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Description: Cilostazol (formerly OPC-13013; Pletal; Cilostazolum; Pletaal; OPC13013; OPC 13013), a potent vasodilator that acts by relaxing the muscles, is a selective cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with beneficial effects on learning impairment. It inhibits PDE3 with an IC50 of 0.2 μM and inhibitor of adenosine uptake.
References: J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504; Cardiovasc Drug Rev. 2001 Winter;19(4):369-86.
Chemical Name: 6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one
InChi Key: RRGUKTPIGVIEKM-UHFFFAOYSA-N
InChi Code: 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)
SMILES Code: C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
In vitro activity: Cilostazol (OPC-13013) is a 2-oxo-quinoline derivative with antithrombotic, vasodilator, antimitogenic and cardiotonic properties. The vasodilatory and antiplatelet actions of cilostazol are due mainly to the inhibition of phosphodiesterase 3 (PDE3) and subsequent elevation of intracellular cAMP levels. Cilostazol inhibits platelet aggregation. Cilostazol also possesses the ability to inhibit adenosine uptake. Elevation of interstitial adenosine by cilostazol in the heart is shown to reduce increases in cAMP caused by the PDE3-inhibitory action of cilostazol, thus attenuating the cardiotonic effects. Cilostazol is reported to inhibit smooth muscle cell proliferation. Cilostazol relaxes vascular smooth muscle and causes vasodilatation. Cilostazol inhibits the cytokine-induced expression of monocyte chemoattractant protein-1 (MCP-1). Cilostazol reduced plasma triglycerides and raised plasma HDL-cholesterol.
Kinase Assay: Cilostazol (OPC 13013) is a potent and selective inhibitor of phosphodiesterase (PDE) 3A, the isoform of PDE 3 in the cardiovascular system, with an IC50 of 0.2 μM
Cell Assay: Cilostazol prevents platelet aggregation by specifically and selectively inhibiting PDE3 in platelets with IC50 value of 200 nM. Cilostazol also cause intracellular cAMP levels increasing by inhibiting adenosine uptake leading to increased adenosine levels in cells. Cilostazol also inhibits the expression of platelet surface P-selectin, platelet factor 4 (PF4), thromboxane B2 production release. Cilostazol also cause decrease in triglyceride levels and an increase in high-density lipoprotein.
J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504; Cardiovasc Drug Rev. 2001 Winter;19(4):369-86; Br J Pharmacol. 2010 Dec;161(8):1899-912
Purity ≥ 98%