Cat. No.: HY-17464

Cilostazol

(Synonyms: OPC 13013)

6 Cited Publications

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Based on 6 publication(s) in Google Scholar

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.

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Pureté: 99.77%
CAS No.: 73963-72-1
Formule: C₂₀H₂₇N₅O₂
Masse moléculaire:369.46

Stockage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Cilostazol Chemical Structure

CAS No.: 73963-72-1

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (6)
Solvant et solubilité
- In Vitro
- In Vivo
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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 & Target

IC50: 0.2 μM ( PDE 3A)^[1]

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE) :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	91.2 μM Compound: cilostazol	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
Platelet	IC₅₀	109 μM Compound: Cilostazol	Antiplatelet activity against collagen A23187-induced platelet aggregation in human plasma preincubated for 2 mins before addition of inducer by turbidimetric method Antiplatelet activity against collagen A23187-induced platelet aggregation in human plasma preincubated for 2 mins before addition of inducer by turbidimetric method	[PMID: 23425969]
Platelet	IC₅₀	40 μM Compound: Cilostazol	Antiplatelet activity against collagen collagen-induced platelet aggregation in human plasma preincubated for 2 mins before addition of inducer by turbidimetric method Antiplatelet activity against collagen collagen-induced platelet aggregation in human plasma preincubated for 2 mins before addition of inducer by turbidimetric method	[PMID: 23425969]
Platelet	IC₅₀	73 μM Compound: Cilostazol	Antiplatelet activity against collagen ADP-induced platelet aggregation in human plasma preincubated for 2 mins before addition of inducer by turbidimetric method Antiplatelet activity against collagen ADP-induced platelet aggregation in human plasma preincubated for 2 mins before addition of inducer by turbidimetric method	[PMID: 23425969]
Sf9	IC₅₀	0.84 μM Compound: Cilostazol	Inhibition of human recombinant PDE3 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method Inhibition of human recombinant PDE3 catalytic domain expressed in baculovirus-infected insect Sf9 cells by modified two-step method	[PMID: 19303290]

In Vitro

Cilostazol selectively inhibits cGMP-inhibited phosphodiesterase (PDE 3) and is a potent inhibitor of platelet aggregation induced by various agonists^[2].
? 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[3].
? 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^[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male C57BL/6J mice^[3]
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^[4]
Dosage:

10 mg/kg
Administration:

Intraperitoneal injection; 7 consecutive days after ischemia
Result:

Had an effectve effects for the late injury.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 73963-72-1
Appearance Solid
Masse moléculaire 369.46
Formule C₂₀H₂₇N₅O₂
Color White to off-white
SMILES

O=C1NC2=C(C=C(OCCCCC3=NN=NN3C4CCCCC4)C=C2)CC1
Synonyms

OPC 13013
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (6)

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Cell Death Differ

HERP constrains white adipose expansion and inflammation by STEAP4 stabilization. [Abstract]

2025 Nov 17. PMID: 41249464
Adv Sci (Weinh)

Dipyridamole Acts as Clinical Ferroptosis Inhibitor to Prevent from Tissue Injury. [Abstract]

2025 May 14:e2500566. PMID: 40365742
Cephalalgia

CGRP-dependent signalling pathways involved in mouse models of GTN- cilostazol- and levcromakalim-induced migraine. [Abstract]

2021 Dec;41(14):1413-1426. PMID: 34407650
Chem Biodivers

Secondary Metabolites from the Endophytic Fungus Letendraea helminthicola A820 with Anti-inflammatory Activity. [Abstract]

2025 Feb;22(2):e202402114. PMID: 39340168
Cardiovasc Eng Technol

Cilostazol Promotes Angiogenesis and Increases Cell Proliferation After Myocardial Ischemia-Reperfusion Injury Through a cAMP-Dependent Mechanism. [Abstract]

2019 Dec;10(4):638-647. PMID: 31625080

Cilostazol purchased from MedChemExpress. Usage Cited in: Cardiovasc Eng Technol. 2019 Dec;10(4):638-647. [Abstract]

Cilostazol increases cell proliferation in H/I cell models. The protein expression levels of p-AKT and p-eNOS and proliferation in HUVEC H/I cell model.

Cilostazol purchased from MedChemExpress. Usage Cited in: Cardiovasc Eng Technol. 2019 Dec;10(4):638-647. [Abstract]

Cilostazol increases cell proliferation in H/I cell models. The protein expression levels of p-AKT and p-eNOS and proliferation in VSMCH/I cell model. The protein expression is detected by western blotting, and cell proliferation was analyzed by DAPI/Brdu staining.

Cilostazol purchased from MedChemExpress. Usage Cited in: Cardiovasc Eng Technol. 2019 Dec;10(4):638-647. [Abstract]

Cilostazol increases cell proliferation in H/I cell models. The protein expression levels of p-AKT and p-eNOS and proliferation in VSMCH/I cell model.

Cilostazol purchased from MedChemExpress. Usage Cited in: Cardiovasc Eng Technol. 2019 Dec;10(4):638-647. [Abstract]

Cilostazol increases cell proliferation in H/I cell models. The protein expression levels of p-AKT and p-eNOS and proliferation in VSMCH/I cell model. The protein expression is detected by western blotting, and cell proliferation was analyzed by DAPI/Brdu staining.
Patent

US20230111925A1.

Solvant et solubilité

In Vitro:

DMSO : 50 mg/mL (135.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2 mg/mL (5.41 mM); Suspended solution; Need ultrasonic

This protocol yields a suspended solution of 2 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (277 KB)
SDS (419 KB)
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- Español - ES (419 KB)
- Swedish - SV (419 KB)
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- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Schr?r K. The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.7067 mL	13.5333 mL	27.0665 mL	67.6663 mL
	5 mM	0.5413 mL	2.7067 mL	5.4133 mL	13.5333 mL
	10 mM	0.2707 mL	1.3533 mL	2.7067 mL	6.7666 mL
	15 mM	0.1804 mL	0.9022 mL	1.8044 mL	4.5111 mL
	20 mM	0.1353 mL	0.6767 mL	1.3533 mL	3.3833 mL
	25 mM	0.1083 mL	0.5413 mL	1.0827 mL	2.7067 mL
	30 mM	0.0902 mL	0.4511 mL	0.9022 mL	2.2555 mL
	40 mM	0.0677 mL	0.3383 mL	0.6767 mL	1.6917 mL
	50 mM	0.0541 mL	0.2707 mL	0.5413 mL	1.3533 mL
	60 mM	0.0451 mL	0.2256 mL	0.4511 mL	1.1278 mL
	80 mM	0.0338 mL	0.1692 mL	0.3383 mL	0.8458 mL
	100 mM	0.0271 mL	0.1353 mL	0.2707 mL	0.6767 mL

Keywords

Cilostazol

6 Cited Publications

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Cilostazol

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Publications Citing Use of MedChemExpress (MCE) Cilostazol

Voir tous les produits spécifiques à Isoform Phosphodiesterase (PDE)

Activité biologique

Chemical Information

Publications (6)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Cilostazol Related Classifications

HY-17464 Related Classifications