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

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.

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VDR agonist 5

VDR agonist 5 Chemical Structure

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VDR agonist 5 Related Antibodies

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Description

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].

In Vitro

The VDR agonist 5 (Compound II-8) (0.5 μM) acts as a VDR agonist in human hepatic stellate cell line LX-2, and significantly upregulates the expression level of the VDR target gene CYP24A1[1].
VDR agonist 5 (0.01-1 μM; 48 h) activates VDR-mediated transcription in HEK293 cells, exhibits significant transactivation activity at 0.5 μM, and shows a dose-dependent response within the concentration range of 0.01, 0.1 and 1 μM[1].
The VDR agonist 5 (II-8) (0.5 μM; 24 h) inhibits TGF-β1-induced activation of human hepatic stellate cell line LX-2, significantly reduces the mRNA and protein expression levels of pro-fibrotic markers α-SMA and type I collagen, and its activity persists for at least 48 hours[1].
The VDR agonist 5 (0.5 μM; 24 h) exhibits antifibrotic activity and specifically inhibits TGF-β1-induced activation of LX-2 human hepatic stellate cells. This effect is mediated by the vitamin D receptor, as VDR knockdown significantly impairs its ability to suppress the expression of α-SMA and type I collagen[1].

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

VDR agonist 5 Related Antibodies

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.
In Vivo

VDR agonist 5 (Compound II-8) (500 μg/kg; p.o.; daily; 7 days) significantly attenuates BDL-induced hepatic fibrosis and restores liver function in male C57BL/6 mice without inducing hypercalcemia[1].

MedChemExpress (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).
Molecular Weight

510.66

Formula

C30H42N2O5
SMILES

O=C(C1=CC2=C(C=C1)C(C(CC)(C3=CC=C(OCC(O)CO)C=C3)CC)=CN2CC)NC(C(C)C)CO
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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VDR agonist 5 Related Classifications

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Help & FAQs
  • 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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