Cilostamide
Chemical Name: N-Cyclohexyl-N-methyl-4-(1,2-dihydro-2-oxo-6-quinolyloxy)butyramide
Purity: ≥97%
Biological Activity
Cilostamide is a selective inhibitor of type III phosphodiesterase (PDE3). Displays moderate selectivity for PDE3A isozyme vs. PDE3B (IC50 values are 0.027 and 0.050 μM for PDE3A and PDE3B respectively). Inhibits ADP-induced platelet aggregation (IC50 = 16.8 μM); antithrombotic.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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High-throughput genotoxicity assay identifies antioxidants as inducers of DNA damage response and cell death.
Fox JT, Sakamuru S, Huang R
Proc. Natl. Acad. Sci. U.S.A., 2012;109(14):5423-8. -
beta-Adrenergic cAMP signals are predominantly regulated by phosphodiesterase type 4 in cultured adult rat aortic smooth muscle cells.
Zhai K, Hubert F, Nicolas V, Ji G, Fischmeister R, Leblais V
PLoS ONE, 2012;7(10):e47826. -
Olanzapine: preclinical and clinical profiles of a novel antipsychotic agent.
Tollefson and Taylor
CNS Drug Reviews, 2000;6:303 -
Selective inhibitor of platelet cyclic adenosine monophosphate phosphodiesterase, cilostamide, inhibits platelet aggregation.
Hidaki et al.
J.Pharmacol.Exp.Ther., 1979;211:26 -
Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity.
Sudo et al.
Biochem.Pharmacol., 2000;59:347 -
Isozyme-selective phosphodiesterase inhibitors as antiasthmatic agents.
Christensen and Torphy
Annu.Rep.Med.Chem., 1994;29:185
Product Datasheets
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Citations for Cilostamide
The citations listed below are publications that use Tocris products. Selected citations for Cilostamide include:
5 Citations: Showing 1 - 5
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Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with isoprote.
Authors: Merino Et al.
PLoS One 2015;10:e0132884
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The inotropic effect of the active metabolite of levosimendan, OR-1896, is mediated through inhibition of PDE3 in rat ventricular myocardium.
Authors: Ørstavik Et al.
J Biol Chem 2015;10:e0115547
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Alteration of vascular reactivity in heart failure: role of phosphodiesterases 3 and 4.
Authors: Hubert Et al.
Br J Pharmacol 2014;171:5361
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Increased intracellular magnesium attenuates β-adrenergic stimulation of the cardiac Ca(V)1.2 channel.
Authors: Brunet Et al.
J Gen Physiol 2013;141:85
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β-Adrenergic cAMP signals are predominantly regulated by phosphodiesterase type 4 in cultured adult rat aortic smooth muscle cells.
Authors: Zhai Et al.
PLoS One 2012;7:e47826
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