94192-59-3
Chemical Structure
Lixazinone
Synonym(s): RS-82856
- CAS No.: 94192-59-3
- Formula:C21H28N4O3
- Molecular Weight:384.48
IUPAC Name: N-cyclohexyl-N-methyl-4-((2-oxo-2,3,5,10-tetrahydroimidazo[2,1-b]quinazolin-7-yl)oxy)butanamide
InChIKey: WUECXCBONAGRSA-UHFFFAOYSA-N
SMILES: O=C1N=C2NC3=CC=C(OCCCC(=O)N(C)C4CCCCC4)C=C3CN2C1
Biological Activity: Lixazinone (RS-82856) is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3) with an IC50 value of 22 nM. Lixazinone exhibits positive inotropic effects, afterload reduction and antithrombotic properties. Lixazinone increases cyclic adenosine monophosphate (cAMP) levels in human platelets, inhibits thrombin-induced aggregation of human platelets, and blocks the photolabeling of PDE3 active sites by [32P]cGMP. Lixazinone can be used in the research of polycystic kidney disease and congestive heart failure[1][2][3][4].
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Lixazinone | Lixazinone (RS-82856) is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3) with an IC50 value of 22 nM. Lixazinone exhibits positive inotropic effects, afterload reduction and antithrombotic properties. Lixazinone increases cyclic adenosine monophosphate (cAMP) levels in human platelets, inhibits thrombin-induced aggregation of human platelets, and blocks the photolabeling of PDE3 active sites by [32P]cGMP. Lixazinone can be used in the research of polycystic kidney disease and congestive heart failure. | |||||||||||||||||||||
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- [1]. Cheng J, et al. Lixazinone stimulates mitogenesis of Madin-Darby canine kidney cells. Exp Biol Med (Maywood). 2006;231(3):288-295. [Content Brief]
- [2]. Tang KM, et al. Photoaffinity labelling of cyclic GMP-inhibited phosphodiesterase (PDE III) in human and rat platelets and rat tissues: effects of phosphodiesterase inhibitors. Eur J Pharmacol. 1994;268(1):105-114. [Content Brief]
- [3]. Chini CC, et al. Compartmentalization of cAMP signaling in mesangial cells by phosphodiesterase isozymes PDE3 and PDE4. Regulation of superoxidation and mitogenesis. J Biol Chem. 1997 Apr 11;272(15):9854-9. [Content Brief]
Keywords
