Cilostamide (OPC 3689)A specific phosphodiesterase 3 (PDE3) inhibitor

Cilostamide (OPC 3689) (CAS 68550-75-4)

Cilostamide (OPC 3689) | CAS 68550-75-4 is rated 5.0 out of 5 by 1.
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Synonym: Cilostamidum
Application: A specific phosphodiesterase 3 (PDE3) inhibitor
CAS Number: 68550-75-4
Purity: ≥98%
Molecular Weight: 342.43
Molecular Formula: C20H26N2O3
* Refer to Certificate of Analysis for lot specific data (including water content).
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Cilostamide (OPC 3689) is a specific PDE3 (phosphodiesterase 3) inhibitor. The compound has been shown to block DNA binding of p-Stat3, increase cAMP levels and block the effects of insulin and IGF-1 on meiosis. Additionally, Cilostamide activates K(ATP) channels and produces hyperpolarization in rat mesenteric artery studies. In F/B cells Cliostamide has been reported to inhibit the IGF-1 induced phosphorylation of the apoptotic protein, Bad. Cilostamide (OPC 3689) is a inhibitor of PDE3A and PDE3B.


References

1. Tang, K.M., et al. 1994. Eur. J. Pharmacol. 268: 105-114. PMID: 7925608
2. Verghese, M.W., et al. 1995. J. Pharmacol. Exp. Ther. 272: 1313-1320. PMID: 7891349
3. Andersen, C.B., et al. 1998. J. Biol. Chem. 273: 18705-18708. PMID: 9668041
4. Ahmad, F., et al. 2000. J. Immunol. 164: 4678-4688. PMID: 10779773
5. Zhao, A.Z., et al. 2002. Nat. Neurosci. 5: 727-728. PMID: 12101402
6. Hanson, M.S., et al. 2008. Am. J. Physiol. Heart Circ. Physiol. 295: H786-H793. PMID: 18586889
7. Park, W.K., et al. 2009. Acta Anaesthesiol Scand. 53: 1043-1051. PMID: 19572940
8. Abi-Gerges, A., et al. 2009. Circ. Res. 105: 784-792. PMID: 19745166
9. Kansui, Y., et al. 2009. Clin. Exp. Pharmacol. Physiol. 36: 729-733. PMID: 19207721
10. Dimopoulos, G.J., et al. 2009. Vascul. Pharmacol. 50: 78-82. PMID: 19007913

Physical State :
Solid
Solubility :
Soluble in DMSO (25 mg/ml), and ethanol (15 mg/ml).
Storage :
Store at room temperature
Melting Point :
228.48° C (Predicted)
Boiling Point :
594.32° C at 760 mmHg (Predicted)
Density :
1.19 g/cm3 (Predicted)
Refractive Index :
n20D 1.59 (Predicted)
IC50 :
PDE3A: IC50 = 0.027 µM; PDE3B: IC50 = 0.050 µM; ADP-induced platelet aggregation: IC50 = 16.8 µM; cGMP-inhibited phosphodiesterase: IC50 = 70 nM
Ki Data :
Phosphodiesterase 3B: Ki= 5 nM (human); Phosphodiesterase 3A: Ki= 20 nM (human)
pK Values :
pKb: 9.73 (Predicted)
For Research Use Only. Not Intended for Diagnostic or Therapeutic Use.
WGK Germany :
3
PubChem CID :
2753
MDL Number :
MFCD00673958
SMILES :
CN(C1CCCCC1)C(=O)CCCOC2=CC3=C(C=C2)NC(=O)C=C3

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Cilostamide (OPC 3689)  Product Citations

See how others have used Cilostamide (OPC 3689). Click on the entry to view the PubMed entry .

Citations 1 to 9 of 9 total

PMID: # 19959669  Hertz, AL. et al. 2009. Proc. Natl. Acad. Sci. U.S.A. 106: 21978-21983.

PMID: # 19332778  Puxeddu, E. et al. 2009. Proc. Natl. Acad. Sci. U.S.A. 106: 6158-6163.

PMID: # 11839681  Moon, E. et al. 2002. Clin. Cancer Res. 8: 589-595.

PMID: # 12453887  Onuma, H. et al. 2002. Diabetes. 51: 3362-3367.

PMID: # 10779773  Ahmad, F. et al. 2000. J. Immunol. 164: 4678-4688.

PMID: # 9668041  Andersen, CB. et al. 1998. J. Biol. Chem. 273: 18705-18708.

PMID: # 2550445  Robinson, FW. et al. 1989. J. Biol. Chem. 264: 16458-16464.

PMID: # 2554303  Swinnen, JV. et al. 1989. Proc. Natl. Acad. Sci. U.S.A. 86: 8197-8201.

PMID: # 3018742  Macphee, CH. et al. 1986. Proc. Natl. Acad. Sci. U.S.A. 83: 6660-6663.

Citations 1 to 9 of 9 total
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Rated 5 out of 5 by from Hertz et Hertz et. al. (PubMed ID 19959669) used Cilostamide (OPC 3689) to prevent cAMP degradation by inhibiting the function of phosphodiesterase 3 in order to examine macrophage inflammatory response. -SCBT Publication Review
Date published: 2015-03-19
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