Cilostazol(OPC-13013 OPC13013 OPC 13013)

Molecular Weight (MW)	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)
Other info	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
Synonyms	OPC-13013; Cilostazol; Pletal; Cilostazolum; OPC 13013; OPC13013; Pletaal; Cilostazole;

Molecular Weight (MW)

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)

Other info

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

Synonyms

OPC-13013; Cilostazol; Pletal; Cilostazolum; OPC 13013; OPC13013; Pletaal; Cilostazole;

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: 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.
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.
Animal model	Mice
Formulation & Dosage	100 mg/kg
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

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: 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.

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.

Animal model

Mice

Formulation & Dosage

100 mg/kg

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

CAS NO:	73963-72-1
规格:	≥98%

包装	价格(元)
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议
1g	电议
2g	电议
5g	电议
10g	电议