CILOSTAZOL

Details

Stereochemistry	ACHIRAL
Molecular Formula	C20H27N5O2
Molecular Weight	369.4607
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

SMILES

O=C1CCC2=C(N1)C=CC(OCCCCC3=NN=NN3C4CCCCC4)=C2

InChI

InChIKey=RRGUKTPIGVIEKM-UHFFFAOYSA-N

InChI=1S/C20H27N5O2/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/h10-11,14,16H,1-9,12-13H2,(H,21,26)

HIDE SMILES / InChI

Molecular Formula	C20H27N5O2
Molecular Weight	369.4607
Charge	0
Count	MOL RATIO 1 MOL RATIO (average)

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description

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

Targets

Primary Target	Pharmacology	Condition	Potency
Phosphodiesterase 3 61	Inhibitor 8,504		0.57 µM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Intermittent claudication 12	Palliative		Approved 8,583	CILOSTAZOL

C_max

Value	Dose	Co-administered	Analyte	Population
701 ng/mL	100 mg single, oral		CILOSTAZOL plasma	Homo sapiens

AUC

Value	Dose	Co-administered	Analyte	Population
13724 ng × h/mL	100 mg single, oral		CILOSTAZOL plasma	Homo sapiens

T_1/2

Value	Dose	Co-administered	Analyte	Population
13.5 h	100 mg single, oral		CILOSTAZOL plasma	Homo sapiens

F_unbound

Value	Dose	Co-administered	Analyte	Population
3.5%			CILOSTAZOL plasma	Homo sapiens

Sourcing

Sourcing

Show entries

Vendor/Aggregator	ID	URL
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

Showing 1 to 5 of 7 entries

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PubMed

Show entries

Title	Date	PubMed
Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity.	2000 Feb 15	10644042
Cyclic AMP inhibited proliferation of human aortic vascular smooth muscle cells, accompanied by induction of p53 and p21.	2000 Jan	10642304
Peripheral arterial disease.	2001	11795081
Novel platelet inhibitors.	2001	11160773
New treatment options in intermittent claudication: the US experience.	2001 Apr	11355276

Showing 1 to 5 of 46 entries

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Patents

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.