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Purity: ≥98%
Cilostazol (formerly OPC-13013; Pletal; Cilostazolum; Pletaal; OPC13013; OPC 13013), a potent vasodilator that acts by relaxing the muscles, is a selective cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with beneficial effects on learning impairment. It inhibits PDE3 with an IC50 of 0.2 μM and inhibitor of adenosine uptake.
| ln Vitro |
Cilostazol is a strong inhibitor of platelet aggregation brought on by different agonists and specifically inhibits cGMP-inhibited phosphodiesterase (PDE 3) [2]. With an IC50 of 15 μM for stress-induced human platelet aggregation and 12.5 μM for ADP-induced platelet aggregation, clostazol inhibits both types of human platelet aggregation in a dose-dependent manner [2]. Cilostazol inhibits HSC activation directly and effectively, but not Kupffer cell activation [3].
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| ln Vivo |
In vivo liver fibrosis caused by CCl4 is lessened by clostazol (clinical dosage; oral administration for 2 weeks); this effect may be attributed to direct inhibition of HSC activation [3]. Intraperitoneal injection of cilostazol (10 mg/kg given over 7 days) reduces neurological deficits, brain atrophy, and infarct size. It also prevents astrocyte proliferation and glial scarring during ischemia. After 7 and 28 days, angiogenesis in the ischemic border zone accelerates [4].
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| Animal Protocol |
Animal/Disease Models: Male C57BL/6J mice[3]
Doses: 0.1% w/w, 0.3% w/w Route of Administration: Oral administration; fed a normal diet for 2 weeks Experimental Results: demonstrated a lesser fibrotic area than control groups. Animal/Disease Models: Male ICR mice[4] Doses: 10 mg/kg Route of Administration: intraperitoneal (ip)injection; 7 days after ischemia Experimental Results: Had an effectve effects for the late injury. |
| References |
[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. [4]. Ye YL,et al. Cilostazol, a phosphodiesterase 3 inhibitor, protects mice against acute and late ischemic brain injuries.Eur J Pharmacol. 2007 Feb 14;557(1):23-31. Epub 2006 Nov 10. |
| Molecular Formula |
C20H27N5O2
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| Molecular Weight |
369.46
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| CAS # |
73963-72-1
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| Related CAS # |
Cilostazol-d11;1073608-02-2;Cilostazol-d4;1215541-47-1
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| SMILES |
O=C1NC2=C(C=C(OCCCCC3=NN=NN3C4CCCCC4)C=C2)CC1
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| InChi Key |
RRGUKTPIGVIEKM-UHFFFAOYSA-N
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| InChi Code |
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)
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| Chemical Name |
6-[4-(1-cyclohexyltetrazol-5-yl)butoxy]-3,4-dihydro-1H-quinolin-2-one
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (5.41 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7067 mL | 13.5333 mL | 27.0665 mL | |
| 5 mM | 0.5413 mL | 2.7067 mL | 5.4133 mL | |
| 10 mM | 0.2707 mL | 1.3533 mL | 2.7067 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT01915069 | Completed | Drug: Cilostazol | Contraception | University of Southern California | July 2013 | Phase 2 |
| NCT05671497 | Recruiting | Drug: Cilostazol 100 MG | Rheumatoid Arthritis | Ain Shams University | November 1, 2022 | Phase 2 Phase 3 |
| NCT02374957 | Terminated Has Results | Drug: Cilostazol | Peripheral Arterial Disease Claudication (Finding) |
Wake Forest University Health Sciences | February 2015 | Phase 4 |
| NCT05126836 | Completed Has Results | Drug: Cilostazol 100Mg Tab Drug: Placebo |
Heart Failure With Preserved Ejection Fraction |
University of Minnesota | September 1, 2021 | Phase 2 |
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