HEC96719_product_DataBase

Bioactivity	HEC96719 is a selective and orally active tricyclic farnesoid X receptor (FXR) agonist with EC50 values of 1.37 and 1.55 nM by time-resolved fluorescence energy transfer (TR-FRET) and luciferase reporter assays, respectively. HEC96719 significantly improves non-alcoholic steatohepatitis (NASH) and liver fibrosis with favorable tissue distribution in liver and intestine. HEC96719 can be used for the research of non-alcoholic steatohepatitis[1].
Target	EC50: 1.37 nM (FXR, TR-FRET), 1.55 nM (FXR, luciferase reporter assay).
In Vivo	HEC96719 (0.5，1.5 和 5 mg/kg；口服，每天 1 次，共 14 天) 通过测定增加成纤维细胞生长因子 15 (FGF15) 的水平证明激活了 FXR[1].HEC96719 (5 mg/kg；口服，1 次) 增加肝胆盐输出泵 (BSEP) 的水平和回肠中 FGF15 的水平[1]。HEC96719 (0.1, 0.3 和 1 mg/kg；口服，每日 1 次，持续 6 周) 显著改善非酒精性脂肪性肝炎 (NASH) 症状[1]。HEC96719 (0.1，0.3 和 1 mg/kg；口服，每日 1 次，持续 4 周) 对改善肝纤维化有效果，且优于奥贝胆酸 (OCA)[1]。 Animal Model:
Name	HEC96719
CAS	2181834-03-5
Formula	C29H22Cl2N2O5
Molar Mass	549.40
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Cao S, et al. Discovery of a tricyclic farnesoid X receptor agonist HEC96719, a clinical candidate for treatment of non-alcoholic steatohepatitis. Eur J Med Chem. 2022 Feb 15;230:114089.

PeptideDB

HEC96719

CAS: 2181834-03-5 F: C29H22Cl2N2O5 W: 549.40