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Palosuran

CAS No.:
540769-28-6
Catalog Number:
AG00DB75
Molecular Formula:
C25H30N4O2
Molecular Weight:
418.5313
Pack Size
Purity
Availability
Location
Price(USD)
Quantity
  
5mg
99%
1 week
United States
$423
- +
10mg
99%
1 week
United States
$640
- +
50mg
99%
1 week
United States
$1557
- +
100mg
99%
1 week
United States
$2390
- +
Product Description
Catalog Number:
AG00DB75
Chemical Name:
Palosuran
CAS Number:
540769-28-6
Molecular Formula:
C25H30N4O2
Molecular Weight:
418.5313
MDL Number:
MFCD07772352
IUPAC Name:
1-[2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea
InChI:
InChI=1S/C25H30N4O2/c1-19-17-23(21-9-5-6-10-22(21)27-19)28-24(30)26-13-16-29-14-11-25(31,12-15-29)18-20-7-3-2-4-8-20/h2-10,17,31H,11-16,18H2,1H3,(H2,26,27,28,30)
InChI Key:
WYJCYXOCHXWTHG-UHFFFAOYSA-N
SMILES:
O=C(Nc1cc(C)nc2c1cccc2)NCCN1CCC(CC1)(O)Cc1ccccc1
UNII:
ULD9ZKE457
Properties
Complexity:
572  
Compound Is Canonicalized:
Yes
Covalently-Bonded Unit Count:
1  
Defined Atom Stereocenter Count:
0
Defined Bond Stereocenter Count:
0
Exact Mass:
418.237g/mol
Formal Charge:
0
Heavy Atom Count:
31  
Hydrogen Bond Acceptor Count:
4  
Hydrogen Bond Donor Count:
3  
Isotope Atom Count:
0
Molecular Weight:
418.541g/mol
Monoisotopic Mass:
418.237g/mol
Rotatable Bond Count:
6  
Topological Polar Surface Area:
77.5A^2
Undefined Atom Stereocenter Count:
0
Undefined Bond Stereocenter Count:
0
XLogP3:
3.3  
Literature
Title Journal
Prolidase could act as a diagnosis and treatment mediator in lung fibrosis. Inflammation 20121001
The efficiency of a urotensin II antagonist in an experimental lung fibrosis model. Inflammation 20120601
Mifepristone, a glucocorticoid receptor antagonist, produces clinical and metabolic benefits in patients with Cushing's syndrome. The Journal of clinical endocrinology and metabolism 20120601
Spironolactone lowers portal hypertension by inhibiting liver fibrosis, ROCK-2 activity and activating NO/PKG pathway in the bile-duct-ligated rat. PloS one 20120101
Down-regulation of GABA(A) receptor via promiscuity with the vasoactive peptide urotensin II receptor. Potential involvement in astrocyte plasticity. PloS one 20120101
Development of filtration-based time-resolved fluorescence assay for the high-throughput screening of urotensin II receptor antagonist. Assay and drug development technologies 20111001
Association analysis of urotensin II gene (UTS2) and flanking regions with biochemical parameters related to insulin resistance. PloS one 20110101
Link-based quantitative methods to identify differentially coexpressed genes and gene pairs. BMC bioinformatics 20110101
Potential Clinical Implications of the Urotensin II Receptor Antagonists. Frontiers in pharmacology 20110101
Urotensin II receptor and acetylcholine release from mouse cervical spinal cord nerve terminals. Neuroscience 20100929
Prediction of the three-dimensional structure for the rat urotensin II receptor, and comparison of the antagonist binding sites and binding selectivity between human and rat receptors from atomistic simulations. ChemMedChem 20100903
Expression of urotensin II and its receptor in human liver cirrhosis and fulminant hepatic failure. Digestive diseases and sciences 20100501
Effect of the urotensin receptor antagonist palosuran in hypertensive patients with type 2 diabetic nephropathy. Hypertension (Dallas, Tex. : 1979) 20100501
Urotensin-II contributes to pulmonary vasoconstriction in a perinatal model of persistent pulmonary hypertension of the newborn secondary to meconium aspiration syndrome. Pediatric research 20100201
Late-onset circulatory dysfunction after thyroid hormone treatment in an extremely low birth weight infant. Journal of pediatric endocrinology & metabolism : JPEM 20100101
Nonpeptide urotensin-II receptor antagonists: a new ligand class based on piperazino-phthalimide and piperazino-isoindolinone subunits. Journal of medicinal chemistry 20091210
Pro-angiogenic activity of Urotensin-II on different human vascular endothelial cell populations. Regulatory peptides 20091009
Pharmacokinetics and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy male subjects. Journal of clinical pharmacology 20091001
Effect of the urotensin-II receptor antagonist palosuran on secretion of and sensitivity to insulin in patients with Type 2 diabetes mellitus. British journal of clinical pharmacology 20091001
Expression and functional role of urotensin-II and its receptor in the adrenal cortex and medulla: novel insights for the pathophysiology of primary aldosteronism. The Journal of clinical endocrinology and metabolism 20090201
Palosuran inhibits binding to primate UT receptors in cell membranes but demonstrates differential activity in intact cells and vascular tissues. British journal of pharmacology 20081001
Urotensin II in cardiovascular regulation. Vascular health and risk management 20080801
Urotensin II and urotensin II-related peptide (URP) in cardiac ischemia-reperfusion injury. Peptides 20080501
Evidence for endogenous urotensin-II as an inhibitor of insulin secretion. Study in the perfused rat pancreas. Peptides 20080501
Cardiorenovascular effects of urotensin II and the relevance of the UT receptor. Peptides 20080501
Urotensin II and urotensin II-related peptide activate somatostatin receptor subtypes 2 and 5. Peptides 20080501
Hemodynamic effects of urotensin II and its specific receptor antagonist palosuran in cirrhotic rats. Hepatology (Baltimore, Md.) 20080401
Non peptidic urotensin II antagonists: perspectives for a new class of drugs. Cardiovascular & hematological agents in medicinal chemistry 20080401
Urotensin II: a new pharmacologic target in the treatment of cardiovascular disease. Cardiology in review 20080101
Comparative understanding of UTS2 and UTS2R genes for their involvement in type 2 diabetes mellitus. International journal of biological sciences 20080101
Role of urotensin II and its receptor in health and disease. Journal of anesthesia 20070101
Urotensin-II and its receptor (UT-R) are expressed in rat brain endothelial cells, and urotensin-II via UT-R stimulates angiogenesis in vivo and in vitro. International journal of molecular medicine 20061201
Pharmacodynamics and pharmacokinetics of the urotensin II receptor antagonist palosuran in macroalbuminuric, diabetic patients. Clinical pharmacology and therapeutics 20060901
Urotensin-II and UII-receptor expression and function in the rat adrenal cortex. International journal of molecular medicine 20060601
The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. The Journal of pharmacology and experimental therapeutics 20060301
Effect of lesions of cerebellar fastigial nuclei on lymphocyte functions of rats. Neuroscience research 20050301
Pharmacology of the urotensin-II receptor antagonist palosuran (ACT-058362; 1-[2-(4-benzyl-4-hydroxy-piperidin-1-yl)-ethyl]-3-(2-methyl-quinolin-4-yl)-urea sulfate salt): first demonstration of a pathophysiological role of the urotensin System. The Journal of pharmacology and experimental therapeutics 20041001
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