MI891 | PXR antagonist | Probechem Biochemicals

Chemical Structure : MI891

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MI891 (MI-891)

货号: PC-24990Not For Human Use, Lab Use Only.

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生物&药学活性

MI891 is a potent, selective pregnane X receptor (PXR) inverse agonist/antagonist, displays antagonistic activity with an IC50 of 378 nM for rifampicin (1 μM)-activated PXR, binds to the ligand-binding domain (LBD) of PXR.
MI891 exhibits inverse agonistic activity with an IC50 of 6.1 μM and maximal inhibition of 68.8 ± 5.5% at 10 μM.
MI891 also suppresses both rifampicin-induced and basal (constitutive) CYP3A4 mRNA expression in HepaRG cells in a concentration-dependent manner.
MI891 binding (MST, KD=1.7 uM) abrogates PXR LBD coactivation with steroid receptor coactivator 1 (SRC1).
MI891 shows no binding activity on CAR, and no significant agonistic or antagonistic activities of MI891 on human VDR, FXR, LXRβ, LXRα, and PPARα receptors.

物理化学性质&存储条件

分子量	499.30
分子式	C23H14Cl2F2N6O
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	2-chloro-5-((4-(2-(4-chlorophenyl)-6,8-difluoroimidazo[1,2-a]pyridin-3-yl)-1H-1,2,3-triazol-1-yl)methyl)benzamide

参考文献

1. Kamaraj R, et al. J Med Chem. 2025 Jul 12. doi: 10.1021/acs.jmedchem.4c03134.

MI891 (MI-891)

生物&药学活性

物理化学性质&存储条件

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MI891 (MI-891)

生物&药学活性

物理化学性质&存储条件

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