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Chemical Structure| 73963-72-1 Chemical Structure| 73963-72-1

Structure of Cilostazol
CAS No.: 73963-72-1

Chemical Structure| 73963-72-1

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Cilostazol is a potent cyclic nucleotide phosphodiesterase type 3 (PDE3) inhibitor with IC50 of 0.2 μM and inhibitor of adenosine uptake.

Synonyms: OPC 13013; OPC 21; Cilostazolum

4.5 *For Research Use Only !

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Product Citations

Product Citations

Silva Franco, Lucas ; Rodrigues, Daniel Alencar ; Baumart, Gabriela Joras ; de Jesus, Bárbara da Silva Mascarenhas ; Gomes, Flávia Carvalho Alcantara ; Lima, Lídia Moreira , et al.

Abstract: kinases are key players in neurodegenerative diseases such as Alzheimer’s disease (AD), making them attractive therapeutic targets. In this study, we developed a pharmacophoric map of inhibitors and highlighted the key affinity sites in ROCK1/2 through molecular modeling. Virtual screening led to the identification of six approved drugs as inhibitors: (36), (37), (38), (39), (40), and (41). (36) (hROCK1 IC50 = 0.025 μM; hROCK2 IC50 = 0.007 μM) and (37) (hROCK1 IC50 = 0.019 μM; hROCK2 IC50 = 0.011 μM) showed the highest potency, while (39) displayed 15-fold selectivity for ROCK2 over ROCK1. Molecular dynamics revealed that (36) forms stable bidentate hydrogen bonds with the hinge region and has selectivity across the AGC kinase family. Biological assays confirmed ruxolitinib’s (36) safety in neuronal and glial cells and its ability to reduce C3 immunolabeling, a glial inflammation marker, in LPS-treated astrocytes. These findings not only highlight (36) as a promising candidate for AD but also provide a structural basis for designing novel dual JAK-ROCK inhibitors and pave the way for further in vitro and in vivo studies. Moreover, the validated pharmacophoric map for inhibition highlights the identification of an affinity pocket that can be useful for the design of new inhibitors.

Alternative Products

Product Details of Cilostazol

CAS No. :73963-72-1
Formula : C20H27N5O2
M.W : 369.46
SMILES Code : O=C1NC2=C(C=C(OCCCCC3=NN=NN3C4CCCCC4)C=C2)CC1
Synonyms :
OPC 13013; OPC 21; Cilostazolum
MDL No. :MFCD00866780
InChI Key :RRGUKTPIGVIEKM-UHFFFAOYSA-N
Pubchem ID :2754

Safety of Cilostazol

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H315-H319-H228
Precautionary Statements:P240-P210-P241-P264-P280-P302+P352-P370+P378-P337+P313-P305+P351+P338-P362+P364-P332+P313
Class:4.1
UN#:1325
Packing Group:

Isoform Comparison

Biological Activity

Target
  • PDE3

    PDE3, IC50:0.2 μM

In Vitro:

Cell Line
Concentration Treated Time Description References
Rat articular chondrocytes 30 μM 24 h Cilostazol pre-treatment protected articular chondrocytes from oleate-induced lipoapoptosis by upregulating PKCK2 expression and reversed the oleate-induced decrease in FSP27 protein expression level. Bone Res. 2018 Jul 6;6:20.
Rat primary vascular smooth muscle cells 10 μM 60 min To investigate the effect of Cilostazol on BAY-induced VASP phosphorylation. Results showed that Cilostazol significantly reduced BAY-mediated VASP Ser239 phosphorylation. Front Pharmacol. 2012 Feb 7;3:10.
Human peripheral blood mononuclear cell (PBMC) basophils 100 µM 30 min To study the effect of PDE3 inhibitors on basophil degranulation, results showed that Cilostazol was able to impair basophil degranulation. Front Pharmacol. 2020 May 1;11:470.
A7r5 rat vascular smooth muscle cells 100 and 200 μM 24 h To investigate the effect of cilostazol on HG-induced dysfunction in A7r5 cells, the results showed that cilostazol significantly suppressed the expressions of RAGE, FAK, MMP-2, ICAM-1, and VCAM-1, and reversed cell proliferation, adhesion, and migration. J Biomed Sci. 2019 Sep 6;26(1):68.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Tauopathy model Intraperitoneal injection 3 mg/kg Twice daily for 30 days Cilostazol enhanced proteasome function via the cAMP/PKA pathway, reduced tau accumulation, and attenuated tauopathy and cognitive decline. Transl Res. 2018 Mar;193:31-41
Mice Tg2576 transgenic mice Oral 0.01% Daily, for 7-9 months To investigate whether lower-dose cilostazol can decrease micro-hemorrhages and Aβ deposition in the brain of Tg2576 mice. Results showed that the CAA score was significantly lower in the cilostazol group compared to the control group at 21-23 months, indicating that lower-dose cilostazol can reduce the vascular amyloid burden. Int J Mol Sci. 2020 Mar 26;21(7):2295
CD-1 mice Stable closed femoral fracture model Oral gavage 30 mg/kg Daily administration for 2 or 5 weeks Cilostazol accelerates fracture healing and induces bone formation in aged mice by stimulating angiogenesis and increasing the expression of PI3K and RUNX2. Int J Mol Sci. 2024 Jan 6;25(2):755
Mice High-fat diet-induced osteoarthritis model Oral 30 mg·kg-1 Once daily for 10 weeks Cilostazol significantly reduced high-fat diet-induced cartilage degeneration and increased the population of PKCK2-, STAMP2-, and FSP27-positive chondrocytes. Bone Res. 2018 Jul 6;6:20.
Mice ApoE null mice Dietary supplementation 0.1% 16 weeks Co-treatment of cilostazol with GbE significantly reduced atherosclerotic lesion area in ApoE null mice and decreased the expression of inflammatory cytokines and adhesion molecules. Exp Mol Med. 2012 May 31;44(5):311-8

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT04753970 Cerebral Small Vessel Diseases... More >>|Cerebral Autosomal Dominant Arteriopathy With Subcortical Infarcts and Leukoencephalopathy|Cerebral Microbleeding|Sporadic White Matter Disease Less << PHASE1|PHASE2 RECRUITING 2025-06-26 Mayo Clinic Florida, Jacksonvi... More >>lle, Florida, 32224, United States Less <<
NCT00602173 Intermittent Claudication COMPLETED 2025-05-03 CEDRA Clinical Research, LLC, ... More >>Austin, Texas, 78759, United States Less <<
NCT00048776 Raynaud's Disease PHASE4 COMPLETED 2025-06-03 Advanced Medical Clinical Ther... More >>apeutics, Anchorage, Alaska, 99508, United States|Advanced Medical Research Institute, Fresno, California, 93710, United States|Madera Family Medical Group, Madera, California, 93637, United States|Connecticut Children's Medical Center, Hartford, Connecticut, 06106, United States|LaRabida Children's Hospital, Chicago, Illinois, 60649, United States|Children's Hospital Boston, Boston, Massachusetts, 02115, United States|St. Louis University Health Sciences Center, St. Louis, Missouri, 63104, United States|Children's Hospital, Omaha, Nebraska, 68114, United States|Asthma & Allergy Research Center, Newark, New Jersey, 07103, United States|SUNY Downstate Medical Center, Brooklyn, New York, 11203, United States|Children's Hospital of Buffalo, Buffalo, New York, 14222, United States|Schneider Children's Hospital, New Hyde Park, New York, 11040, United States|New York Medical College, Valhalla, New York, 10595, United States|Jobst Vascular Center, Toledo, Ohio, 43606, United States|Altoona Center for Clinical Research, Duncansville, Pennsylvania, 16635, United States|The Milton S. Hershey Medical Center, Hershey, Pennsylvania, 17033, United States|Medical University of South Carolina, Charleston, South Carolina, 29425, United States|Monarch Research Associates, Norfolk, Virginia, 23510, United States|Children's Hospital and Regional Medical Center, Seattle, Washington, 98105, United States Less <<
NCT00048763 Raynaud's Disease PHASE4 COMPLETED 2025-06-03 Advanced Medical Clinical Ther... More >>apeutics, Anchorage, Alaska, 99508, United States|Advanced Medical Research Institute, Fresno, California, 93710, United States|Madera Family Medical Group, Madera, California, 93637, United States|Connecticut Children's Medical Center, Hartford, Connecticut, 06106, United States|LaRabida Children's Hospital, Chicago, Illinois, 60649, United States|Children's Hospital Boston, Boston, Massachusetts, 02115, United States|St. Louis University Health Sciences Center, St. Louis, Missouri, 63104, United States|Children's Hospital, Omaha, Nebraska, 68114, United States|Asthma & Allergy Research Center, Newark, New Jersey, 07103, United States|SUNY Downstate Medical Center, Brooklyn, New York, 11203, United States|Children's Hospital of Buffalo, Buffalo, New York, 14222, United States|Schneider Children's Hospital, New Hyde Park, New York, 11040, United States|New York Medical College, Valhalla, New York, 10595, United States|Jobst Vascular Center, Toledo, Ohio, 43606, United States|The Milton S. Hershey Medical Center, Hershey, Pennsylvania, 17033, United States|Medical University of South Carolina, Charleston, South Carolina, 29425, United States|Monarch Research Associates, Norfolk, Virginia, 23510, United States|Children's Hospital and Regional Medical Center, Seattle, Washington, 98105, United States Less <<
NCT00431249 Hemodialysis Patients|Peripher... More >>al Vascular Disease Less << PHASE4 COMPLETED 2025-04-08 -
NCT01915069 Contraception PHASE2 COMPLETED 2025-08-14 University of Southern Califor... More >>nia Fertility Clinic, Los Angeles, California, 90017, United States Less <<
NCT00602407 Intermittent Claudication COMPLETED 2025-03-04 CEDRA Clinical Research, LLC, ... More >>Austin, Texas, 78759, United States Less <<
NCT00404716 Acute Coronary Syndrome PHASE4 COMPLETED 2025-02-07 -
NCT00773630 Intermittent Claudication PHASE1 COMPLETED 2025-03-09 AAIPharma Deutschland GmbH & C... More >>o. KG, Neu-Ulm, 89231, Germany Less <<
NCT01455558 Healthy PHASE1 COMPLETED 2025-09-09 Severance Hospital, Seoul, 120... More >>-752, Korea, Republic of Less <<
NCT02094469 Vasospastic Angina PHASE3 COMPLETED 2025-01-16 Yangsan Busan University Hospi... More >>tal, Busan, 626-770, Korea, Republic of Less <<
NCT02374957 Peripheral Arterial Disease|Cl... More >>audication (Finding) Less << PHASE4 TERMINATED 2017-06-30 Wake Forest Baptist Health, Wi... More >>nston-Salem, North Carolina, 27106, United States Less <<
NCT01076478 Polyneuropathy PHASE4 COMPLETED 2025-11-09 University of Santo Tomas Hosp... More >>ital, Manila, Philippines Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.71mL

0.54mL

0.27mL

13.53mL

2.71mL

1.35mL

27.07mL

5.41mL

2.71mL

References

 

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