| CAS |
73963-72-1 |
| Chinese Name |
西洛他唑 |
| English Name |
Cilostazol |
| Synonyms |
OPC-13013;西洛他唑;OPC 21 |
| Molecular Formula |
C20H27N5O2 |
| Molecular Weight |
369.46 |
| Solubility |
Soluble in DMSO |
| Purity |
≥99% |
| Appearance |
White to off-white Solid |
| Storage |
Powder:2-8℃，2 years;Insolvent(Mother Liquid):-20℃，6 months;-80℃，1 year |
| EC |
EINECS 689-122-9 |
| MDL |
MFCD00866780 |
| SMILES |
O=C1NC2=C(C=C(OCCCCC3=NN=NN3C4CCCCC4)C=C2)CC1 |
| 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 |
| Target Point |
Phosphodiesterase (PDE) |
| Passage |
Metabolic Enzyme&Protease |
| Background |
It is a potent and selective inhibitor of phosphodiesterase type 3 (PDE3). It is also an inhibitor of adenosine uptake. |
| Biological Activity |
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 |
0.2μM( 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]. |
| Data Literature Source |
[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. |
| Unit |
Bottle |
| Specification |
10mg 50mg 100mg |
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