CILOSTAMIDE Struktur

CILOSTAMIDE

Bezeichnung:CILOSTAMIDE

CAS-Nr68550-75-4

Englisch Name:CILOSTAMIDE

CBNumberCB1444199

SummenformelC20H26N2O3

Molgewicht342.43

MOL-Datei68550-75-4.mol

CILOSTAMIDE physikalisch-chemischer Eigenschaften

Schmelzpunkt	186～188℃
Siedepunkt	594.3±50.0 °C(Predicted)
Dichte	1.18±0.1 g/cm3(Predicted)
storage temp.	0-6°C
Löslichkeit	Soluble in DMSO (up to 30 mg/ml).
Aggregatzustand	White solid
pka	11.12±0.70(Predicted)
Farbe	White
Stabilität	Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20° for up to 3 months.

Sicherheit

RIDADR	3249
WGK Germany	3
HazardClass	6.1(b)
PackingGroup	III

Gefahreninformationscode (GHS)

CILOSTAMIDE Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
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
Verwenden
Serotonin receptor ligand
Verwenden
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.
Biologische Aktivität
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.
Lager
Store at RT
Einzelnachweise
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

CILOSTAMIDE Upstream-Materialien And Downstream Produkte

CILOSTAMIDE Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

68550-75-4, CILOSTAMIDE Verwandte Suche:

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