CILOSTAMIDE Chemical Properties

Melting point:

186～188℃

Boiling point:

594.3±50.0 °C(Predicted)

Density 

1.18±0.1 g/cm3(Predicted)

storage temp. 

0-6°C

solubility 

Soluble in DMSO (up to 30 mg/ml).

form 

White solid

pka

11.12±0.70(Predicted)

color 

White

Stability:

Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Safety Information

RIDADR 

3249

WGK Germany 

3

HazardClass 

6.1(b)

PackingGroup 

III

CILOSTAMIDE Usage And Synthesis

Description

Cilostamide (68550-75-4) is a selective inhibitor of phosphodiesterase-3 (PDE3). Displays limited selectivity for PDE3A versus PDE3B (IC50 = 27 and 50 nM).1,2 Blocks PKB/Akt signaling pathway downstream via inhibition of Akt-activated PDE3B.3 Cilostamide reverses the effect of leptin on food intake and body weight.4

Uses

Serotonin receptor ligand

Uses

Cilostamide (OPC 3689) is a specific phosphodiesterase 3 (PDE3) inhibitor.

Definition

ChEBI: N-cyclohexyl-N-methyl-4-[(2-oxo-1H-quinolin-6-yl)oxy]butanamide is a member of quinolines.

Biological Activity

Selective inhibitor of type III phosphodiesterase (PDE3). Displays moderate selectivity for PDE3A isozyme vs. PDE3B (IC 50 values are 0.027 and 0.050 μ M for PDE3A and PDE3B respectively). Inhibits ADP-induced platelet aggregation (IC 50 = 16.8 μ M); anti-thrombotic. Also available as part of the Phosphodiesterase Inhibitor Tocriset™ .

Biochem/physiol Actions

Selective inhibitor of PDE3 (cGMP-inhibited phosphodiesterase); IC50 = 70 ± 9 nM. This inhibitory effect increases intracellular cAMP and inhibits platelet aggregation.

storage

Store at RT

References

1) Hidaka et al. (1979), Selective inhibitor of platelet cyclic adenosine monophosphate phosphodiesterase, cilostamide, inhibits platelet aggregation; J. Pharmacol. Exp. Ther., 211 26 2) Christensen and Torphy et al. (1994), Isozyme-Selective Phosphodiesterase Inhibitors as Antiasthmatic Agents; Annu. Rep. Med. Chem., 29 185 3) Ahmad et al. (2000), Cyclic nucleotide phosphodiesterase 3B is a downstream target of protein kinase B and may be involved in regulation of effects of protein kinase B on thymidine incorporation in FDCP2 cells; J. Immunol., 164 4678 4) Zhao et al. (2002), A phosphatidylinositol 3-kinase phosphodiesterase 3B-cyclic AMP pathway in hypothalamic action of leptin on feeding; Nat. Neuroscience, 5 727

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