Cilostazol

SKU: orb1224101

Description

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.

Key Properties

• CAS Number: 73963-72-1
• MW: 369.4607
• Purity: >98% (HPLC)
• Formula: C₂₀H₂₇N₅O₂
• SMILES: C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4
• Target: PDE
• Solubility: 10 mM in DMSO

Bioactivity

• In Vivo:
  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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

OPC 13013 | OPC 21

Quick Database Links

Gene Symbol

PDE