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| | CILOSTAMIDE Basic information |
| Product Name: | CILOSTAMIDE | | Synonyms: | OPC 3689;OCP 3689;N-CYCLOHEXYL-N-METHYL-4-(1,2-DIHYDRO-2-OXO-6-QUINOLYLOXY)BUTYRAMIDE;CILOSTAMIDE;Cilostamide,OPC 3689;ciloalaMide;6-[3-(N-Cyclohexyl-N-methylcarbamoyl)propoxy]quinolin-2[1H]-one;N-Cyclohexyl-4-[(1,2-dihydro-2-oxoquinolin-6-yl)oxy]-N-methylbutanamide | | CAS: | 68550-75-4 | | MF: | C20H26N2O3 | | MW: | 342.43 | | EINECS: | | | Product Categories: | Cyclic Nucleotide related | | Mol File: | 68550-75-4.mol |  |
| | 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. |
| 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 |
| | CILOSTAMIDE Preparation Products And Raw materials |
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