CilostazolA PDE inhibitor, antimitogenic, antithrombotic, and cardiotonic agent

Cilostazol (CAS 73963-72-1)

Cilostazol | CAS 73963-72-1 is rated 5.0 out of 5 by 1.
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Synonym: 6-[4-(1-Cyclohexyl-1H-tetrazol-5-yl)-butoxy]-3,4-dihydro-2(1H)-quinolinone; Pletal; Cilostazolum
Application: A PDE inhibitor, antimitogenic, antithrombotic, and cardiotonic agent
CAS Number: 73963-72-1
Purity: 98%
Molecular Weight: 369.5
Molecular Formula: C20H27N5O2
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cilastazol is a 2-oxo-quinoline with vasodilator, antimitogenic, antithrombotic, and cardiotonic properties. This compound has been shown to cause inhibition of adenosine uptake, eventually resulting in changes to cAMP levels. Studies have shown Cilostazol to be a potent inhibitor of PDE3A (phosphodiesterase 3A) in vitro. PDE3A is often in the Cardiac system. In addition Cilastazol has also been observed to inhibit mitogenesis, migration of vascular smooth muscle cells, and platelet aggregation in vitro. Cilostazol displays a capacity to lower levels of serum triglycerides and cause some increase in HDL-cholesterol levels in vitro.


References

1. Schrör, K. 2002. Diabetes Obes Metab. 4: S14-S19. PMID: 12180353
2. Kambayashi, J., et al. 2003. Curr. Pharm. Des. 9: 2289-2302. PMID: 14529391
3. Lee, J.H., et al. 2004. J. Pharmacol. Exp. Ther. 308: 896-903. PMID: 14634032
4. Lee, J.H., et al. 2008. CNS Neurosci Ther. 14: 143-152. PMID: 18482026

Physical State :
Solid
Solubility :
Soluble in DMSO (18 mg/ml), ethanol (4 mg/ml), acetic acid, chloroform, and n-methyl-2-pyrrolidone.
Storage :
Store at room temperature
Melting Point :
236.84° C (Predicted)
Boiling Point :
~664.7° C at 760 mmHg (Predicted)
Density :
~1.3 g/cm3 (Predicted)
Refractive Index :
n20D 1.68 (Predicted)
IC50 :
Adenosine A2a receptor: IC50 = 29 µM (human); Adenosine A2b receptor: IC50 = 29 µM (human); Adenosine A1 receptor: IC50 = 29 µM (Oryctolagus cuniculus); Plasma: IC50 = 40 µM (Rattus norvegicus); Adenosine A3 receptor: IC50 = 29 µM (Oryctolagus cuniculus); PDE3A: IC50 = 0.2 µM
pK Values :
pKb: 2.19
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
2
RTECS :
VC8277500
PubChem CID :
2754
Merck Index :
14: 2277
MDL Number :
MFCD00866780
Beilstein Registry :
3632017
SMILES :
C1CCC(CC1)N2C(=NN=N2)CCCCOC3=CC4=C(C=C3)NC(=O)CC4

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Certificate of Analysis

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Cilostazol  Product Citations

See how others have used Cilostazol. Click on the entry to view the PubMed entry .

Citations 1 to 2 of 2 total

PMID: # 25843350  Kim, T. et al. 2015. Metab. Eng. 29: 169-79.

PMID: # 15908466  Matsumoto, T. et al. 2005. Am. J. Physiol. Heart Circ. Physiol. 289: H1933-H1940.

Citations 1 to 2 of 2 total
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Rated 5 out of 5 by from Matsumoto Matsumoto, et. al. (PubMed ID 15908466) found that cilostazol improved EDHF-type relaxations in streptozotocin-induced diabetic rats via an increae in cAMP and PKA signaling.
Date published: 2015-03-31
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