Cilostazol
![Cilostazol Structure](CAS/GIF/73963-72-1.gif)
- CAS No.
- 73963-72-1
- Chemical Name:
- Cilostazol
- Synonyms
- RETAL;OPC 21;PLETAL;PLETAAL;Cilostal;OPC 13013;Cilostazo;CILASTAZOL;CILOSTAZOL;CILOSTAZOLE
- CBNumber:
- CB2362876
- Molecular Formula:
- C20H27N5O2
- Molecular Weight:
- 369.46
- MOL File:
- 73963-72-1.mol
- MSDS File:
- SDS
- Modify Date:
- 2024/6/13 17:03:25
Melting point | 159-160°C |
---|---|
Boiling point | 499.57°C (rough estimate) |
Density | 1.1832 (rough estimate) |
refractive index | 1.7600 (estimate) |
storage temp. | Inert atmosphere,Room Temperature |
solubility | DMSO: 18 mg/mL, soluble |
form | solid |
pka | 14.22±0.20(Predicted) |
color | off-white |
λmax | 257nm(MeOH)(lit.) |
Merck | 14,2277 |
Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 2 months |
InChIKey | RRGUKTPIGVIEKM-UHFFFAOYSA-N |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() GHS08 |
---|---|
Signal word | Warning |
Hazard statements | H361d |
Precautionary statements | P201-P202-P280-P308+P313-P405-P501 |
Hazard Codes | Xi |
WGK Germany | 2 |
RTECS | VC8277500 |
HS Code | 29339900 |
Toxicity | LD50 in mice, rats (mg/kg): >2000, >2000 i.p.; >5000, >5000 orally (Nomura) |
Cilostazol price More Price(5)
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
Sigma-Aldrich(India) | PHR1503 | Cilostazol Pharmaceutical Secondary Standard; Certified Reference Material | 73963-72-1 | 1G | ₹15025.1 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | C0737 | Cilostazol ≥98% (HPLC), powder | 73963-72-1 | 10MG | ₹20177.8 | 2022-06-14 | Buy |
Sigma-Aldrich(India) | C0737 | Cilostazol ≥98% (HPLC), powder | 73963-72-1 | 50MG | ₹80646.25 | 2022-06-14 | Buy |
TCI Chemicals (India) | C2587 | Cilostazol | 73963-72-1 | 1G | ₹7500 | 2022-05-26 | Buy |
TCI Chemicals (India) | C2587 | Cilostazol | 73963-72-1 | 5G | ₹8000 | 2022-05-26 | Buy |
Cilostazol Chemical Properties,Uses,Production
Description
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.
Chemical Properties
Colourless Needles
Uses
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
Definition
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.
General Description
Cilostazol is a potent cyclic nucleotide phosphodiesterase inhibitor. It is mainly used as antiplatelet agent.
Biological Activity
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).
Metabolism
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 Preparation Products And Raw materials
Raw materials
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chevron_rightPreparation Products
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
Cadila Pharmaceuticals Ltd | +91-7069076657 +91-7069076657 | Ahmedabad, India | 54 | 58 | Inquiry |
SEUTIC | +91-8309787199 +91-8309787199 | Hyderabad, India | 124 | 58 | Inquiry |
KARUNESH REMEDIES | +919998776849 | Gujarat, India | 18 | 58 | Inquiry |
Glenmark Pharmaceuticals Limited | +912240189999 | Maharashtra, India | 93 | 58 | Inquiry |
Hetero Drugs Limited | +91-4023704923 +91-4023704923 | Telangana, India | 296 | 58 | Inquiry |
Ipca Laboratories Ltd | +91-2262105000 +91-2262105000 | Maharashtra, India | 61 | 58 | Inquiry |
Dayaram Pharma Chem | +91-9601766800 +91-9601766800 | Gujarat, India | 61 | 58 | Inquiry |
Afton Pharma | +91-9712000202 +91-9712000202 | Gujarat, India | 63 | 58 | Inquiry |
Fleming Laboratories Ltd | +91-9666407333 +91-9666022445 | Hyderabad, India | 22 | 58 | Inquiry |
Cleargreens Pharmaceutical Private Limited | +91-9879791802 +91-9579898158 | Gujarat, India | 14 | 58 | Inquiry |
Supplier | Advantage |
---|---|
Cadila Pharmaceuticals Ltd | 58 |
SEUTIC | 58 |
KARUNESH REMEDIES | 58 |
Glenmark Pharmaceuticals Limited | 58 |
Hetero Drugs Limited | 58 |
Ipca Laboratories Ltd | 58 |
Dayaram Pharma Chem | 58 |
Afton Pharma | 58 |
Fleming Laboratories Ltd | 58 |
Cleargreens Pharmaceutical Private Limited | 58 |
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