CAS 68550-75-4|Cilostamide

Introduction:Basic information about CAS 68550-75-4|Cilostamide, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common NameCilostamide
CAS Number68550-75-4Molecular Weight342.432
Density1.2±0.1 g/cm3Boiling Point594.3±50.0 °C at 760 mmHg
Molecular FormulaC20H26N2O3Melting Point/
MSDSChineseUSAFlash Point313.2±30.1 °C

Names

NameCilostamide
SynonymMore Synonyms

Cilostamide BiologicalActivity

DescriptionCilostamide 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 CatalogSignaling Pathways >>Metabolic Enzyme/Protease >>Phosphodiesterase (PDE)Research Areas >>Cardiovascular Disease
Target

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

In VitroCilostamide 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 AdminPlatelet 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.

Chemical & Physical Properties

Density1.2±0.1 g/cm3
Boiling Point594.3±50.0 °C at 760 mmHg
Molecular FormulaC20H26N2O3
Molecular Weight342.432
Flash Point313.2±30.1 °C
Exact Mass342.194336
PSA62.40000
LogP2.70
Vapour Pressure0.0±1.7 mmHg at 25°C
Index of Refraction1.586
InChIKeyUIAYVIIHMORPSJ-UHFFFAOYSA-N
SMILESCN(C(=O)CCCOc1ccc2[nH]c(=O)ccc2c1)C1CCCCC1
Storage condition-20℃

Safety Information

Personal Protective EquipmentEyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADRUN 3249
Packaging GroupIII
Hazard Class6.1(b)

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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
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