HEC72702
HEC72702 is a potent and orally active hepatitis B virus capsid inhibitor with an EC50 values of 0.039 µM. HEC72702 dose-dependently reduced HBV DNA in both the plasma and livers.
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- CAS. Nr.: 1793063-59-8
- Formel: C24H26BrFN4O5S
- Molecular Weight:581.45
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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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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
EC50: 0.039 µM (hepatitis B virus capsid)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>30 μM
Compound: 58; HEC72702
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Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual-patch-clamp electrophysiology assay
Inhibition of human ERG expressed in HEK293 cells at -80 mV holding potential by manual-patch-clamp electrophysiology assay
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[PMID: 29381358] |
| HepG2 | CC50 |
96.76 μM
Compound: 58; HEC72702
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Cytotoxicity against human HepG2 cells by CellTiter-Blue assay
Cytotoxicity against human HepG2 cells by CellTiter-Blue assay
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[PMID: 29381358] |
Pharmacokinetic Parameters of HEC72702 in Male Sprague-Dawley rats[1].
| dose (mg/kg) | iv (2) | po (5) |
| AUC(0-24 h) (h*ng/mL) | 4110 | 4900 |
| CL (mL/min/kg) | 8.11 | |
| VSS (L/kg) | 0.41 | |
| F % | 47.7 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-7 weeks, 16-18 g, Female BALB/c mice(HDI mouse model)[1]
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Dosage:50, 100 mg/kg
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Administration:P.o.; daily for 7 days
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Result:Demonstrated a dose-dependent reduction of HBV DNA in the plasma of infected mice.
Chemical Information
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CAS. Nr. 1793063-59-8
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Molecular Weight 581.45
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Formel C24H26BrFN4O5S
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SMILES
O=C(O)CC[C@@H]1CN(CC2=C(C(OCC)=O)[C@H](C3=CC=C(F)C=C3Br)N=C(C4=NC=CS4)N2)CCO1
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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
[1]. Ren Q, et al. 3-((R)-4-(((R)-6-(2-Bromo-4-fluorophenyl)-5-(ethoxycarbonyl)-2-(thiazol-2-yl)-3,6-dihydropyrimidin-4-yl)methyl)morpholin-2-yl)propanoic Acid (HEC72702), a Novel Hepatitis B Virus Capsid Inhibitor Based on Clinical Candidate GLS4. J Med Chem. 2018 Feb 8;61(3):1355-1374. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
HEC72702 Related Classifications
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