PRX-08066游离态

• 常用名: PRX-08066游离态
• 英文名: PRX-08066
• CAS号: 866206-54-4
• 分子量: 401.888
• 密度: 1.4±0.1 g/cm3
• 沸点: 579.9±50.0 °C at 760 mmHg
• 分子式: C₁₉H₁₇ClFN₅S
• 熔点: N/A
• 闪点: 304.5±30.1 °C

PRX-08066游离态用途

PRX-08066是5-HT受体2B(5-HT2BR)拮抗剂,IC50为3.4 nM,能选择性的促使肺动脉血管舒张。

PRX-08066游离态名称

• 中文名: PRX-08066
• 英文名: 5-[[4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl]methyl]-2-fluorobenzonitrile

PRX-08066游离态生物活性

• 描述: PRX-08066是5-HT受体2B(5-HT2BR)拮抗剂,IC50为3.4 nM,能选择性的促使肺动脉血管舒张。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
  信号通路 >> 神经信号通路 >> 5-HT受体
  研究领域 >> 心血管疾病
• 参考文献:

  [1]. Porvasnik SL, et al. PRX-08066, a novel 5-hydroxytryptamine receptor 2B antagonist, reduces monocrotaline-induced pulmonary arterial hypertension and right ventricular hypertrophy in rats. J Pharmacol Exp Ther. 2010 Aug;334(2):364-72.

  [2]. Svejda B, et al. The 5-HT(2B) receptor plays a key regulatory role in both neuroendocrine tumor cell proliferation and the modulation of the fibroblast component of the neoplastic microenvironment. Cancer. 2010 Jun 15;116(12):2902-12.

  [3]. Warburton R.R., et al. Online University.

PRX-08066游离态物理化学性质

• 密度: 1.4±0.1 g/cm3
• 沸点: 579.9±50.0 °C at 760 mmHg
• 分子式: C₁₉H₁₇ClFN₅S
• 分子量: 401.888
• 闪点: 304.5±30.1 °C
• 精确质量: 401.087708
• PSA: 93.08000
• LogP: 4.22
• InChIKey: IENZFHBNCRQMNP-UHFFFAOYSA-N
• SMILES: N#Cc1cc(CN2CCC(Nc3ncnc4sc(Cl)cc34)CC2)ccc1F
• 蒸汽压: 0.0±1.6 mmHg at 25°C
• 折射率: 1.682
• 储存条件: 2-8°C，避光，保存于惰性气体中

PRX-08066游离态靶点实验

查看更多实验

实验名称：Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibitio... 来源：ChEMBL 靶标：5-hydroxytryptamine receptor 2B External Id：CHEMBL968751

实验名称：Antagonist activity at 5-HT2B receptor expressed in CHOK1 cells assessed as inhibitio... 来源：ChEMBL 靶标：5-hydroxytryptamine receptor 2B External Id：CHEMBL968750

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：Selectivity for 5-HT2B receptor over 5-HT2A receptor 来源：ChEMBL 靶标：N/A External Id：CHEMBL968746

实验名称：Protein binding in plasma by dialysis method 来源：ChEMBL 靶标：N/A External Id：CHEMBL968748

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：Hepatic blood flow in Wistar rat at 1 mg/kg, iv 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL969579

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：AUC in Wistar rat at 10 mg/kg, po 来源：ChEMBL 靶标：Rattus norvegicus External Id：CHEMBL969581

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PRX-08066游离态英文别名

• 5-({4-[(6-chlorothieno[2,3-d]pyrimidin-4-yl)amino]piperidin-1-yl}methyl)-2-fluorobenzonitrile
• PRX-08066
• 5-({4-[(6-Chlorothieno[2,3-d]pyrimidin-4-yl)amino]-1-piperidinyl}methyl)-2-fluorobenzonitrile
• 5-((4-(6-chlorothieno[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl)methyl)-2-fluorobenzonitrile