VDR agonist 4
VDR agonist 4 is an orally active potent VDR agonist. VDR agonist 4 exerts VDR-dependent antifibrotic activity by regulating multiple fibrosis-related genes to suppress α-SMA and collagen I production, thereby inhibiting hepatic stellate cell (HSC) activation. VDR agonist 4 improves CCl4 (HY-RS16594)-induced hepatic fibrosis in mice. VDR agonist 4 can be used for liver fibrosis research.
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- No. CAS: 3136765-61-9
- Fòrmula: C27H37NO6
- Peso molecular:471.59
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Actividad biológica
Descripciòn
In Vitro
VDR agonist 4 (compound B15) (0.1 μM, 48 h) downregulates 991 differentially expressed genes (DEGs) and upregulates 249 DEGs in LX-2 cells, and increases the expression of CYP24A1[1].
VDR agonist 4 presents a favorable safety profile, with no significant cytotoxicity in LX-2 cells (IC50 > 50 μM) and negligible hERG-mediated cardiotoxicity (IC50 > 30 μM)[1].
VDR agonist 4 (0.1 μM, 24 h) significantly inhibits the expression of COL1A1, ACTA2, and collagen I in LX-2 cells, while this inhibitory effect is abolished upon VDR depletion, thereby demonstrating that its potent antifibrotic activity is strictly VDR-dependent[1].
VDR agonist 4 (0.1 μM, 48 h) downregulates core fibrogenic pathways (TGFβ/SMAD3, PEGF, JAK) and collagen synthesis genes (COL1A2, COL3A1) in LX-2 cells, while upregulating collagen degradation genes (MMP1, MMP3), thereby demonstrating the suppression of collagen production and promotion of its breakdown[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LX-2 cells
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Concentration:0.1 μM
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Incubation Time:24 h
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Result:Significantly suppressed the production of α-SMA and collagen I.
Its inhibitory effect was abolished upon VDR depletion.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6 mice (8 weeks old) intraperitoneally injected with CCl4/corn oil (1/50, v/v) mixture at a dose of 0.5 mL/kg three times a week for 4 weeks[1]
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Dosage:500 μg/kg
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Administration:p.o., five times weekly for 2 weeks
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Result:Exhibited potent inhibitory effects on target gene expression (Fn, Ctgf, Timp-1), with efficacy comparable to Calcipotriol (HY-10001).
Resulted in marked attenuation of hepatic inflammation and significant amelioration of fibrotic lesions, as evidenced by reduced inflammatory markers and collagen accumulation.
Resulted in a significant decrease in ALT, AST, and TBA levels.
Did not result in increased serum calcium levels.
Chemical Information
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No. CAS 3136765-61-9
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Peso molecular 471.59
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Fòrmula C27H37NO6
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SMILES
CCN(C(CCCCCOC1=CC2=CC=C(C=C2C=C1)OCC3=C[C@H]([C@H]([C@@H](C3)O)O)O)=O)CC
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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)
VDR agonist 4 Related Classifications
HY-178328 Related Classifications
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