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KI1083Cilostazol25 mg$154
Cilostazol100 mg$432

Chemical Characteristic

Product NameCilostazol
SynonymsPletal
CAS No.73963-72-1
Molecular Weight 369.46
FormulaC20H27N5O2
Chemical Name6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydroquinolin-2(1H)-one
SmilesN1C(=O)CCc2cc(ccc12)OCCCCc1n(nnn1)C1CCCCC1
Chemical Structure

Biological activities

Cilostazol is a phosphodiesterase 3 inhibitor with antiplatelet and antithrombotic properties. Cilostazol is used for a treatment of ischemic symptoms related to peripheral arterial occlusive diseases and intermittent claudication. In vitro, cilostazol inhibits lipopolysaccharide (LPS)-induced monocyte chemoattractant protein-1 (MCP-1) and matrix metalloproteinase-9 (MMP-9) expression. Cilostazol significantly inhibits LPS-induced activation of p38, JNK, and nuclear factor-κB.[1] Cilostazol inhibits stress-induced platelet aggregation (SIPA) with an IC50 of 15 µM. And the IC50 for inhibition of 2 µM ADP-induced platelet aggregation is 12.5 µM. [2] Cilostazol exerts its antiplatelet effect through a slight increase in cAMP level in human platelet by inhibiting the activity of PDE. [3] In vivo, cilostazol administered with LPS reduces neointimal hyperplasia and macrophage infiltration in the balloon-injured rabbit aorta. [1] Doses above 30 mg/kg p.o. cilostazol inhibit thrombotic occlusion in an artificial vessel implanted in the femoral artery of a dog. [3]

Protocols

Cilostazol is dissolved in DMSO and diluted with saline. [2]

References

[1] Tsai CS, et al. Cilostazol attenuates MCP-1 and MMP-9 expression in vivo in LPS-administrated balloon-injured rabbit aorta and in vitro in LPS-treated monocytic THP-1 cells. J Cell Biochem. 2008, 103(1): 54-66.
[2] Minami N, et al. Inhibition of shear stress-induced platelet aggregation by cilostazol, a specific inhibitor of cGMP-inhibited phosphodiesterase, in vitro and ex vivo. Life Sci. 1997, 61(25): PL 383- PL 389.
[3] Okuda Y, et al. Cilostazol. Cardiovascular Drug Reviews. 1993, 11(4): 451??65.

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