Constitutive Androstane Receptor Agonist

MI-883 is orally active constitutive androstane receptor (CAR) (EC₅₀ of 73 nM) agonist and pregnane X Receptor (PXR) (IC₅₀ of 100 nM) antagonist. MI-883 binds to CAR and PXR ligand-binding domains, promotes CAR LBD assembly, activates CAR3 variant, stimulates CAR cytoplasmic-nuclear translocation, upregulates CAR target genes, recruits coactivators NCOA1, NCOA2, NCOA3, inhibits basal and agonist-induced PXR activation, downregulates PXR target genes, disrupts PXR-NCOR2 interaction, blocks agonist-mediated PXR-NCOA1 recruitment. MI-883 reduces plasma total cholesterol, LDL cholesterol, and hepatic free cholesterol levels, increases fecal bile acid excretion, regulates genes involved in xenobiotic metabolism, cholesterol homeostasis, and bile acid homeostasis. MI-883 exhibits metabolic stability, liver-predominant distribution, a safety profile with no observed toxicity, and does not stimulate human hepatocyte hypertrophy or hyperplasia. MI-883 can be used for the research of diet-induced hypercholesterolemia.

Isobutylparaben (Isobutyl 4-hydroxybenzoate) is the agonist for PXR, CAR and PPAR. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics.

Z-CITCO is the cis isomer of CITCO (HY-103244). Z-CITCO is an agonist of constitutive androstane receptor (CAR) with an EC₅₀ value of 3.9 µM.

Isobutylparaben (Standard) is the analytical standard of Isobutylparaben. This product is intended for research and analytical applications. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is the agonist for PXR, CAR and PPAR. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics.

DL5050 is a selective and potent human constitutive androstane receptor (hCAR) agonist that does not activate pregnane X receptor (PXR). DL5050 preferentially induces the expression of CYP2B6 (target of hCAR) over CYP3A4 (target of hPXR) on both the mRNA and protein levels. DL5050 can be used for the researches of cancer and metabolic disease, such as diabetes.

Isobutylparaben-d₄ is the deuterium labeled Isobutylparaben. Isobutylparaben (Isobutyl 4-hydroxybenzoate) is the agonist for PXR, CAR and PPAR. Isobutylparaben has a broad-spectrum antimicrobial activity and widely used in personal care products and cosmetics.

DL5055 (compound 6k) is a potent and selective hCAR activator with an EC₅₀ of 0.35 μM. DL5055 induces CYP2B6 expression and hCAR nuclear translocation in human primary hepatocytes.