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Cilostazol PDE inhibitor

Cat.No.S1294

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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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 74 mg/mL (200.29 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 6 mg/mL

Water : Insoluble

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In vivo
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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 369.46 Formula

C20H27N5O2

Storage (From the date of receipt)
CAS No. 73963-72-1 Download SDF Storage of Stock Solutions

Synonyms OPC-13013 SMILES C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4

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Mechanism of Action

Targets/IC50/Ki
PDE3
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 this compound are due mainly to the inhibition of phosphodiesterase 3 (PDE3) and subsequent elevation of intracellular cAMP levels. It inhibits platelet aggregation. This compound also possesses the ability to inhibit adenosine uptake. Elevation of interstitial adenosine by this chemical in the heart is shown to reduce increases in cAMP caused by the PDE3-inhibitory action of cilostazol, thus attenuating the cardiotonic effects. It is reported to inhibit smooth muscle cell proliferation. This agent relaxes vascular smooth muscle and causes vasodilatation. It inhibits the cytokine-induced expression of monocyte chemoattractant protein-1 (MCP-1). This compound reduced plasma triglycerides and raised plasma HDL-cholesterol .

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/12180353/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-07-31)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06530537 RECRUITING
Cerebral Microbleeds; Stroke
Zhejiang Provincial People's Hospital
2024-07-18 PHASE3
NCT07174414 NOT_YET_RECRUITING
Stroke Recurrence; Myocardial Infarction; Vascular Death; Ischemic Stroke; TIA (Transient Ischemic Attack); Stroke (CVA) or Transient Ischemic Attack; Recurrent Stroke
Stanford University
2026-08 PHASE3
NCT04753970 RECRUITING
Cerebral Small Vessel Diseases; Cerebral Autosomal Dominant Arteriopathy With Subcortical Infarcts and Leukoencephalopathy; Cerebral Microbleeding; Sporadic White Matter Disease
Mayo Clinic
2021-02-09 PHASE1; PHASE2
NCT07144956 NOT_YET_RECRUITING
Aneurysmal Subarachnoid Hemorrhage
Centre Hospitalier St Anne
2025-12-15 PHASE3
NCT06919835 NOT_YET_RECRUITING
Stroke
Northern California Institute of Research and Education
2026-08-01 PHASE3
NCT07719894 RECRUITING
Type 2 Diabetes Mellitus (T2DM); Atherosclerosis
Seoul National University Bundang Hospital
2026-05-06 PHASE4

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