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.
引用文献 (Citations)
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製品資料 (Product Documents)
Purity:>99.50%Appearance:A solid
化学的性質 (Chemical Properties)
CAS番号
73963-72-1
同義語
OPC 13013, OPC 21, Pletaal, Pletal
化学名
6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one
SMILES
C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4
分子式
C20H27N5O2
分子量
369.46
溶解性
≥ 15.4 mg/mL in DMSO, ≥ 3.95 mg/mL in EtOH with ultrasonic and warming
保存条件
Store at -20°C
一般的な注意事項
製品の溶解性データに基づいて適切な溶媒を選択してください。調製後は、凍結融解の繰り返しを避けるため、ストック溶液を小分けしてください。
ストック溶液は、-80°Cで保存する場合は6か月以内、-20°Cで保存する場合は1か月以内に使用してください。
溶解性を高めるには、チューブを37°Cに温め、適切な時間超音波処理してください。
ストック溶液は、-80°Cで保存する場合は6か月以内、-20°Cで保存する場合は1か月以内に使用してください。
溶解性を高めるには、チューブを37°Cに温め、適切な時間超音波処理してください。
配送条件
評価用サンプルは保冷剤とともに発送します。その他の容量は室温で発送し、ご要望に応じて保冷剤を同梱します。
計算ツール (Calculators)モル濃度 / 希釈 / 分子量 / 単位変換 / in vivo製剤 / 溶解度
g/mol
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