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

VDR agonist 4 是一种口服有效的强效 VDR 激动剂。VDR agonist 4 通过调节多种纤维化相关基因抑制 α-SMA 和 collagen I 的生成，从而抑制肝星状细胞活化，发挥 VDR 依赖性抗纤维化活性。VDR agonist 4 可改善 CCl4 (HY-RS16594) 诱导的小鼠肝纤维化。VDR agonist 4 可用于肝纤维化相关研究。

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VDR agonist 4

VDR agonist 4 Chemical Structure

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VDR agonist 4 相关抗体

Top Publications Citing Use of Products

查看 MMP 亚型特异性产品:

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8

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JAK1 JAK2 JAK3 Tyk2 JAK

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

VDR agonist 4 (compound B15) (0.1 μM，48 小时) 可下调 LX-2 细胞中 991 个差异表达基因 (DEGs) 的表达，上调 249 个 DEG 的表达，并增加 CYP24A1 的表达[1]。
VDR agonist 4 具有良好的安全性，对 LX-2 细胞无显著细胞毒性 (IC50 > 50 μM)，且 hERG 介导的心脏毒性可忽略不计 (IC50 > 30 μM)[1]。
VDR agonist 4 (0.1 μM，24 小时) 可显著抑制 LX-2 细胞中 COL1A1、ACTA2 和 I 型胶原的表达，而 VDR 耗竭后，这种抑制作用消失，表明其强大的抗纤维化活性严格依赖于 VDR[1]。
VDR agonist 4 (0.1 μM，48 小时) 在 LX-2 细胞中能够下调促纤维化核心通路 (TGFβ/SMAD3、PEGF、JAK) 和胶原合成基因 (COL1A2、COL3A1)，同时上调胶原降解基因 (MMP1、MMP3)，从而证实其具有抑制胶原生成并促进胶原降解的作用[1]。

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

VDR agonist 4 相关抗体:

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.
体内研究
(In Vivo)

VDR agonist 4 (500 μg/kg，口服，每周 5 次，持续 2 周) 可有效缓解 CCI4 诱导的小鼠肝纤维化中的炎症反应和纤维化重构[1]。

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.
分子量

471.59

Formula

C27H37NO6
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

VDR agonist 4 相关分类

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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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