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Cilostamide (Synonyms: OPC 3689)

Catalog No.GC10109

type III phosphodiesterase (PDE3) inhibitor

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Cilostamide Chemical Structure

Cas No.: 68550-75-4

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10mM (in 1mL DMSO)
$69.00
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1mg
$39.00
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5mg
$63.00
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10mg
$101.00
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25mg
$202.00
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50mg
$302.00
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100mg
$454.00
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Sample solution is provided at 25 µL, 10mM.

Description of Cilostamide

Cilostamide is a selective and potent PDE3 inhibitor, with IC50s of 27 nM and 50 nM for PDE3A and PDE3B, respectively, and has antithrombotic and anti-intimal hyperplastic activity.

Cilostamide is a selective and potent PDE3 inhibitor, with IC50s of 27 nM and 50 nM for PDE3A and PDE3B, respectively, and has antithrombotic and anti-intimal hyperplastic activity. Cilostamide weakly inhibits PDE2, PDE4, PDE5, PDE7, and PDE1, with IC50s of 12.5, 88.8, 15.2, 22.0 and > 300 μM, respectively. Cilostamide potently inhibits thrombin-induced platelet aggregation (IC50, 1.1 μM)[1].

References:
[1]. Sudo T, et al. Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity. Biochem Pharmacol. 2000 Feb 15;59(4):347-56.

Protocol of Cilostamide

Animal experiment:

Platelet aggregation is investigated in the assay. Washed platelets (200 μL of a suspension containing 3 × 108 cells/mL in Tyrode HEPES buffer, pH 7.4) are incubated for 3 min at 37°C in the presence or absence of different concentrations of OPC-33540, OPC-33536, and Cilostamide alone, or in combination with 3 nM PGE1, followed by incubation with 5 μL of 2 units/mL of thrombin for 5 min at 37°C. The intensity of light transmitted over 5 min is measured using a PAM-8C aggregometer. The inhibition rate is calculated by comparison of maximum aggregation rates with the control value[1].

References:

[1]. Sudo T, et al. Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity. Biochem Pharmacol. 2000 Feb 15;59(4):347-56.

Chemical Properties of Cilostamide

Cas No. 68550-75-4 SDF
Synonyms OPC 3689
Chemical Name N-cyclohexyl-N-methyl-4-((2-oxo-1,2-dihydroquinolin-6-yl)oxy)butanamide
Canonical SMILES O=C(CCCOC1=CC=C(C(C=C2)=C1)NC2=O)N(C)C3CCCCC3
Formula C20H26N2O3 M.Wt 342.44
Solubility DMF: 0.25 mg/ml Storage Store at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of Cilostamide

Prepare stock solution
1 mg 5 mg 10 mg
1 mM 2.9202 mL 14.6011 mL 29.2022 mL
5 mM 0.584 mL 2.9202 mL 5.8404 mL
10 mM 0.292 mL 1.4601 mL 2.9202 mL
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In vivo Formulation Calculator (Clear solution) of Cilostamide

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 28 reference(s) in Google Scholar.)

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