| Identification | Back Directory | [Name]
CILOSTAMIDE | [CAS]
68550-75-4 | [Synonyms]
OPC 3689
OCP 3689
CILOSTAMIDE
ciloalaMide
Cilostamide,OPC 3689
Cilostamide - CAS 68550-75-4 - Calbiochem
6-[3-(N-Cyclohexyl-N-methylcarbamoyl)propoxy]quinolin-2[1H]-one
N-cyclohexyl-4-[(2-hydroxyquinolin-6-yl)oxy]-N-methylbutanamide
N-CYCLOHEXYL-N-METHYL-4-(1,2-DIHYDRO-2-OXO-6-QUINOLYLOXY)BUTYRAMIDE
N-Cyclohexyl-4-[(1,2-dihydro-2-oxoquinolin-6-yl)oxy]-N-methylbutanamide
N-Cyclohexyl-4-[(1,2-dihydro-2-oxoquinolin-6-yl)oxy]-N-methylbutyramide
Butanamide, N-cyclohexyl-4-[(1,2-dihydro-2-oxo-6-quinolinyl)oxy]-N-methyl- | [Molecular Formula]
C20H26N2O3 | [MDL Number]
MFCD00673958 | [MOL File]
68550-75-4.mol | [Molecular Weight]
342.43 |
| Chemical Properties | Back Directory | [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. |
| Hazard Information | Back Directory | [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 | [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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