2. GPCR/G Protein TGF-beta/Smad Metabolic Enzyme/Protease
  3. G protein-coupled Bile Acid Receptor 1 TGF-β Receptor MMP
  4. 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.

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LIFR/GPBAR1 modulator 1

LIFR/GPBAR1 modulator 1 Chemical Structure

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LIFR/GPBAR1 modulator 1 Related Antibodies

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Description

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].

IC50 & Target

MMP9

 

In Vitro

LIFR/GPBAR1 modulator 1 (Compound 2o) (0.1-50 μM) shows an inhibitory efficiency of 89.6 % on LIFR at a concentration of 10 μM in HepG2 cells (IC50 = 7.9 μM). In HEK293T cells, it shows an activation efficiency of 79.4 % on GPBAR1 at 10 μM (EC50 = 0.2 μM)[1].
LIFR/GPBAR1 modulator 1 (1–10 μM, 24 h) regulates the expression of fibrosis-related genes in a concentration-dependent manner, in leukaemia inhibitory factor (LIF)-mediated human hepatic stellate cells (HSC) LX2. At a concentration of 10 μM, it upregulates the mRNA expression of LIFR and GPBAR1 and significantly reduces the expression of pro-fibrosis markers (COL1A1, ASMA, and TGFβ). Simultaneously, it reduces TIMP1 expression and increases MMP9 expression, indicating that it promotes ECM degradation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

LIFR/GPBAR1 modulator 1 Related Antibodies

Real Time qPCR[1]

Cell Line: Leukaemia inhibitory factor (LIF)-mediated human HSC LX2
Concentration: 1 μM, 5 μM, 10 μM
Incubation Time: 24 h
Result: Upregulated the mRNA expression of LIFR and GPBAR1 and significantly reduced the expression of pro-fibrosis markers (COL1A1, ASMA, and TGFβ).
Reduced TIMP1 expression and increased MMP9 expression.
In Vivo

LIFR/GPBAR1 modulator 1 (Compound 2o) (10 mg/kg, p.o., once daily for 7 days) can effectively reverse Carbon tetrachloride (HY-Y0298) (CCl4)-induced acute liver fibrosis in mice, specifically by reducing hepatocyte damage, inhibiting inflammatory responses, reducing extracellular matrix (ECM) deposition, and downregulating the expression of pro-fibrotic genes[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Liver fibrosis was induced by intraperitoneal (i.p.) administration of carbon tetrachloride (CCl4) at a dose of 500 μL/kg, dissolved in an equal volume of olive oil, and administered twice per week for 1 week to Male C57BL/6J mice[1].
Dosage: 10 mg/kg
Administration: P.o., once daily for 7 days
Result: Reduced weight loss.
Significantly reduced plasma levels of AST, ALT, bilirubin, and LDH.
Reduced CCl4-induced white blood cell (WBC) count elevation and modulated the percentages of neutrophils, lymphocytes, and monocytes.
Improved hepatocellular necrosis and inflammatory infiltration and significantly reduced collagen deposition and fibrosis area.
Significantly downregulated the mRNA expression of fibrosis marker genes (Colla1, aSma, Tgβ) in liver tissue.
Molecular Weight

461.59

Formula

C32H31NO2
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LIFR/GPBAR1 modulator 1 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LIFR/GPBAR1 modulator 1G protein-coupled Bile Acid Receptor 1TGF-β ReceptorMMPG-protein coupled receptor 19GPCR19TGR5GPBAR1Transforming growth factor beta receptorsMatrix metalloproteinasesLIFRLiver fibrosisHepatic stellate cellsHSCInhibitorinhibitorinhibit

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