Cilostazol
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Cilostazol ??
- ???
- 159-160°C
- ?? ?
- 499.57°C (rough estimate)
- ??
- 1.1832 (rough estimate)
- ???
- 1.7600 (estimate)
- ?? ??
- Inert atmosphere,Room Temperature
- ???
- DMSO: 18mg/mL, ???
- ??? ??
- ??
- ??? ??
- ??? ??
- ?? ?? (pKa)
- 14.22±0.20(Predicted)
- ??
- ???
- ?? ??(λmax)
- 257nm(MeOH)(lit.)
- Merck
- 14,2277
- ???
- -20°C?? DMSO? ?? 2?? ?? ?? ??
- ?? ??
- ???(???)
- InChI
- 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)
- InChIKey
- RRGUKTPIGVIEKM-UHFFFAOYSA-N
- SMILES
- N1C2=C(C=C(OCCCCC3N(C4CCCCC4)N=NN=3)C=C2)CCC1=O
??
| ??? ?? | Xi | ||
|---|---|---|---|
| WGK ?? | 2 | ||
| RTECS ?? | VC8277500 | ||
| HS ?? | 29339900 | ||
| ???? ??? | 11 - Combustible Solids | ||
| Hazard Classifications | Repr. 2 | ||
| ?? ?? ??? | 73963-72-1(Hazardous Substances Data) | ||
| ?? | LD50 in mice, rats (mg/kg): >2000, >2000 i.p.; >5000, >5000 orally (Nomura) |
Cilostazol C??? ??, ??, ??
??
Cilostazol is a platelet aggregation inhibitor with cerebral vasodilating activity, indicated for use in stroke and myocardial infarction. In patients with cerebral thrombosis, transient ischemia and cerebral arteriosclerosis, cilostazol significantly inhibits ADP-, collagenand epinephrine-induced platelet aggregation. Side effects include headache and tachycardia.??? ??
Colourless Needles??
A potent phosphodiesterase III A (PDE3A) inhibitor (IC50=0.2uM) and inhibitor of adenosine uptake. Has antimitogeni, antithrombotic, vasodilatory and cardiotonic properties in vivo. Also affects lipid levels in vivo??
ChEBI: A lactam that is 3,4-dihydroquinolin-2(1H)-one in which the hydrogen at position 6 is substiuted by a 4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy group.?? ??
Cilostazol is a potent cyclic nucleotide phosphodiesterase inhibitor. It is mainly used as antiplatelet agent.???? ??
Potent phosphodiesterase III A (PDE3A) inhibitor (IC 50 = 0.2 μ M) and inhibitor of adenosine uptake. Has antimitogenic, antithrombotic, vasodilatory and cardiotonic properties in vivo . Also affects lipid levels in vivo .Mechanism of action
Cilostazol exhibits greater selectivity than dipyridamole as an inhibitor of PDE3A. The drug does not affect the other PDEs (PDEs 1, 2, or 4). Cilostazol reversibly inhibit platelet aggregation induced by a number of stimuli, such as thrombin, ADP, collagen, or stress from exercise. Additionally, cilostazol inhibits adenosine uptake, leading to increased activity of adenosine at A1 and A2 receptors.Clinical Use
Cilostazol, a quinolinone derivative, is a potent orally active antiplatelet drug approved for the treatment of intermittent claudication (a peripheral artery disease resulting from blockage of blood vessels in the limbs).?? ??
Cilostazol is rapidly absorbed after oral administration, particularly with a high-fat meal, which greatly increases its bioavailability to approximately 90%. It is extensively metabolized in the liver by various cytochromes. The most important cytochromes appear to be CYP3A4 and, to lesser extent, by CYP2C19, with an elimination half-life of approximately 11 to 13 hours. Among the various metabolites produced (11 metabolites are known), the two major metabolites are 3,4-dehydrocilostazol and 4′-trans-hydroxycliostazol. These two metabolites are pharmacologically active. Studies indicate that the concomitant administration of cilostazol with CYP3A inhibitors can greatly increase cilostazol blood concentrations, and a dose reduction may be required. Similar results are seen when CYP2C19 is inhibited, leading to decreased formation of 4-trans-hydroxycliostazol and significant increases in cilostazol and 3,4-dehydrocilostazol.Cilostazol ?? ?? ? ???
???
Pentanamide
?? ???
1H-????
3,4-DIHYDROQUINOLIN-2(1H)-ONE
?
? ?????
2(1H)-Quinolinone, 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-, sulfate (1:1)
6-Hydroxy-2(1H)-3,4-dihydroquinolinone
2(1H)-Quinolinone, 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-, ethanedioate (1:1)
2(1H)-Quinolinone, 6-[4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy]-3,4-dihydro-, (2Z)-2-butenedioate (1:1)
?? ??
Cilostazol ?? ??
???( 596)?? ??
| ??? | ?? | ??? | ?? | ?? ? | ?? |
|---|---|---|---|---|---|
| Hangzhou Hyper Chemicals Limited | +86-0086-57187702781 +86-13675893055 |
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| BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD. | +86-18600796368 |
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| Capot Chemical Co.,Ltd. | +86-（0）57185586718 +86-13336195806 |
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| Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 |
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| Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
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| career henan chemical co | +86-0371-86658258 |
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| Xiamen AmoyChem Co., Ltd | +86-86-5926051114 |
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| CONIER CHEM AND PHARMA LIMITED | |
sales@conier.com | China | 49906 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354; +1-00000000000 |
marketing@targetmol.com | United States | 32431 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 |
1059@dideu.com | China | 29096 | 58 |
Cilostazol ?? ??:
5-???-????? 2-??????? ?????????
Pentetrazol
N-Hexadecyltrimethylammonium chloride
3-azidopropanoic acid
6-[3-(1-CYCLOHEXYL-1H-TETRAZOL-5-YL) PROPOXY]-2(1H)-QUINOLINONE
GJXNGCFWGJQETE-UHFFFAOYSA-N
Cilostazol Impurity
Cilostazol Related Compound C (50 mg) (1-(4-(5-Cyclohexyl-1H-tetrazol-1-yl)butyl)-6-(4-(1-cyclohexyl-1H-tetrazol-5-yl)butoxy)-3,4-dihydroquinolin-2(1H)-one)
Epoprostenol
6-HYDROXY-2(1H)-3,4-DIHYDROQUINOLINONE CILOSTAZOL INTERMEDIATE,The intermediate of Cilostazol,Intermediate of Cilostazol
6-Methoxy-3,4-dihydro-1H-quinolin-2-one
5-(4-chlorobutyl)-1-cyclohexyl-1H-tetrazole (intermediate of cilostazol)
3,4-Dehydro Cilostazol
4-CIS-HYDROXY CILOSTAZOL
4trans-Hydroxy Cilostazol
Cilostazol-d11,CILOSTAZOL METABOLITE