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] H HIDAKA. Selective inhibitor of platelet cyclic adenosine monophosphate phosphodiesterase, cilostamide, inhibits platelet aggregation.[J]. Journal of Pharmacology and Experimental Therapeutics, 1979, 211 1: 26-30.
[2] S. CHRISTENSEN T T. Chapter 19. Isozyme-Selective Phosphodiesterase Inhibitors as Antiasthmatic Agents[J]. Annual Reports in Medicinal Chemistry, 1994, 29 1: 185-194. DOI:10.1016/s0065-7743(08)60732-0
[3] F AHMAD. 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]. Journal of immunology, 2000, 164 9: 4678-4688. DOI:10.4049/jimmunol.164.9.4678
[4] ALLAN Z. ZHAO. A phosphatidylinositol 3-kinase–phosphodiesterase 3B–cyclic AMP pathway in hypothalamic action of leptin on feeding[J]. Nature neuroscience, 2002, 5 8: 727-728. DOI:10.1038/nn885

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