2. Vitamin D Related/Nuclear Receptor
  3. VD/VDR
  4. VDR agonist 5

VDR agonist 5 是一种口服有效的 VDR 激动剂。VDR agonist 5 可激活 VDR 介导的信号通路以减缓肝纤维化进展。VDR agonist 5 不会诱发高钙血症。VDR agonist 5 可用于肝纤维化的相关研究。

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VDR agonist 5

VDR agonist 5 Chemical Structure

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VDR agonist 5 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

VDR agonist 5 is an oral active VDR agonist. VDR agonist 5 activates VDR-mediated signaling to reduce liver fibrosis progression. VDR agonist 5 does not induce hypercalcemia. VDR agonist 5 can be used for the research of hepatic fibrosis[1].

体外研究
(In Vitro)

VDR agonist 5 (Compound II-8) (0.5 μM) 在人肝星状细胞 LX-2 中发挥 VDR 激动剂作用，可显著上调 VDR 靶基因 CYP24A1 的表达水平[1]。
VDR agonist 5 (0.01-1 μM; 48 h) 可激活 HEK293 细胞中 VDR 介导的转录，在 0.5 μM 时具有显著的反式激活活性，且在 0.01、0.1 和 1 μM 浓度范围内呈现剂量依赖性响应[1]。
VDR agonist 5 (II-8) (0.5 μM; 24 h) 可抑制 TGF-β1 诱导的人肝星状细胞 LX-2 的活化，显著降低促纤维化标志物 α-SMA 和 I 型胶原蛋白的 mRNA 及蛋白表达，且活性可持续至少 48 小时[1]。
VDR agonist 5 (0.5 μM; 24 h) 具有抗纤维化活性，可特异性抑制 TGF-β1 诱导的 LX-2 人肝星状细胞活化，该作用由维生素 D 受体介导，因为敲低 VDR 可显著降低其抑制 α-SMA 和 I 型胶原蛋白表达的能力[1]。

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

VDR agonist 5 相关抗体:

Western Blot Analysis[1]

Cell Line: LX-2 human hepatic stellate cell line activated with TGF-β1
Concentration: 0.5 μM
Incubation Time: 24 h (post-siRNA transfection, alongside TGF-β1 activation)
Result: Significantly reduced TGF-β1-induced upregulation of α-SMA and collagen I protein expression compared to TGF-β1-only treated cells in siNC-transfected cells.
Markedly attenuated the ability to reduce α-SMA and collagen I protein expression in siVDR-transfected cells, with protein levels significantly increased compared to siNC-transfected cells treated with the target reagent and TGF-β1.
体内研究
(In Vivo)

VDR agonist 5 (Compound II-8) (500 μg/kg; p.o.; daily; 7 days) 可显著减轻雄性 C57BL/6 小鼠中 BDL 诱导的肝纤维化并恢复肝功能，且不会诱发高钙血症[1]。

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

Animal Model: C57BL/6 (male, 8 weeks old, BDL-induced hepatic fibrosis)[1]
Dosage: 500 μg/kg
Administration: p.o.; daily; 7 days
Result: Significantly attenuated fibrotic lesions and reduced collagen I deposition (comparable to positive control calcipotriol).
Significantly downregulated hepatic mRNA expression of fibrosis-associated genes Timp-1, Ctgf, and Fn.
Significantly reduced hepatic protein levels of α-SMA, CTGF, and Fibronectin.
Significantly lowered serum levels of ALT, AST, and TBA.
Did not induce hypercalcemia (serum calcium levels remained comparable to control and untreated BDL mice).
分子量

510.66

Formula

C30H42N2O5
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 5 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 5VDR agonist5VDR agonist-5VD/VDRVitamin DVitamin D receptorTGF-β1HEK293 cellscollagen ILX-2 human hepatic stellate cellshepatic stellate cell activationCYP24A1VDRα-SMAliver fibrosisC57BL/6 miceInhibitorinhibitorinhibit

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