Cilostazol

Catalog No.S1294 Synonyms: OPC-13013

Cilostazol Chemical Structure

Molecular Weight(MW): 369.46

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

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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

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]

Protocol

Solubility (25°C)

In vitro DMSO 74 mg/mL (200.29 mM)
Ethanol 6 mg/mL warmed (16.23 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 369.46
Formula

C20H27N5O2
CAS No. 73963-72-1
Storage powder
in solvent
Synonyms OPC-13013

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03156920 Completed Drug: Placebo|Drug: Sumatriptan Migraine Danish Headache Center May 23 2017 Not Applicable
NCT02625714 Completed Drug: Renexin®|Drug: SID142 Arterial Occlusive Diseases SK Chemicals Co. Ltd. June 2015 Phase 1
NCT02374957 Terminated Drug: Cilostazol Peripheral Arterial Disease|Claudication (Finding) Wake Forest University Health Sciences February 2015 Phase 4
NCT02098460 Unknown status Drug: Atorvastatin Probucol Cilostazol Severe Hypercholesterolemia Otsuka Beijing Research Institute October 2013 Phase 4
NCT01841827 Completed Drug: Cilostazol|Drug: Placebo Migraine Danish Headache Center April 2013 Not Applicable
NCT00886574 Unknown status Drug: Cilostazol|Drug: Aspirin Type 2 Diabetes Mellitus Hanyang University|Ajou University School of Medicine|Kyunghee University Medical Center|Korea University Guro Hospital|Inha University Hospital|Inje University|Hallym University Medical Center April 2009 Phase 4

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PDE Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID