Cilostazol

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Cilostazol (OPC 13013, OPC 21) 是一种有效的 PDE3A 抑制剂，IC50 为 0.2 uM；抑制血小板聚集，在体内具有显着的抗血栓作用。

Cilostazol (OPC 13013, OPC 21) is a potent inhibitor of PDE3A with IC50 of 0.2 uM; inhibits platelet aggregation and has considerable antithrombotic effects in vivo. The compound relaxes vascular smooth muscle and inhibits mitogenesis and migration of vascular smooth muscle cells; also upregulates autophagy via SIRT1 activation, has preventive effects on various central nervous system (CNS) diseases.Stroke Approved(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.Cilostazol directly and effectively inhibits the activation of HSC but not of Kupffer cells.(In Vivo):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.Cilostazol (intraperitoneal injection; 10 mg/kg; 7 consecutive days after ischemia) attenuates neurological dysfunctions, brain atrophy and infarct volume, and inhibits astrocyte proliferation/glial scar formation and accelerated the angiogenesis in the ischemic boundary zone 7 and 28 days after ischemia.

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Animal Model:Male C57BL/6J mice Dosage:0.1% w/w, 0.3% w/w Administration:Oral administration; fed a normal diet for 2 weeks Result:Exhibited a lesser fibrotic area than control groups.Animal Model:Male ICR mice Dosage:10 mg/kg Administration:Intraperitoneal injection;7 consecutive days after ischemia Result:Had an effectve effects for the late injury.

OPC 13013 | OPC 21

Angiogenesis

PDE

PDE3

Neurological Disease

Stroke

73963-72-1

369.4607

C20H27N5O2

>98% (HPLC)

10 mM in DMSO

C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4

2(1H)-Quinolinone, 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-

(-20℃)

With Ice Pack

≥ 2 years