Isradipine

Synonyms: PN 200-110

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

Isradipine Chemical Structure

Isradipine Chemical Structure

CAS No. 75695-93-1

Purity & Quality Control

Isradipine Related Products

Biological Activity

Description Isradipine (PN 200-110) is a potent and selective L-type voltage-gated calcium channel blocker, used to treat high blood pressure.
Targets
Calcium channel [1]
In vitro
In vitro Isradipine produces inhibition of both growth cultures and oxygen consumption on epimastigotes of Trypanosoma cruzi Tulahuen strain, at micromolar concentrations. Isradipine 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
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. Isradipine prevents hypobaric hypoxia along with augmented neurodegeneration and memory impairment induced increased expression of calpain and caspase 3. [2] Isradipine (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] Isradipine 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] Isradipine suppresses the reinforcing properties of morphine and cocaine and may be an effective pharmacotherapy for treatment of cocaine and heroin abuse in mice. [5]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00753636 Completed
Parkinson''s Disease
Northwestern University|Northwestern Memorial Hospital
April 2008 Phase 2

Chemical Information & Solubility

Molecular Weight 371.39 Formula

C19H21N3O5

CAS No. 75695-93-1 SDF Download Isradipine SDF
Smiles CC1=C(C(C(=C(N1)C)C(=O)OC(C)C)C2=CC=CC3=NON=C32)C(=O)OC
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (199.25 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 74 mg/mL

Water : Insoluble


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In vivo
Batch:

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In vivo Formulation Calculator

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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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