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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Constitutive androstane receptor (CAR)-MI-883
MI-883

Chemical Structure : MI-883

CAS No.: 2530027-71-3

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MI-883 (MI 883, MI883)

货号: PC-23984Not For Human Use, Lab Use Only.

MI-883 is a potent, dual acting constitutive androstane receptor (CAR) agonist/pregnane X receptor (PXR) antagonist with EC50 of 73 nM in TR-FRET CAR coactivation assays, competes with fluorophore binding to recombinant PXR LBD with IC50 of 0.1 uM.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MI-883 is a potent, dual acting constitutive androstane receptor (CAR) agonist/pregnane X receptor (PXR) antagonist with EC50 of 73 nM in TR-FRET CAR coactivation assays, competes with fluorophore binding to recombinant PXR LBD with IC50 of 0.1 uM.
MI-883 significantly stimulates CAR LBD assembly (EC50=0.38 uM), CAR3 variant activationand the translocation of EGFR-CAR+A hybrid protein into nucleus, which is an initial step of CAR activation.
MI-883 significantly upregulates CYP2B6 mRNA in HepaRG and primary human hepatocytes (PHH), but not in HepaRG KO CAR cells with ablated CAR expression.
MI-883 significantly suppresses both basal and rifampicin-induced PXR activation in HepG2 cells with IC50 of 2.03 uM and 3.60 uM respectively in transient transfection luciferase reporter assays.
MI-883 induces significant CYP3A4 mRNA downregulation, pER6-luc luciferase construct inhibition below the control (basal) expression, and significant suppression of PXR ligand activity in LS174T cells.
MI-883 effectively regulates genes related to xenobiotic metabolism and cholesterol/bile acid homeostasis by leveraging CAR and PXR interactions in gene regulation.
MI-883 significantly reduces plasma cholesterol levels and enhances fecal bile acid excretion in humanized PXR-CAR-CYP3A4/3A7 mice fed high-fat and high-cholesterol diets.

物理化学性质&存储条件

分子量 481.31
分子式 C23H15Cl2FN6O
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)-7-fluoroimidazo[1,2-a]pyridin-3-yl)-1H-1,2,3-triazol-1-yl)methyl)benzamide

参考文献

1. Dusek J, et al. Nat Commun. 2025 Feb 6;16(1):1418.

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