytosolic phospholipase A(2) and cyclooxygenases (COX-2) along with concomitant decrease in free radical generation and cytochrome c release. This compound prevents hypobaric hypoxia along with augmented neurodegeneration and memory impairment induced increased expression of calpain and caspase 3. [2] It (at the dose of 1 mg/kg three times a day) reduces ethanol intake by over 70% in ethanol-preferring rats, the reduction in ethanol intake is compensated by a proportional increase in water consumption and the inhibitory effect persisted throughout the 5 days of treatment. [3] This chemical significantly reduces the arterial wall collagen contents in both strains, with marked increases in the elastin content in the carotid but not in the aortic wall in spontaneously hypertensive rats. [4] It suppresses the reinforcing properties of morphine and cocaine and may be an effective pharmacotherapy for treatment of cocaine and heroin abuse in mice. [5]
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/7994851/
  • [5] https://pubmed.ncbi.nlm.nih.gov/1533936/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00753636 Completed
Parkinson''s Disease
Northwestern University|Northwestern Memorial Hospital
April 2008 Phase 2

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