MI891
Based on 1 Customer Validation
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 99.90%
- No. CAS: 2530027-77-9
- Fòrmula: C23H14Cl2F2N6O
- Peso molecular:499.30
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Almacenamiento:
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)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Actividad biológica
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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No. CAS 2530027-77-9
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Appearance Solid
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Peso molecular 499.30
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Fòrmula 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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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
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)
Solvente y solubilidad
DMSO : 4.55 mg/mL (9.11 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (277 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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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0028 mL | 10.0140 mL | 20.0280 mL | 50.0701 mL |
| 5 mM | 0.4006 mL | 2.0028 mL | 4.0056 mL | 10.0140 mL |
MI891 Related Classifications
HY-175264 Related Classifications
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