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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Formel: C30H42N2O5
- Molecular Weight:510.66
-
Speicherung:
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
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
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.
-
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.
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).
Chemical Information
-
Molecular Weight 510.66
-
Formel 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
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
VDR agonist 5 Related Classifications
HY-181486 Related Classifications
Powered by Bioz