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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- 分子式: C27H37NO6
- 分子量:471.59
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
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.
化学情報
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分子量 471.59
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
VDR agonist 4 関連分類
HY-178328 関連分類
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