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LIFR/GPBAR1 modulator 1

LIFR/GPBAR1 modulator 1 is an orally active, potent GPBAR1 agonist (EC50 = 0.2 μM) and LIFR inhibitor (IC50 = 7.9 μM) . LIFR/GPBAR1 modulator 1 upregulates leukaemia inhibitory factor (LIF) -mediated mRNA expression of LIFR and GPBAR1 and significantly reduces the expression of pro-fibrosis markers (COL1A1, ASMA, and TGFβ), and reduces TIMP1 expression and increases MMP9 expression. LIFR/GPBAR1 modulator 1 can be used for the study of human fibrotic disorders[1].

Product Specifications

UNSPSC

12352005

Target

G protein-coupled Bile Acid Receptor 1; MMP; TGF-β Receptor

Related Pathways

GPCR/G Protein; Metabolic Enzyme/Protease; TGF-beta/Smad

Field of Research

Metabolic Disease; Inflammation/Immunology

Smiles

CC1=CC=C(C#N)C=C1C2=CC=C([C@@H]3C([C@]4([H])[C@@](CCC5=O)([H])[C@]5(C)C3)=C(CC6)C(CC4)=CC6=O)C=C2

Molecular Formula

C32H31NO2

Molecular Weight

461.59

References & Citations

[1]De Gregorio R, et al. Harnessing the Estradienone Scaffold to Develop Dual GPBAR1 and LIFR Modulators for Liver Fibrosis. J Med Chem. 2025 Oct 9;68 (19) :20037-20059.

Shipping Conditions

Room temperature

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Isoform

MMP-9

Curated Selection

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