101626-67-9
Chemical Structure
Lixazinone hydrogensulfate
Synonym(s): RS-82856 hydrogensulfate
- CAS No.: 101626-67-9
- Formula:C21H32N4O8S
- Molecular Weight:500.57
IUPAC Name: N-cyclohexyl-N-methyl-4-((2-oxo-2,3,5,10-tetrahydroimidazo[2,1-b]quinazolin-7-yl)oxy)butanamide sulfate hydrate
InChIKey: IXJGUUXNDBSBPT-UHFFFAOYSA-N
SMILES: O=C1N=C2NC3=CC=C(C=C3CN2C1)OCCCC(N(C4CCCCC4)C)=O.O=S(O)(O)=O.O
Biological Activity: Lixazinone (RS-82856) hydrogensulfate is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3) with an IC50 value of 22 nM. Lixazinone hydrogensulfate exhibits positive inotropic effects, afterload reduction and antithrombotic properties. Lixazinone hydrogensulfate 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 hydrogensulfate can be used in the research of polycystic kidney disease and congestive heart failure[1][2][3][4].
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Lixazinone hydrogensulfate | Lixazinone (RS-82856) hydrogensulfate is a selective inhibitor of cGMP-inhibited phosphodiesterase (PDE3) with an IC50 value of 22 nM. Lixazinone hydrogensulfate exhibits positive inotropic effects, afterload reduction and antithrombotic properties. Lixazinone hydrogensulfate 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 hydrogensulfate can be used in the research of polycystic kidney disease and congestive heart failure. | |||||||||||||||||||||
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- [1]. Dickinson NT, et al. Activation of cGMP-stimulated phosphodiesterase by nitroprusside limits cAMP accumulation in human platelets: effects on platelet aggregation. Biochem J. 1997;323 ( Pt 2)(Pt 2):371-377. [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]. Cheng J, et al. Lixazinone stimulates mitogenesis of Madin-Darby canine kidney cells. Exp Biol Med (Maywood). 2006;231(3):288-295. [Content Brief]
- [4]. 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
