CAY10580

• 常用名: CAY10580
• 英文名: CAY10580
• CAS号: 64054-40-6
• 分子量: 341.49
• 密度: 1.0±0.1 g/cm3
• 沸点: 534.4±25.0 °C at 760 mmHg
• 分子式: C₁₉H₃₅NO₄
• 熔点: N/A
• 闪点: 277.0±23.2 °C

CAY10580用途

CAY10580是一种有效和选择性的前列腺素EP4受体激动剂(Ki=35 nM)[1]。

CAY10580名称

• 英文名: 7-[2-(3-hydroxyoctyl)-5-oxopyrrolidin-1-yl]heptanoic acid

CAY10580生物活性

• 描述: CAY10580是一种有效和选择性的前列腺素EP4受体激动剂(Ki=35 nM)[1]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> 前列腺素受体
  研究领域 >> 代谢疾病
• 靶点实验:

  EP4:35 nM (Ki)

  EP4 Receptor:35 nM (Ki)

  EP2 Receptor:3000 nM (Ki)

  EP3 receptor:2000 nM (Ki)

• 体外研究: CAY10580(10-10000纳米；40分钟)在100-10000纳米时显著增加MDCK细胞中AQP2的顶膜丰度[2]。
• 体内研究: CAY10580(200μg/kg体重；腹腔注射；每日三周)有效预防饮食诱导的高胆固醇血症,增强内源性胆汁酸合成及其排泄[3]。动物模型：6周龄雄性EP4+/+小鼠(治疗高脂饮食攻击小鼠)[3]剂量：200μg/kg体重给药：腹腔注射；结果：高脂饮食喂养的小鼠与溶媒组相比,总胆固醇水平降低了28.5%。总胆固醇水平从137.4毫克/分升降至98.2毫克/分升,使血浆胆固醇恢复到接近正常值。
• 参考文献:

  [1]. Billot X, et al. Discovery of a potent and selective agonist of the prostaglandin EP4 receptor. Bioorg Med Chem Lett. 2003;13(6):1129-1132.

  [2]. Olesen ET, et al. Vasopressin-independent targeting of aquaporin-2 by selective E-prostanoid receptor agonists alleviates nephrogenic diabetes insipidus. Proc Natl Acad Sci U S A. 2011;108(31):12949-12954.

  [3]. Ying F, et al. EP4 emerges as a novel regulator of bile acid synthesis and its activation protects against hypercholesterolemia. Biochim Biophys Acta Mol Cell Biol Lipids. 2018;1863(9):1029-1040.

CAY10580物理化学性质

• 密度: 1.0±0.1 g/cm3
• 沸点: 534.4±25.0 °C at 760 mmHg
• 分子式: C₁₉H₃₅NO₄
• 分子量: 341.49
• 闪点: 277.0±23.2 °C
• 精确质量: 341.256622
• PSA: 77.84000
• LogP: 2.88
• InChIKey: CBWGHEDGUILASE-UHFFFAOYSA-N
• SMILES: CCCCCC(O)CCC1CCC(=O)N1CCCCCCC(=O)O
• 蒸汽压: 0.0±3.2 mmHg at 25°C
• 折射率: 1.494

CAY10580靶点实验

查看更多实验

实验名称：Binding affinity towards FP receptor expressed in HEK293 ebna cells recombinantly exp... 来源：ChEMBL 靶标：Prostaglandin F2-alpha receptor External Id：CHEMBL767494

实验名称：Binding affinity towards EP1 receptor expressed in HEK293 ebna cells recombinantly ex... 来源：ChEMBL 靶标：Prostaglandin E2 receptor EP1 subtype External Id：CHEMBL765913

实验名称：Dissociation constant, pKa of the compound 来源：ChEMBL 靶标：N/A External Id：CHEMBL3282300

实验名称：Binding affinity towards EP4 receptor expressed in HEK293 ebna cells recombinantly ex... 来源：ChEMBL 靶标：Prostaglandin E2 receptor EP4 subtype External Id：CHEMBL767817

实验名称：Retardation factor, Rf of the compound 来源：ChEMBL 靶标：N/A External Id：CHEMBL3282299

实验名称：Binding affinity to prostaglandin receptor in Charles River CD-1 mouse ovary assessed... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3282302

实验名称：Binding affinity towards EP2 receptor expressed in HEK293 ebna cells recombinantly ex... 来源：ChEMBL 靶标：Prostaglandin E2 receptor EP2 subtype External Id：CHEMBL765914

实验名称：Binding affinity to prostaglandin receptor in Charles River CD-1 mouse ovary assessed... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3282301

实验名称：Binding affinity towards EP3 receptor expressed in HEK293 ebna cells recombinantly ex... 来源：ChEMBL 靶标：Prostaglandin E2 receptor EP3 subtype External Id：CHEMBL765915

实验名称：Displacement of [3H-PGE1] from Sprague-Dawley rat kidney prostaglandin receptor after... 来源：ChEMBL 靶标：N/A External Id：CHEMBL3282304

共14条，当前第1页，共2页

1

2

CAY10580英文别名

• 7-[2-(3-Hydroxyoctyl)-5-oxo-1-pyrrolidinyl]heptanoic acid