MI891
MI891 is a highly selective PXR antagonist (IC50 = 3.76 μM, Kd = 1.7 μM) and inverse agonist (IC50 = 6.1 μM). MI891 selectively disrupts the interaction between PXR and its coactivator SRC1. MI891 effectively inhibits Rifampicin (HY-B0272)-induced PXR activation. MI891 is useful for the study of metabolic diseases and other diseases.
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- Pureté: 99.90%
- CAS No.: 2530027-77-9
- Formule: C23H14Cl2F2N6O
- Masse moléculaire:499.30
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Stockage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
MI891 (0-10 μM) abrogates PXR activation by Rifampicin (HY-B0272) and displays antagonistic activity with an IC50 of 378 nM[1].
MI891 (0-20 μM, 48 h) suppresses both rifampicin-induced and basal (constitutive) CYP3A4 mRNA expression in HepaRG cells[1].
MI891 (1-10 μM) disrupts the wt-PXR-LBD/SRC1-VP16 interaction, does not activate the obstructed mutated PXR LBD in wild-type (wt-PXR LBD) or triple mutant (S208W/S247W/C284W) in HepG2 cells[1].
MI891 (48 h) shows no binding activity (EC50 > 10 μM) in wild-type CAR; requires high concentrations to activate CAR (EC50 = 137 μM) and has no significant activation of either CARwt or CAR3 variant in human CARwt and CAR3 in HepG2 cells[1].
MI891 (10 μM, 48 h) exhibits selective antagonism and inverse agonism on hPXR, but has no agonistic or antagonistic activities of MI891 on human VDR, FXR, LXRβ, LXRα, PPARα, PPARγ, AhR, or ERα/β receptors[1].
MI891 (24 h) demonstrates no effects on viability in various cell lines (up to 30 μM), including COS-1, HepG2, and HK-2[1].
MI891 (5-10 μM, 48 h) suppresses the expression of CYP3A4, CYP7A1, HMGCS2, PCK1, and MKI67 mRNA in primary human hepatocytes[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 2530027-77-9
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Appearance Solid
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Masse moléculaire 499.30
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Formule C23H14Cl2F2N6O
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Color White to off-white
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SMILES
O=C(N)C1=CC(CN2N=NC(C3=C(C4=CC=C(Cl)C=C4)N=C5C(F)=CC(F)=CN53)=C2)=CC=C1Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Pureté et documentation
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Fiche technique (273 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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