GLPG3808
GLPG3808 is an orally active PAPD5/7 inhibitor. GLPG3808 inhibits the expression of HBcAg in various cells infected with HBV. GLPG3808 reduces the hepatitis B surface antigen levels in HBV-infected animal models. GLPG3808 can be used for the research of hepatitis B virus infection.
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- No. CAS: 2346450-55-1
- Fòrmula: C24H26ClNO7
- Peso molecular:475.92
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
Descripciòn
In Vitro
GLPG3808 (serial dilutions; 6 days post-infection) potently inhibits HBcAg expression in HBV-infected HepG2-NTCP cells with an IC50 of 0.12 nM, with no detectable cytotoxicity at tested concentrations[1].
GLPG3808 (0.25-20 μM) strongly and specifically engages both PAPD5 and PAPD7 proteins in a yeast three-hybrid competition assay, completely inhibiting probe-induced yeast growth at all tested concentrations (0.25-20 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Parmacokinetics
| Species | Dose | Route | CL | CLunbound | Vss | T1/2 | F | AUC0-24 |
|---|---|---|---|---|---|---|---|---|
| Mice[1] | 0.1 mg/kg | i.v. | 0.86 L/h/kg | 3.1 L/h/kg | 2.4 L/kg | 1.9 h | / | / |
| Mice[1] | 5 mg/kg | p.o. | / | / | / | 3.0 h | 68 % | / |
| Rat[1] | 0.1 mg/kg | i.v. | 0.72 L/h/kg | / | 1.4 L/kg | 1.3 h | / | / |
| Rat[1] | 5 mg/kg | p.o. | / | / | / | 4.6 h | 87 % | / |
| Dog[1] | 0.5 mg/kg | i.v. | 0.22 L/h/kg | 0.59 L/h/kg | 1.27 L/kg | 4.0 h | / | / |
| Dog[1] | 5 mg/kg | p.o. | / | / | / | 3.7 h | 46 % | / |
| Mice[1] | 0.03 mg/kg | p.o. | / | / | / | / | / | 6.94 ng·h/mL |
| Mice[1] | 0.1 mg/kg | p.o. | / | / | / | / | / | 23.5 ng·h/mL |
| Mice[1] | 3 mg/kg | p.o. | / | / | / | / | / | 748 ng·h/mL |
In Vivo
GLPG3808 (0.3-20 mg/kg; p.o.; QD; 91 days) causes a dose-dependent decrease in tail nerve conduction velocity in SD rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:
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Dosage:0.03, 0.1, 3 mg/kg
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Administration:p.o; QD;
28 days -
Result:Reduced serum HBsAg levels by
approximately 1 log unit.
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Animal Model:SD rat (male and female, 10 weeks old, 262-474 g)[1]
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Dosage:0.3 , 1, 2, 3, 6, 20 mg/kg
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Administration:p.o.; QD; 91 days
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Result:Caused a dose-dependent decrease in tail nerve conduction velocity.
Chemical Information
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No. CAS 2346450-55-1
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Peso molecular 475.92
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Fòrmula C24H26ClNO7
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SMILES
COCCCOC(C=C1O[C@@H](C2(C)COC2)C(C=C(C(N3C4CC4)=O)C(O)=O)=C3C1=C5)=C5Cl
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
GLPG3808 Related Classifications
HY-181347 Related Classifications
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