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Submit ReviewCilostamide
Description: PDE3 inhibitor
Alternative Names: OCP 3689
Chemical Name: N-Cyclohexyl-N-methyl-4-(1,2-dihydro-2-oxo-6-quinolyloxy)butyramide
Purity: ≥97% (HPLC)
Biological Activity for Cilostamide
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 for Cilostamide
| M. Wt | 342.44 |
| Formula | C20H26N2O3 |
| Storage | Store at RT |
| Purity | ≥97% (HPLC) |
| CAS Number | 68550-75-4 |
| PubChem ID | 2753 |
| InChI Key | UIAYVIIHMORPSJ-UHFFFAOYSA-N |
| Smiles | CN(C1CCCCC1)C(=O)CCCOC1=CC=C2NC(=O)C=CC2=C1 |
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.
Solubility Data for Cilostamide
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 6.85 | 20 with gentle warming |
Preparing Stock Solutions for Cilostamide
The following data is based on the product molecular weight 342.44. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.2 mM | 14.6 mL | 73.01 mL | 146.01 mL |
| 1 mM | 2.92 mL | 14.6 mL | 29.2 mL |
| 2 mM | 1.46 mL | 7.3 mL | 14.6 mL |
| 10 mM | 0.29 mL | 1.46 mL | 2.92 mL |
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Product Datasheets for Cilostamide
References for Cilostamide
References are publications that support the biological activity of the product.
Hidaki et al (1979) Selective inhibitor of platelet cyclic adenosine monophosphate phosphodiesterase, cilostamide, inhibits platelet aggregation. J.Pharmacol.Exp.Ther. 211 26 PMID: 226672
Sudo et al (2000) Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity. Biochem.Pharmacol. 59 347 PMID: 10644042
Christensen and Torphy (1994) Isozyme-selective phosphodiesterase inhibitors as antiasthmatic agents. Annu.Rep.Med.Chem. 29 185
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Keywords: Cilostamide, Cilostamide supplier, PDE3, inhibitors, inhibits, Phosphodiesterases, OCP3689, OCP, 3689, 0915, Tocris Bioscience
5 Citations for Cilostamide
Citations are publications that use Tocris products. Selected citations for Cilostamide include:
Brunet et al (2013) Increased intracellular magnesium attenuates β-adrenergic stimulation of the cardiac Ca(V)1.2 channel. J Gen Physiol 141 85 PMID: 23250865
Merino et al (2015) Glucagon Increases Beating Rate but Not Contractility in Rat Right Atrium. Comparison with isoprote. PLoS One 10 e0132884 PMID: 26222156
Ørstavik et al (2015) The inotropic effect of the active metabolite of levosimendan, OR-1896, is mediated through inhibition of PDE3 in rat ventricular myocardium. J Biol Chem 10 e0115547 PMID: 25738589
Hubert et al (2014) Alteration of vascular reactivity in heart failure: role of phosphodiesterases 3 and 4. Br J Pharmacol 171 5361 PMID: 25048877
Zhai et al (2012) β-Adrenergic cAMP signals are predominantly regulated by phosphodiesterase type 4 in cultured adult rat aortic smooth muscle cells. PLoS One 7 e47826 PMID: 23094097
Do you know of a great paper that uses Cilostamide from Tocris? Please let us know.
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