ACT 058362; PALOSURAN,

• 常用名: ACT 058362; PALOSURAN,
• 英文名: Palosuran
• CAS号: 540769-28-6
• 分子量: 418.53100
• 密度: N/A
• 沸点: N/A
• 分子式: C₂₅H₃₀N₄O₂
• 熔点: N/A
• 闪点: N/A

ACT 058362; PALOSURAN,用途

Palosuran (ACT-058362)是高活性人UT受体特异性拮抗剂,IC50为3.6 nM。

ACT 058362; PALOSURAN,名称

• 中文名: Palosuran
• 英文名: 1-[2-(4-benzyl-4-hydroxypiperidin-1-yl)ethyl]-3-(2-methylquinolin-4-yl)urea

ACT 058362; PALOSURAN,生物活性

• 描述: Palosuran (ACT-058362)是高活性人UT受体特异性拮抗剂,IC50为3.6 nM。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> Urotensin Receptor
  研究领域 >> 代谢疾病
• 参考文献:

  [1]. Clozel M, et al. 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 S

  [2]. Clozel M, et al. The urotensin-II receptor antagonist palosuran improves pancreatic and renal function in diabetic rats. J Pharmacol Exp Ther. 2006 Mar;316(3):1115-21.

  [3]. Sidharta PN, et al. Pharmacodynamics and pharmacokinetics of the urotensin II receptor antagonist palosuran in macroalbuminuric, diabetic patients. Clin Pharmacol Ther. 2006 Sep;80(3):246-56.

  [4]. Trebicka J, et al. Hemodynamic effects of urotensin II and its specific receptor antagonist palosuran in cirrhotic rats. Hepatology. 2008 Apr;47(4):1264-76.

  [5]. Sidharta PN, et al. Pharmacokinetics and pharmacodynamics of the urotensin-II receptor antagonist palosuran in healthy male subjects. J Clin Pharmacol. 2009 Oct;49(10):1168-75.

ACT 058362; PALOSURAN,物理化学性质

• 分子式: C₂₅H₃₀N₄O₂
• 分子量: 418.53100
• 精确质量: 418.23700
• PSA: 84.21000
• LogP: 3.29850
• InChIKey: WYJCYXOCHXWTHG-UHFFFAOYSA-N
• SMILES: Cc1cc(NC(=O)NCCN2CCC(O)(Cc3ccccc3)CC2)c2ccccc2n1
• 外观性状: white solid
• 储存条件: -20℃

ACT 058362; PALOSURAN,靶点实验

查看更多实验

实验名称：Primary qHTS assay for small molecule inhibitors of Inositol hexaphosphate kinase 1 (... 来源：NCGC External Id：IP6K1-p1

实验名称：Thermal Shift Assay. Domain: start/stop: M1-L298 来源：ChEMBL 靶标：Cyclin-dependent kinase 2 External Id：CHEMBL5062802

实验名称：Thermal Shift Assay. Domain: start/stop: N44-E168 来源：ChEMBL 靶标：Bromodomain-containing protein 4 External Id：CHEMBL5061773

实验名称：Cytochrome P450 family 3 subfamily A member 4 (CYP3A4) small molecule antagonists: lu... 来源：NCGC External Id：CYP3A4437

实验名称：Cytochrome P450 family 2 subfamily D member 6 (CYP2D6) small molecule antagonists: lu... 来源：NCGC External Id：CYP2D6395

实验名称：Cytochrome P450 family 2 subfamily C member 9 (CYP2C9) small molecule antagonists: lu... 来源：NCGC External Id：CYP2C9536

实验名称：Human UT receptor (Urotensin receptor) 来源：IUPHAR-DB 靶标：UT receptor (Urotensin receptor) [Homo sapiens] External Id：365_Human

实验名称：Primary qHTS for Identification of Calcium Integrin Binding Protein 1 (CIB1) Competit... 来源：NCGC External Id：CIB1-p1-p2

实验名称：Thermal Shift Assay. Domain: start/stop: M26-R383 来源：ChEMBL 靶标：Glycogen synthase kinase-3 beta External Id：CHEMBL5065589

实验名称：Thermal Shift Assay. Domain: start/stop: S229-K512 来源：ChEMBL 靶标：Tyrosine-protein kinase ABL1 External Id：CHEMBL5060015

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ACT 058362; PALOSURAN,英文别名

• UNII-ULD9ZKE457
• Palosuran
• ACT 058362