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Cilostazol
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Cilostazol图片
CAS NO:73963-72-1
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
50mg电议
100mg电议

产品介绍
Cilostazol (OPC 13013) 是一种有效的选择性磷酸二酯酶 (PDE) 3A 抑制剂,PDE 3 在心血管系统中的同工型,IC50 为 0.2 μM。
Cas No.73963-72-1
别名西洛他唑; OPC 13013
化学名6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one
Canonical SMILESC1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4
分子式C20H27N5O2
分子量369.46
溶解度≥ 15.4 mg/mL in DMSO, ≥ 3.95 mg/mL in EtOH with ultrasonic and warming
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Cilostazol is specific inhibition of cyclic nucleotide phosphodiesterase 3 (PDE3) with IC50 value of 200 nM.[1]
PDE3 is one of phosphodiesterase. PDE3 plays an important role in regulating vascular smooth muscle, heart muscle and platelet aggregation, so, it is clinically significant. The PDE3 family consists of two members including PDE3A and PDE3B. PDE3A is mainly related cardiovascular function and PDE3B is mainly related to lipolysis. The activity of PDE3 is regulated by phosphorylation pathways. PDE 3 is activited via phosphorylation at different phosphorylation sites by protein kinase A and protein kinase B. PDE3 enzymes also are involved in regulation of vascular and  cardiac smooth muscle contractility.
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. [1]
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.[2]
References:
[1].    Rondina MT, Weyrich AS: Targeting phosphodiesterases in anti-platelet therapy. Handb Exp Pharmacol 2012(210):225-238.
[2].    Hiramatsu M, Takiguchi O, Nishiyama A, Mori H: Cilostazol prevents amyloid beta peptide(25-35)-induced memory impairment and oxidative stress in mice. Br J Pharmacol 2010, 161(8):1899-1912.