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Cilostazol PDE inhibitor

Name: Cilostazol
Brand: Selleck Chemicals
SKU: S1294
Availability: InStock
Rating: 5 (11 reviews)

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.

Chemical Structure

Molecular Weight: 369.46

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

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Chemical Information, Storage & Stability

Molecular Weight	369.46	Formula	C₂₀H₂₇N₅O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	73963-72-1	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	OPC-13013			Smiles	C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4

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

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
=	×	×

Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.850mg/ml (5.01mM)	Taking the 1 mL working solution as an example, add 50 μL of 37 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.250mg/ml (3.38mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Calculation results:

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	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 this compound are due mainly to the inhibition of phosphodiesterase 3 (PDE3) and subsequent elevation of intracellular cAMP levels. It inhibits platelet aggregation. ^[1] This compound also possesses the ability to inhibit adenosine uptake. ^[3] 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. ^[2] 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 . ^[4]
References	[1] https://pubmed.ncbi.nlm.nih.gov/10511123/ [2] https://pubmed.ncbi.nlm.nih.gov/11830753/ [3] https://pubmed.ncbi.nlm.nih.gov/12352320/ [4] https://pubmed.ncbi.nlm.nih.gov/12180353/

Clinical Trial Information

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

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

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