1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECilostazolCat. No.: HY-17464CAS No.: 73963-72-1Synonyms: OPC 13013; OPC 21分式: CHNO分量: 369.46作靶點: Phosphodiesterase (PDE); Autophagy作通路: Metabolic Enzyme/Protease; Autophagy儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 mont

2、hs-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 50 mg/mL (135.33 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.7067 mL 13.5333 mL 27.0665 mL5 mM 0.5413 mL 2.7067 mL 5.4133 mL10 mM 0.2707 mL 1.3533 mL 2.7067 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓?/p>

3、儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (6.77 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemE物活性 Cilostazol (OPC 13013; OPC 21)有效、選擇性的管系統(tǒng)中磷酸酯酶 3 亞型 PDE

4、3A 的抑制劑，IC50 值為 0.2 M 1 2。IC50 & Target IC50: 0.2 M ( PDE 3A) 1體外研究 Cilostazol selectively inhibits cGMP-inhibited phosphodiesterase (PDE 3) and is a potent inhibitor of plateletaggregation induced by various agonists 2.Cilostazol inhibits stress-induced human platelet aggregation (SIPA) dose-depend

5、ently, with an IC50 of 15 Mfor SIPA, and with a similar IC50 of 12.5 M for ADP-induced platelet aggregation 2.Cilostazol directly and effectively inhibits the activation of HSC but not of Kupffer cells 3.體內(nèi)研究 Cilostazol (100 mg; p.o.) produces a significant inhibition of SIPA in healthy volunteers 2

6、.Cilostazol (clinically used doses; p.o.; for 2 weeks) could alleviate CCl4 -induced hepatic fibrogenesis in vivo,presumably due to its direct effect to suppress HSC activation 3.Animal Model: Male C57BL/6J mice 3Dosage: 0.1% w/w, 0.3% w/wAdministration: Oral administration; fed a normal diet for 2

7、weeksResult: Exhibited a lesser fibrotic area than control groups.REFERENCES1. Schr?r K. The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9.2. Minami N, et al. Inhibition of shear stress-induced platelet aggregation by cilostazol, a specific inhibitor of cGMP-inhibitedphos

8、phodiesterase, in vitro and ex vivo. Life Sci. 1997;61(25):PL 383-9.3. Saito S, et al. Cilostazol attenuates hepatic stellate cell activation and protects mice against carbon tetrachloride-induced liver fibrosis.Hepatol Res. 2013 Apr 19.McePdfHeightCaution: Product has not been fully validated for medical applications.Fo