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.
For research use only. We do not sell to patients.
- Formula: C30H42N2O5
- Molecular Weight:510.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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Cell Line:LX-2 human hepatic stellate cell line activated with TGF-β1
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Concentration:0.5 μM
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Incubation Time:24 h (post-siRNA transfection, alongside TGF-β1 activation)
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (male, 8 weeks old, BDL-induced hepatic fibrosis)[1]
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Dosage:500 μg/kg
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Administration:p.o.; daily; 7 days
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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).
Chemical Information
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Molecular Weight 510.66
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Formula C30H42N2O5
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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
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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