Home Metabolism PDE inhibitor Cilostazol For research use only.

Cilostazol

Synonyms: OPC-13013

Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.

Cilostazol Chemical Structure

Cilostazol Chemical Structure

CAS No. 73963-72-1

Purity & Quality Control

Cilostazol Related Products

Signaling Pathway

PDE Signaling Pathways

PDE Signaling Pathway

Biological Activity

Description Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.
Targets
PDE3 [4]
0.2 μM
In vitro
In vitro

Cilostazol (OPC-13013) is a 2-oxo-quinoline derivative with antithrombotic, vasodilator, antimitogenic and cardiotonic properties. The vasodilatory and antiplatelet actions of cilostazol are due mainly to the inhibition of phosphodiesterase 3 (PDE3) and subsequent elevation of intracellular cAMP levels. Cilostazol inhibits platelet aggregation. [1] Cilostazol also possesses the ability to inhibit adenosine uptake. [3] Elevation of interstitial adenosine by cilostazol in the heart is shown to reduce increases in cAMP caused by the PDE3-inhibitory action of cilostazol, thus attenuating the cardiotonic effects. Cilostazol is reported to inhibit smooth muscle cell proliferation. [2] Cilostazol relaxes vascular smooth muscle and causes vasodilatation. Cilostazol inhibits the cytokine-induced expression of monocyte chemoattractant protein-1 (MCP-1). Cilostazol reduced plasma triglycerides and raised plasma HDL-cholesterol . [4]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03156920 Completed
Migraine
Danish Headache Center
 May 23 2017 Not Applicable
NCT02625714 Completed
Arterial Occlusive Diseases
SK Chemicals Co. Ltd.
 June 2015 Phase 1
NCT02374957 Terminated
Peripheral Arterial Disease|Claudication (Finding)
Wake Forest University Health Sciences
 February 2015 Phase 4
NCT02098460 Unknown status
Severe Hypercholesterolemia
Otsuka Beijing Research Institute
 October 2013 Phase 4
NCT01841827 Completed
Migraine
Danish Headache Center
 April 2013 Not Applicable

Chemical Information & Solubility

Molecular Weight 369.46 Formula

C20H27N5O2
CAS No. 73963-72-1 SDF Download Cilostazol SDF
Smiles C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 74 mg/mL ( (200.29 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 6 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.

Handling Instructions

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