CAS Number73963-72-1
Synonyms6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydrochinolin-2(1H)-on; RETAL; Cilostazol; Cilostal; CILOSTAZOLE; Pletal; MFCD00866780; 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone; PLETAAL; CILASTAZOL; 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydroquinolin-2(1H)-one; CILOSTAZOL JP
Molecular FormulaC20H27N5O2
Molecular Weight369.46
Purity99.5%
Density1.3±0.1 g/cm3
Boiling Point664.7±55.0 °C at 760 mmHg
Melting Point159-160ºC
Appearanceoff-white solid
Symbol
Signal WordWarning
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 73963-72-1 |
| Catalog No. | 2A-9009792 |
| Chinese Name | 西洛他唑 |
| Synonyms | 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydrochinolin-2(1H)-on; RETAL; Cilostazol; Cilostal; CILOSTAZOLE; Pletal; MFCD00866780; 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-2(1H)-quinolinone; PLETAAL; CILASTAZOL; 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydroquinolin-2(1H)-one; CILOSTAZOL JP |
| Molecular Formula | C20H27N5O2 |
| Molecular Weight | 369.46 |
| Purity | 99.5 |
| Density | 1.3±0.1 g/cm3 |
| Boiling Point | 664.7±55.0 °C at 760 mmHg |
| Melting Point | 159-160ºC |
| Appearance | off-white solid |
| Water Solubility | DMSO: 18 mg/mL, soluble |
| Storage Condition | Store at RT |
| Application | Cilostazol (OPC 13013; OPC 21) is a PDE3A inhibitor present in the cardiovascular system with an IC50 of 200 nM. |
| HTC | 2933990090 |
| PubChem ID | 329823424 |
| MDL Number | MFCD00866780 |
| SMILES | O=C1CCc2cc(OCCCCc3nnnn3C4CCCCC4)ccc2N1 |
| InChI | 1S/C20H27N5O2/c26-20-12-9-15-14-17(10-11-18(15)21-20)27-13-5-4-8-19-22-23-24-25(19)16-6-2-1-3-7-16/h10-11,14,16H,1-9,12-13H2,(H,21,26) |
| InChI Key | RRGUKTPIGVIEKM-UHFFFAOYSA-N |
| NACRES Code | NA.24 |
| UNSPSC | 41116107 |
| Hazard Symbols | Transport |
| MSDS | msds/9792_1_73963_72_1.pdf |
| Bioactivity | Cilostazol(OPC 13013; OPC 21) is a potent inhibitor of PDE3A, the isoform of PDE 3 in the cardiovascular system (IC50=0.2 uM).IC50 Value: 0.2 uM [1]Target: PDE3Ain vitro: Cilostazol caused a concentration-dependent increase in the cAMP level in rabbit and human platelets with similar potency. Furthermore, cilostazol and milrinone were equally effective in inhibiting human platelet aggregation with a median inhibitory concentration (IC50) of 0.9 and 2 microM, respectively. In rabbit ventricular myocytes, however, cilostazol elevated cAMP levels to a significantly lesser extent (p < 0.05 vs. milrinone) [2]. Cilostazol inhibited SIPA dose-dependently in vitro. The IC50 value of cilostazol for inhibition of SIPA was 15 ± 2.6 microM (m ± SE, n=5), which was very similar to that (12.5 ± 2.1 microM) for inhibition of ADP-induced platelet aggregation. Cilostazolpotentiates the inhibition of SIPA by PGE1 and enhances its ability to increase cAMP concentrations [3].in vivo: A single oral adminstration of 100 mgcilostazol to healthy volunteers produced a significant inhibition of SIPA [3]. Male C57BL/6J mice were assigned to five groups: mice fed a normal diet (groups 1 and 2); 0.1% or 0.3% cilostazol-containing diet (groups 3 and 4, respectively); and 0.125% clopidogrel-containing diet (group 5). Two weeks after feeding, groups 2-5 were intraperitoneally administered carbon tetrachloride (CCl4 ) twice a week for 6 weeks, while group 1 was treated with the vehicle alone [4].Toxicity: Cilostazol in addition to dual antiplatelet therapy appears to be effective in reducing the risk of restenosis and repeat revascularization after PCI without any significant benefits for mortality or stent thrombosis [5]. Related Catalog Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Cardiovascular Disease References [1]. Schr?r K. The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9. [2]. Cone J, et al. Comparison of the effects of cilostazol and milrinone on intracellular cAMP levels and cellular function in platelets and cardiac cells. J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504. [3]. Minami N, et al. Inhibition of shear stress-induced platelet aggregation by cilostazol, a specific inhibitor of cGMP-inhibited phosphodiesterase, in vitro and ex vivo. Life Sci. 1997;61(25):PL 383-9. [4]. Saito S, et al. Cilostazol attenuates hepatic stellate cell activation and protects mice against carbon tetrachloride-induced liver fibrosis. Hepatol Res. 2013 Apr 19. [5]. Jang JS, et al. A meta-analysis of randomized controlled trials appraising the efficacy and safety of cilostazol after coronary artery stent implantation. Cardiology. 2012;122(3):133-43. Chemical & Physical Properties Density 1.3±0.1 g/cm3 Boiling Point 664.7±55.0 °C at 760 mmHg Melting Point 159-160ºC Molecular Formula C20H27N5O2 Molecular Weight 369.461 Flash Point 355.8±31.5 °C Exact Mass 369.216461 PSA 81.93000 LogP 3.05 Vapour Pressure 0.0±2.0 mmHg at 25°C Index of Refraction 1.676 InChIKey RRGUKTPIGVIEKM-UHFFFAOYSA-N SMILES O=C1CCc2cc(OCCCCc3nnnn3C3CCCCC3)ccc2N1 Storage condition Store at RT Water Solubility DMSO: 18 mg/mL, soluble |
| Use of | Properties Articles56 Name cilostazol Synonym More Synonyms Cilostazol Biological Activity Related Catalog Signaling Pathways >> Autophagy >> Autophagy Signaling Pathways >> Metabolic Enzyme/Protease >> Phosphodiesterase (PDE) Research Areas >> Cardiovascular Disease References [1]. Schr?r K. The pharmacology of cilostazol. Diabetes Obes Metab. 2002 Mar;4 Suppl 2:S14-9. [2]. Cone J, et al. Comparison of the effects of cilostazol and milrinone on intracellular cAMP levels and cellular function in platelets and cardiac cells. J Cardiovasc Pharmacol. 1999 Oct;34(4):497-504. [3]. Minami N, et al. Inhibition of shear stress-induced platelet aggregation by cilostazol, a specific inhibitor of cGMP-inhibited phosphodiesterase, in vitro and ex vivo. Life Sci. 1997;61(25):PL 383-9. [4]. Saito S, et al. Cilostazol attenuates hepatic stellate cell activation and protects mice against carbon tetrachloride-induced liver fibrosis. Hepatol Res. 2013 Apr 19. [5]. Jang JS, et al. A meta-analysis of randomized controlled trials appraising the efficacy and safety of cilostazol after coronary artery stent implantation. Cardiology. 2012;122(3):133-43. Chemical & Physical Properties Molecular Formula C20H27N5O2 Exact Mass 369.216461 PSA 81.93000 Index of Refraction 1.676 InChIKey RRGUKTPIGVIEKM-UHFFFAOYSA-N Storage condition Store at RT |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Shipping Name: UN |
| MSDS Transport Info | Module 14. Shipping information 14.1 United Nations number European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.2 United Nations shipping name European Land Transport Dangerous Regulations: Non-dangerous goods IMDG Code: Non-dangerous goods International air transport dangerous goods regulations: non-dangerous goods 14.3 Transport hazard categories European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.4 Package group European Land Transport Dangerous Regulations: -International Maritime Dangerous Regulations: -International Air Transport Dangerous Regulations: - 14.5 Environmental hazards European Land Transport Danger Regulations: No International Maritime Danger Regulations International Air Transport Danger Regulations: No Marine pollutants (yes/no): No 14.6 Special precautions No data available The above information is believed to be correct, but is not all-inclusive and should be used as a guide only. The information in this document is based on our current knowledge and is Correct safety instructions apply to this product. This information does not represent a warranty as to the properties of this product. See reverse side of invoice or packing slip. |
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