Cilostazol (Synonyms: OPC 13013)

Name: Cilostazol
Brand: MedChemExpress
SKU: HY-17464
Rating: 5.0 (8 reviews)

Cat. No.: HY-17464 Purity: 99.87%: FAQs
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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.

For research use only. We do not sell to patients.

Cilostazol Chemical Structure

CAS No. : 73963-72-1

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 73	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 73	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	USD 66	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 8 publication(s) in Google Scholar

Other Forms of Cilostazol:

4 Publications Citing Use of MCE Cilostazol

: 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.

: 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. The protein expression is detected by western blotting, and cell proliferation was analyzed by DAPI/Brdu staining.

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Biological Activity
Purity & Documentation
References
Customer Review

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]

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.

Clinical Trial

Molecular Weight

369.46

Formula

C₂₀H₂₇N₅O₂

CAS No.

73963-72-1

Appearance

Solid

Color

White to off-white

SMILES

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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)

Preparing
Stock Solutions

Concentration Solvent Mass	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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.87%

Select Batch:

Data Sheet (277 KB) SDS (419 KB)

COA (247 KB) HNMR (185 KB) LCMS (113 KB)

Handling Instructions (2659 KB)

References

[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]

Complete Stock Solution Preparation Table

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

Cilostazol Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Cilostazol73963-72-1OPC 13013OPC13013OPC-13013Phosphodiesterase (PDE)AutophagylateinjurycardiovascularhepaticfibrogenesisInhibitorinhibitorinhibit

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Cilostazol (Synonyms: OPC 13013)

Customer Review

Other Forms of Cilostazol:

Cilostazol Related Antibodies

4 Publications Citing Use of MCE Cilostazol

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Phosphodiesterase (PDE) Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Cilostazol Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Cilostazol Related Classifications

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Customer Review

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