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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Farnesoid X Receptor (FXR)-HPG1860
HPG1860

Chemical Structure : HPG1860

CAS No.: 2226133-29-3

HPG1860 (HPG-1860)

货号: PC-20980Not For Human Use, Lab Use Only.

HPG1860 is a potent, selective, nonbile acid full FXR agonist with EC50 of 5 nM and 18 nM in FR-FRET and luciferase assays, respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

HPG1860 is a potent, selective, nonbile acid full FXR agonist with EC50 of 5 nM and 18 nM in FR-FRET and luciferase assays, respectively.
HPG1860 shows extensive selectivity profiling across TGR5, and 13 relevant nuclear receptors in a cAMP biological assay with EC50s >30.0 μM.
HPG1860 (3 mg/kg, oral) shows clear in vivo efficacy of upregulating FXR target genes (SHP, BSEP, and FGF15) in liver and ileum in male C57/BL6J mice.
HPG1860 (30 mg/kg) shows potent antifibrosis and anti-NASH activities in HFD-CCl4-induced mouse model.

物理化学性质&存储条件

分子量 573.49
分子式 C27H26Cl2N4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

O=C(C1=CC(OC)=C2N=C(N3[C@H](C)CN(CC4=C(C5CC5)ON=C4C6=C(Cl)C=CC=C6Cl)CC3)SC2=C1)O

参考文献

1. Mo C, et al. J Med Chem. 2023 Jul 9. doi: 10.1021/acs.jmedchem.3c00456.

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