General Information
Drug ID
DR01322
Drug Name
Cilostazol
Synonyms
Cilostazole; 3,4-Dihydro-6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-2(1H)-quinolinone; 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydro-2(1H)-quinolinone; 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydrocarbostyril; 6-(4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxyl)-3,4-dihydrocarobostyril; 6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydroquinolin-2(1H)-one; 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-2(1H)-quinolinone; 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydroquinolin-2(1H)-one; 6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one; 73963-72-1; BRN 3632107; C 0737; C20H27N5O2; CHEBI:31401; CL23867; Cilostazol (JP15/USAN/INN); Cilostazol [INN:JAN]; Cilostazole; Cilostazolum; Cilostazolum [INN-Latin]; MLS000028470; OPC 13013; OPC 21; OPC-13013; OPC-21; Otsuka brand of cilostazol; Pleta (TN); Pletaal; Pletal; Pletal (TN); Pletal, Cilostazol; UNII-N7Z035406B; cilostazol
Drug Type
Small molecular drug
Indication Intermittent claudication [ICD11:BD40.00] Approved [1]
Therapeutic Class
Vasodilator Agents
Structure
3D MOL 2D MOL
Formula
C20H27N5O2
Canonical SMILES
C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4
InChI
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)
InChIKey
RRGUKTPIGVIEKM-UHFFFAOYSA-N
CAS Number
CAS 73963-72-1
Pharmaceutical Properties Molecular Weight 369.5 Topological Polar Surface Area 81.9
Heavy Atom Count 27 Rotatable Bond Count 7
Hydrogen Bond Donor Count 1 Hydrogen Bond Acceptor Count 5
XLogP
3.1
PubChem CID
2754
PubChem SID
855683 ,6897916 ,7848958 ,7978527 ,8151779 ,11110906 ,11113335 ,11372358 ,11374323 ,11484992 ,11488934 ,11490985 ,11492587 ,11528739 ,12012700 ,14755273 ,14828756 ,17404781 ,24278291 ,26612838 ,26680450 ,26719653 ,26719654 ,26746958 ,26746959 ,29221909 ,46386747 ,46386994 ,46506317 ,47365365 ,48259412 ,48259413 ,49834949 ,50100194 ,50103999 ,50104000 ,50409718 ,53777324 ,53787948 ,56422089 ,56463107 ,57321435 ,68530811 ,85230957 ,85787626 ,87218800 ,87218801 ,87219014 ,90341176 ,92124839
ChEBI ID
CHEBI:29007
TTD Drug ID
D03VPC
DT(s) Transporting This Drug OAT3 Transporter Info Organic anion transporter 3 Substrate [2]
OATP1B1 Transporter Info Organic anion transporting polypeptide 1B1 Substrate [3]
OATP1B3 Transporter Info Organic anion transporting polypeptide 1B3 Substrate [3]
Drug-Transporter Activity Data
Drug-Transporter Activity Data OATP1B1 Transporter Info Km =17.7 microM Human embryonic kidney cells (HEK293)-OATP1B1 [3]
OATP1B3 Transporter Info Km =2.7 microM Human embryonic kidney cells (HEK293)-OATP1B3 [3]
References
1 Cilostazol was approved by FDA. The official website of the U.S. Food and Drug Administration. (2019)
2 Aspirin and probenecid inhibit organic anion transporter 3-mediated renal uptake of cilostazol and probenecid induces metabolism of cilostazol in the rat. Drug Metab Dispos. 2014 Jun;42(6):996-1007.
3 Organic Anion-Transporting Polypeptide and Efflux Transporter-Mediated Hepatic Uptake and Biliary Excretion of Cilostazol and Its Metabolites in Rats and Humans. J Pharm Sci. 2017 Sep;106(9):2515-2523.

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