U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS
This repository is under review for potential modification in compliance with Administration directives.

Details

Stereochemistry ABSOLUTE
Molecular Formula C20H27N5O2.C10H18O
Molecular Weight 523.71
Optical Activity UNSPECIFIED
Defined Stereocenters 3 / 3
E/Z Centers 0
Charge 0

SHOW SMILES / InChI
Structure of Cilostazol Dexborneol

SMILES

CC1(C)[C@@H]2CC[C@@]1(C)[C@@H](O)C2.O=C3CCC4=C(N3)C=CC(OCCCCC5=NN=NN5C6CCCCC6)=C4

InChI

InChIKey=GYOUKZRGDOIBGD-VTLWDLMQSA-N
InChI=1S/C20H27N5O2.C10H18O/c26-20-12-9-15-14-17(10-11-18(15)21-20)27-13-5-4-8-19-22-23-24-25(19)16-6-2-1-3-7-16;1-9(2)7-4-5-10(9,3)8(11)6-7/h10-11,14,16H,1-9,12-13H2,(H,21,26);7-8,11H,4-6H2,1-3H3/t;7-,8+,10+/m.1/s1

HIDE SMILES / InChI
Molecular Formula C20H27N5O2
Molecular Weight 369.4607
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE
Molecular Formula C10H18O
Molecular Weight 154.2493
Charge 0
Count
Stereochemistry ABSOLUTE
Additional Stereochemistry No
Defined Stereocenters 3 / 3
E/Z Centers 0
Optical Activity UNSPECIFIED

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/11830753

Cilostazol is a PDE3 inhibitor which is used for the treatment of intermittent claudication. The drug positively affects the platelet aggregation and may be used off-label as a measure to prevent coronary thrombosis/restenosis and stroke recurrence.

Originator

Approval Year

1999
175
Targets

Targets

Primary TargetPharmacologyConditionPotency
Inhibitor
8504
 0.57 µM [IC50]
Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Palliative
Approved
8583
CILOSTAZOL

Approved Use

Cilostazol tablets are indicated for the reduction of symptoms of intermittent claudication, as indicated by an increased walking distance.

Launch Date

2004
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
701 ng/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/31372190
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CILOSTAZOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
13724 ng × h/mL
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/31372190
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CILOSTAZOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
13.5 h
EXPERIMENT
https://www.ncbi.nlm.nih.gov/pubmed/31372190
100 mg single, oral
dose: 100 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
CILOSTAZOL plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
3.5%
DRUG LABEL
https://www.accessdata.fda.gov/drugsatfda_docs/label/2005/020863s011lbl.pdf
CILOSTAZOL plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Sourcing

Sourcing

Vendor/AggregatorIDURL
ChEBI
CHEBI:31401
https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:31401
ChemicalBook
CB2362876
https://www.chemicalbook.com/ChemicalProductProperty_EN_CB2362876
eMolecules
27518122
https://www.emolecules.com/cgi-bin/more?vid=27518122
eMolecules
535670
https://www.emolecules.com/cgi-bin/more?vid=535670
MolPort
MolPort-001-758-007
https://www.molport.com/shop/molecule-link/MolPort-001-758-007
Selleck Chemicals
Cilostazol
http://www.selleckchem.com/products/Cilostazol.html
ZINC
ZINC000001552174
http://zinc15.docking.org/substances/ZINC000001552174
PubMed

PubMed

TitleDatePubMed
Effects of cilostazol on resting ankle pressures and exercise-induced ischemia in patients with intermittent claudication.
2001
Effect of cilostazol on endothelial cell denudation and proliferation in canine vein grafts.
2001
New treatment options in intermittent claudication: the US experience.
2001 Apr
Cilostazol: a novel treatment option in intermittent claudication.
2001 Apr
A new treatment for peripheral arterial disease.
2001 Apr
[Pressure wire guide provisional coronary stent implantation].
2001 Apr
Decrease in carotid intima media thickness after 1 year of cilostazol treatment in patients with type 2 diabetes mellitus.
2001 Apr
Endothelium-dependent relaxation by cilostazol, a phosphodiesteras III inhibitor, on rat thoracic aorta.
2001 Aug 31
Differential effect of phosphodiesterase inhibitors on IL-13 release from peripheral blood mononuclear cells.
2001 Dec
Is cilostazol more effective than pentoxifylline in the treatment of symptoms of intermittent claudication?
2001 Feb
Comparison of ticlopidine and cilostazol for the prevention of restenosis after percutaneous transluminal coronary angioplasty.
2001 Jan
[Effects of cilostazol in patients with bradycardiac atrial fibrillation].
2001 Jan
Determination of cilostazol and its metabolites in human urine by high performance liquid chromatography.
2001 Jan
Cilostazol: treatment of intermittent claudication.
2001 Jan
Medical management of peripheral arterial disease.
2001 Jul-Aug
The effect of cilostazol on glucose tolerance and insulin resistance in a rat model of non-insulin dependent diabetes mellitus.
2001 Jun
Intermittent claudication: magnitude of the problem, patient evaluation, and therapeutic strategies.
2001 Jun 28
Antithrombotic therapy for prevention of pneumonia.
2001 May
Effect of cilostazol on restenosis after coronary angioplasty and stenting in comparison to conventional coronary artery stenting with ticlopidine.
2001 May
Pharmacotherapy of intermittent claudication.
2001 Nov
What can I do to continue walking despite intermittent claudication?
2001 Nov
Interplay between inhibition of adenosine uptake and phosphodiesterase type 3 on cardiac function by cilostazol, an agent to treat intermittent claudication.
2001 Nov
Management of peripheral arterial disease and intermittent claudication.
2001 Nov-Dec
Differential lipogenic effects of cilostazol and pentoxifylline in patients with intermittent claudication: potential role for interleukin-6.
2001 Oct
Systemic atherosclerosis risk and the mandate for intervention in atherosclerotic peripheral arterial disease.
2001 Oct 11
Cilostazol (pletal): a dual inhibitor of cyclic nucleotide phosphodiesterase type 3 and adenosine uptake.
2001 Winter
Cilostazol treatment of claudication in diabetic patients.
2002
Can claudication be improved with medication?
2002 Dec
Meta-analysis of results from eight randomized, placebo-controlled trials on the effect of cilostazol on patients with intermittent claudication.
2002 Dec 15
Cilostazol.
2002 Feb 1
[Etiology, pathogenesis and management of senile inflammatory pulmonary diseases].
2002 Jan
Cilostazol in intermittent claudication.
2002 Jan 1
Successful pharmacologic treatment of lower extremity ulcerations in 5 patients with chronic critical limb ischemia.
2002 Jan-Feb
Effects of a single oral dose of cilostazol on epicardial coronary arteries and hemodynamics in humans.
2002 Mar
Neuroprotective effect of cilostazol against focal cerebral ischemia via antiapoptotic action in rats.
2002 Mar
Effects of cilostazol, a selective cyclic AMP phosphodiesterase inhibitor on isolated rabbit spinal arterioles.
2002 Oct
Comparison of the effects of cilostazol and milrinone on cAMP-PDE activity, intracellular cAMP and calcium in the heart.
2002 Sep
Cilostazol: an "intermittent claudication" remedy for the management of third-degree AV block.
2003 Apr
Effects of cilostazol on serum lipid concentrations and plasma fatty acid composition in type 2 diabetic patients with peripheral vascular disease.
2003 Feb
Patents

Patents

JP2007117742A
2
JP2010525083A
52
JP2011063611A
2
JP5299949B2
2
JPH0776584A
2

Sample Use Guides

In Vivo Use Guide
The recommended dosage of cilostazol tablets is 100 mg b.i.d. taken at least half an hour before or 2 hours after breakfast and dinner.
Route of Administration: Oral
In Vitro Use Guide
In vitro assay of anti-platelet effects of cilostazol against collagen-induced aggregation using Multiplate produced a graded dose-dependent inhibition curve with IC50 value of 75.4 ± 2.4 uM while it showed a highly sensitive and all-or-none type inhibition response from 25 uM in PFA-100.
Substance Class Chemical
Created
by admin
on Wed Apr 02 17:38:43 GMT 2025
Edited
by admin
on Wed Apr 02 17:38:43 GMT 2025
Record UNII
463NWV9Y86
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
Cilostazol Dexborneol
Preferred Name English
Code System Code Type Description
FDA UNII
463NWV9Y86
Created by admin on Wed Apr 02 17:38:43 GMT 2025 , Edited by admin on Wed Apr 02 17:38:43 GMT 2025
PRIMARY
PUBCHEM
169490784
Created by admin on Wed Apr 02 17:38:43 GMT 2025 , Edited by admin on Wed Apr 02 17:38:43 GMT 2025
PRIMARY
Related Record Type Details
Structure of CILOSTAZOL
PARENT -> SALT/SOLVATE
Related Record Type Details
Structure of CILOSTAZOL
ACTIVE MOIETY
NIH
NCATS
PRIVACY ACT
ACCESSIBILITY
DISCLAIMER
HHS VULNERABILITY DISCLOSURE
For language access assistance, contact the NCATS Public Information Officer
National Center for Advancing Translational Sciences (NCATS),
6701 Democracy Boulevard, Bethesda MD 20892-4874 • 301-594-8966