Chemical Structure : MI891
CAS No.:
2530027-77-9
MI891
(MI-891)
Catalog No.: PC-24990Not For Human Use, Lab Use Only.
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.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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499.30
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Formula
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C23H14Cl2F2N6O
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Kamaraj R, et al. J Med Chem. 2025 Jul 12. doi: 10.1021/acs.jmedchem.4c03134.
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