2. Anti-infection
  3. HBV
  4. 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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GLPG3808

GLPG3808 Chemical Structure

CAS No. : 2346450-55-1

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GLPG3808 Related Antibodies

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Description

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[1].

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.

GLPG3808 Related Antibodies
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 (0.03-30 mg/kg; p.o.; QD; 28 days) reduces serum HBsAg levels by approximately 1 log unit in HBV-infected humanized FRG mice[1].
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.

Animal Model: HBV-infected FRG
humanized liver
mouse[1]
Dosage: 0.03, 0.1, 3 mg/kg
Administration: p.o; QD;
28 days
Result: Reduced serum HBsAg levels by
approximately 1 log unit.
Animal Model: SD rat (male and female, 10 weeks old, 262-474 g)[1]
Dosage: 0.3 , 1, 2, 3, 6, 20 mg/kg
Administration: p.o.; QD; 91 days
Result: Caused a dose-dependent decrease in tail nerve conduction velocity.
Molecular Weight

475.92

Formula

C24H26ClNO7
CAS No.
SMILES

COCCCOC(C=C1O[C@@H](C2(C)COC2)C(C=C(C(N3C4CC4)=O)C(O)=O)=C3C1=C5)=C5Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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GLPG3808 Related Classifications

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  • Dilution Calculator

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GLPG38082346450-55-1GLPG 3808GLPG-3808HBVHepatitis B virusPAPD7PAPD5HepG2-NTCP cellsSprague-Dawley ratsiCell Hepatocytes 2.0hepatitis B virus infectionInhibitorinhibitorinhibit

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