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68550-75-4

68550-75-4 structure
68550-75-4 structure
  • Name: Cilostamide
  • Chemical Name: Cilostamide
  • CAS Number: 68550-75-4
  • Molecular Formula: C20H26N2O3
  • Molecular Weight: 342.432
  • Catalog: Signaling Pathways Metabolic Enzyme/Protease Phosphodiesterase (PDE)
  • Create Date: 2018-09-16 08:48:26
  • Modify Date: 2024-01-01 20:05:53
  • Cilostamide is a selective and potent PDE3 inhibitor, with IC50s of 27 nM and 50 nM for PDE3A and PDE3B, respectively, and has antithrombotic and anti-intimal hyperplastic activity.
Name Cilostamide
Synonyms Butanamide, N-cyclohexyl-4-[(1,2-dihydro-2-oxo-6-quinolinyl)oxy]-N-methyl-
N-Cyclohexyl-N-methyl-4-[(2-oxo-1,2-dihydro-6-quinolinyl)oxy]butanamide
MFCD00673958
N-Cyclohexyl-N-methyl-4-[(2-oxo-1,2-dihydroquinolin-6-yl)oxy]butanamide
N-cyclohexyl-N-methyl-4-[(2-oxo-1H-quinolin-6-yl)oxy]butanamide
N-cyclohexyl-4-[(2-hydroxyquinolin-6-yl)oxy]-N-methylbutanamide
Description Cilostamide is a selective and potent PDE3 inhibitor, with IC50s of 27 nM and 50 nM for PDE3A and PDE3B, respectively, and has antithrombotic and anti-intimal hyperplastic activity.
Related Catalog
Target

IC50: 27 nM (PDE3A), 50 nM (PDE3B)[1]

In Vitro Cilostamide is a selective and potent PDE3 inhibitor, with IC50s of 27 nM and 50 nM for PDE3A and PDE3B, respectively, and has antithrombotic and anti-intimal hyperplastic activity. Cilostamide weakly inhibits PDE2, PDE4, PDE5, PDE7, and PDE1, with IC50s of 12.5, 88.8, 15.2, 22.0 and > 300 μM, respectively. Cilostamide potently inhibits thrombin-induced platelet aggregation (IC50, 1.1 μM)[1].
Animal Admin Platelet aggregation is investigated in the assay. Washed platelets (200 μL of a suspension containing 3 × 108 cells/mL in Tyrode HEPES buffer, pH 7.4) are incubated for 3 min at 37°C in the presence or absence of different concentrations of OPC-33540, OPC-33536, and Cilostamide alone, or in combination with 3 nM PGE1, followed by incubation with 5 μL of 2 units/mL of thrombin for 5 min at 37°C. The intensity of light transmitted over 5 min is measured using a PAM-8C aggregometer. The inhibition rate is calculated by comparison of maximum aggregation rates with the control value[1].
References

[1]. Sudo T, et al. Potent effects of novel anti-platelet aggregatory cilostamide analogues on recombinant cyclic nucleotide phosphodiesterase isozyme activity. Biochem Pharmacol. 2000 Feb 15;59(4):347-56.
Density 1.2±0.1 g/cm3
Boiling Point 594.3±50.0 °C at 760 mmHg
Molecular Formula C20H26N2O3
Molecular Weight 342.432
Flash Point 313.2±30.1 °C
Exact Mass 342.194336
PSA 62.40000
LogP 2.70
Vapour Pressure 0.0±1.7 mmHg at 25°C
Index of Refraction 1.586
Storage condition -20℃
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR UN 3249
Packaging Group III
Hazard Class 6.1(b)
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