BZZ-034
BZZ-034 is an orally active and selective PXR dual agonist with an IC50 of 0.47 μM against human PXR. BZZ-034 binds to the PXR ligand-binding domain, activates PXR-mediated transcription, and upregulates the expression of downstream CYP3A4/Cyp3a11 and Oatp2 target genes. BZZ-034 induces physiological hepatomegaly, centrilobular hepatocellular hypertrophy, and periportal hepatocellular proliferation, and accelerates liver regeneration after partial hepatectomy. BZZ-034 can be used for research on liver regeneration.
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- CAS. Nr.: 3116532-77-2
- Formel: C21H25NO6
- Molecular Weight:387.43
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
CYP3A4 |
In Vitro
BZZ-034 (10 μM) activates hPXR-driven CYP3A4 transcription in HepG2 cells with an EC50 of 1.5 μM and 86% agonist activity at 10 μM; it also induces CYP3A4 mRNA 2.18-fold in HepG2 cells[1].
BZZ-034 (10 μM; 24 h) activates hPXR LBD in HEK293T cells, with an agonistic activity of 130% at 10 μM[1].
BZZ-034 (1-10 μM) induces Cyp3a11 and Oatp2 mRNA by 12.0-fold and 6.84-fold, respectively, in mouse primary hepatocytes[1].
BZZ-034 is rapidly metabolized in human and mouse liver microsomes, with T1/2 of 12.5 min and 1.98 min, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
In Vivo
BZZ-034 (50 mg/kg; p.o.; twice daily; 2 days) accelerates liver regeneration in mice undergoing 70% partial hepatectomy (70% PHx), increases the liver/body weight ratio, and promotes regional hepatocyte hypertrophy and proliferation[1].
BZZ-034 (12.5-100 mg/kg; p.o.; twice daily; 2 days) dose-dependently promotes liver regeneration in mice subjected to 70% PHx[1].
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, 6-8 weeks old)[1]
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Dosage:12.5, 25, 50, and 100 mg/kg
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Administration:p.o.; twice daily; 2 days
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Result:Produced dose‑dependent increases in liver size and liver/body weight ratio, yielding 4.2%, 11.9%, 18.0%, and 23.8% elevations at respective doses of 12.5, 25, 50, and 100 mg/kg.
Increased hepatocyte size within the central vein area and the population of Ki67‑positive cells within the portal vein area in a dose‑dependent manner.
Upregulated CYP3A11 protein expression in a dose‑dependent fashion.
Chemical Information
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CAS. Nr. 3116532-77-2
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Molecular Weight 387.43
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Formel C21H25NO6
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SMILES
COC(C=CC(C1=CC2=C(C=C1C(NCC(C)C)=O)OCO2)=C3OC)=C3OC
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Versand
Room temperature in continental US; may vary elsewhere.
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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)
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