2. Vitamin D Related/Nuclear Receptor Cytoskeleton TGF-beta/Smad Stem Cell/Wnt Metabolic Enzyme/Protease JAK/STAT Signaling Epigenetics Protein Tyrosine Kinase/RTK
  3. VD/VDR Collagen TGF-beta/Smad MMP JAK
  4. 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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VDR agonist 4

VDR agonist 4 Chemical Structure

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VDR agonist 4 Related Antibodies

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Description

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[1].

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.

VDR agonist 4 Related Antibodies

Western Blot Analysis[1]

Cell Line: LX-2 cells
Concentration: 0.1 μM
Incubation Time: 24 h
Result: Significantly suppressed the production of α-SMA and collagen I.
Its inhibitory effect was abolished upon VDR depletion.
In Vivo

VDR agonist 4 (500 μg/kg, p.o., five times weekly for 2 weeks) effectively mitigates both inflammatory responses and fibrotic remodeling in CCI4-induced hepatic fibrosis in mice[1].

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

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]
Dosage: 500 μg/kg
Administration: p.o., five times weekly for 2 weeks
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.
Molecular Weight

471.59

Formula

C27H37NO6
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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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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VDR agonist 4 Related Classifications

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  • 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:

VDR agonist 4VDR agonist4VDR agonist-4VD/VDRCollagenTGF-beta/SmadMMPJAKVitamin DVitamin D receptorTransforming growth factor betaMatrix metalloproteinasesJanus kinaseVDRfibrosis-related genesα-SMAcollagen IHSCliver fibrosisInhibitorinhibitorinhibit

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