HPG1860

CAS: 2226133-29-3 F: C27H26Cl2N4O4S W: 573.49

HPG1860 is an orally active, highly selective and potent FXR agonist, with an EC50 of 18 nM (FXR-luciferase reporter ass

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Bioactivity	HPG1860 is an orally active, highly selective and potent FXR agonist, with an EC50 of 18 nM (FXR-luciferase reporter assay). HPG1860 has EC50 values >30.0 μM for TGR5 and 13 other related nuclear receptors (cAMP biological assay). HPG1860 can be used for the research of non-alcoholic steatohepatitis (NASH)[1].
Invitro	HPG1860 (Compound 23) 通过时间分辨荧光能量转移 (TR-FRET) 和荧光素酶报告实验测得对 FXR 的 EC50 值分别为 5 nM 和 18 nM[1]。HPG1860 具有良好的人、大鼠、狗和猴肝微粒体稳定性，t1/2 分别为 447.18、115.79、237.17 和 154.38 min[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> HPG1860 相关抗体:
In Vivo	HPG1860 (3 mg/kg，口服) 可显著促进肝脏和回肠中 FXR 靶基因 (SHP, BSEP and FGF15) 的表达[1]。HPG1860 (1-10 mg/kg，口服，一天一次，27 天) 在高脂饮食和四氯化碳 (HY-Y0298) 诱导的非酒精性脂肪性肝炎小鼠模型中显示出强烈的抗纤维化和抗非酒精性脂肪性肝炎活性[1]。HPG1860 显示出良好的药代动力学特征[1]。HPG1860 在小鼠、大鼠和狗体内的药代动力学参数
CAS	2226133-29-3
Formula	C27H26Cl2N4O4S
Molar Mass	573.49
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]. Mo C, et al. Discovery of HPG1860, a Structurally Novel Nonbile Acid FXR Agonist Currently in Clinical Development for the Treatment of Nonalcoholic Steatohepatitis. Journal of medicinal chemistry. 2023, 66(14), 9363–9375.