CAY10789 (化合物 6) 是有效的CysLT1R拮抗剂 ，IC50值为2.80 μM。CAY10789 也是一种GPBAR1激动剂 ，EC50为3 μM。CAY10789 显著降低 U937 细胞对 HAEC 的粘附并降低 TNF-α 的表达。CAY10789 表现出有前途的代谢稳定性和出色的药代动力学。 CAY10789 可用于结肠炎、代谢综合征和其他 GPBAR1/CysLT1R 相关疾病的研究。

CAY10789 (compound 6) is a potent CysLT1R (cysteinyl leukotriene receptor 1) antagonist with an IC50 of 2.80 μM. CAY10789 is also a GPBAR1 (G-protein-coupled bile acid receptor 1) agonist with an EC50 of 3 μM. CAY10789 significantly decreases the adhesion of U937 cells to HAEC and decreases the expression of TNF-α. CAY10789 exhibits very promising metabolic stability and excellent pharmacokinetics. CAY10789 can be used in the study of colitis, metabolic syndromes, and other GPBAR1/CysLT1R-related diseases [1].

123226-28-8

C17H15NO2

265.31

(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years