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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- Fòrmula: C32H31NO2
- Peso molecular:461.59
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
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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.
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Cell Line:Leukaemia inhibitory factor (LIF)-mediated human HSC LX2
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Concentration:1 μM, 5 μM, 10 μM
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Incubation Time:24 h
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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.
Parmacokinetics
| Species | Dose | Route | T1/2 | Cmax | Tmax | AUC0-t |
|---|---|---|---|---|---|---|
| Mice | 10 mg/kg | p.o. | 1.6 h | 37.63 ng/mL | 1 h | 113.69 ng·h/mL |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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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].
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Dosage:10 mg/kg
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Administration:P.o., once daily for 7 days
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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.
Chemical Information
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Peso molecular 461.59
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Fòrmula C32H31NO2
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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
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
LIFR/GPBAR1 modulator 1 Related Classifications
HY-178477 Related Classifications
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