西洛他唑
货号：
IC1880
品牌：
Jinpan
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产品简介
| MDL | MFCD00866780 |
| EC | EINECS 689-122-9 |
| InChIKey | RRGUKTPIGVIEKM-UHFFFAOYSA-N |
| InChI | 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) |
| PubChem CID | 2754 |
| 别名 | OPC 21; OPC 13013 |
| 英文名称 | Cilostazol |
| CAS | 73963-72-1 |
| 分子式 | C20H27N5O2 |
| 分子量 | 369.46 |
| 纯度 | ≥99% |
| 单位 | 瓶 |
| 生物活性 | 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[1-2]. |
| IC50 | 0.2 μM ( PDE 3A)[1] |
| In Vitro | Cilostazol selectively inhibits cGMP-inhibited phosphodiesterase (PDE 3) and is a potent inhibitor of platelet aggregation induced by various agonists.Cilostazol inhibits stress-induced human platelet aggregation (SIPA) dose-dependently, with an IC50 of 15 μM for SIPA, and with a similar IC50 of 12.5 μM for ADP-induced platelet aggregation[2]. Cilostazol directly and effectively inhibits the activation of HSC but not of Kupffer cells[3]. |
| In Vivo | ilostazol (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]. |
| SMILES | O=C1NC2=C(C=C(OCCCCC3=NN=NN3C4CCCCC4)C=C2)CC1 |
| 靶点 | Phosphodiesterase (PDE) |
| 数据来源文献 | [1]. 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-inhibited phosphodiesterase, 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. |
| 规格 | 10mg 50mg 100mg |
是一种有效的选择性磷酸二酯酶3型抑制剂（PDE3）。它也是腺苷摄取抑制剂。