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PDE3 inhibitor K-134

Chemical Structure : PDE3 inhibitor K-134

CAS No.: 189362-06-9

PDE3 inhibitor K-134 (OPC-33509, OPC33509, K134)

Catalog No.: PC-28250Not For Human Use, Lab Use Only.

K-134 (OPC-33509) is a potent, selective phosphodiesterase-3 (PDE3) inhibitor with IC50 of 0.1 uM and 0.28 uM for PDE3A and PDE3B, shows much weaker activity for PDE5 and does not inhibit PDE2 and PDE4.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

K-134 (OPC-33509) is a potent, selective phosphodiesterase-3 (PDE3) inhibitor with IC50 of 0.1 uM and 0.28 uM for PDE3A and PDE3B, shows much weaker activity for PDE5 and does not inhibit PDE2 and PDE4.
K-134 also inhibits binding between CD36 and collagen type-I.
K-134 blocks rat platelet aggregation more potently than cilostazol in vitro.
K-134 inhibits mouse platelet aggregation induced by collagen and ADP in a dose-dependent manner.

Physicochemical Properties

M.Wt 399.49
Formula C22H29N3O4
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-cyclopropyl-1-((1R,2R)-2-hydroxycyclohexyl)-3-(3-((2-oxo-1,2-dihydroquinolin-6-yl)oxy)propyl)urea

References

1. Yoshida H, et al. PLoS One. 2012;7(10):e46432.

2. Sasaki Y, et al. Eur J Pharmacol. 2012 Aug 15;689(1-3):132-8.

3. Ikenoya M, et al. Biochem Biophys Res Commun. 2007 Feb 23;353(4):1111-4.

4. Sudo T, et al. Biochem Pharmacol 2000, 59: 347–356.

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