CILOSTAMIDE

CILOSTAMIDE Property

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

RIDADR 

3249

WGK Germany 

3

HazardClass 

6.1(b)

PackingGroup 

III

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

CILOSTAMIDE Chemical Properties,Usage,Production

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