product name Cilostazol
Description: Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake. Cilostazol is a quinolinone-derivative medication used in the alleviation of the symptom of claudication in individuals with peripheral vascular disease. Cilostazol is a phosphodiesterase inhibitor with therapeutic focus on cyclic adenosine monophosphate (cAMP). It inhibits platelet aggregation and is a direct arterial vasodilator. Its main effects are dilation of the arteries supplying blood to the legs and decreasing platelet coagulation.
References: J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504; Cardiovasc Drug Rev. 2001 Winter;19(4):369-86.
369.46
Formula
C20H27N5O2
CAS No.
73963-72-1
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 74 mg/mL (200.3 mM)
Water: <1 mg/mL
Ethanol: 6 mg/mL warmed (16.2 mM)
Solubility (In vivo)
Synonyms
OPC-13013
other peoduct :
| In Vitro |
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: 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. |
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| In Vivo | Cilostazol may has effective function in dementia. Cilostazol has beneficial effects on learning impairment induced by Aβ25-35 in mice. Cilostazol attenuated the impairment induced by Aβ25-35 at 100 mg/kg. |
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| Formulation & Dosage | |
| References | 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 |
