2. Anti-infection
  3. HBV
  4. CAB7-3

CAB7-3 is an orally active HBV capsid assembly modulator (CAM). CAB7-3 exhibits an exceptional antiviral efficacy reducing HBV DNA with an EC50 = 70 nM, CC50 = 32.3 μM in HepDES19 cells. CAB7-3 exhibits significant anti-HBV activity in HBV-integrated HepDES19 (EC50 = 70 nM), HepAD38 (EC50 = 1 nM) and HBV-infected HLCZ01 cells (EC50 = 2 nM), respectively. CAB7-3 effectively reduces Hepatic HBV core protein levels and suppresses viral replication in vivo. CAB7-3 demonstrates a favorable drug-like and safety profile. CAB7-3 can be used for Hepatitis B Virus (HBV) research.

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CAB7-3

CAB7-3 Chemical Structure

CAS No. : 3014372-17-6

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CAB7-3 Related Antibodies

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Description

CAB7-3 is an orally active HBV capsid assembly modulator (CAM). CAB7-3 exhibits an exceptional antiviral efficacy reducing HBV DNA with an EC50 = 70 nM, CC50 = 32.3 μM in HepDES19 cells. CAB7-3 exhibits significant anti-HBV activity in HBV-integrated HepDES19 (EC50 = 70 nM), HepAD38 (EC50 = 1 nM) and HBV-infected HLCZ01 cells (EC50 = 2 nM), respectively. CAB7-3 effectively reduces Hepatic HBV core protein levels and suppresses viral replication in vivo. CAB7-3 demonstrates a favorable drug-like and safety profile. CAB7-3 can be used for Hepatitis B Virus (HBV) research[1].

In Vitro

CAB7-3 (0.001-1 μM, 6 days) shows an antiviral activity in HepAD38 cells with EC50 = 1 nM, CC50 = 26.54 μM, SI = 26540; in HepDES19 cells with EC50 = 7 nM, CC50 = 32 μM, SI = 481; in HBV-infected HLCZ01 cells with EC50 = 2 nM, CC50 = 30.73 μM, SI = 15365[1].
CAB7-3 (0.0003-1 μM, 6 days) blocks new cccDNA formation while leaving HBsAg secretion from pre-existing cccDNA unaffected in HepAD38 and HLCZ01 cells[1].
CAB7-3 (0.006-4 μM, 3 days ) induces HBV Cp degradation and disrupts capsid assembly in HepG2 cells[1].
CAB7-3 (1 mg in 1 mL DMSO and 0.5 mg in 0.5 mL DMSO) shows water solubility (257.42 μg/mL, pH 2.0; 2.57 μg/mL, pH 7.0; 4.14 μg/mL, pH 7.4)[1].
CAB7-3 (1 μM, 0-60 min) shows T1/2 = 169 min, CLint(mic) = 8.2 μL/min/mg, CLint(liver) = 7.4 mL/min/kg and Remaining (T = 60 min) = 78.0% in human microsomes CAB7-3 (10 μM, ) not induce CYP3A4 in primary human hepatocytes (PHHs) [1].
CAB7-3 (0.3-100 μM) exhibits significantly low inhibitory rates on the hERG channel in HEK293 cells with hERG inhibition = 3.52, 14.59, 31.84, 61.05, 83.05, 94.76 % at concentration of 0.3, 1, 3, 10, 30 and 100 μM[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

CAB7-3 Related Antibodies

ELISA Assay[1]

Cell Line: HepAD38 and HLCZ01 cells
Concentration: 0.0003, 0.001, 0.003, 0.1, 0.03, 0.1 and 0.3 μM
Incubation Time: 6 days
Result: Had minimal impact on the production of HBsAg in both HepAD38 cells and HLCZ01 cells.

Western Blot Analysis[1]

Cell Line: HepG2 cells
Concentration: 0.06, 0.13, 0.25, 0.5, 1.0, 2.0, 4.0 μM
Incubation Time: 3 days
Result: Reduced intracellular Cp expression in a dose-dependent manner.
Parmacokinetics
Species Dose Route T1/2 Tmax Cmax AUC0-t AUC0-∞ MRT0-t MRT0-∞ F C0 Vz CL
Mice[1] 10 mg/kg p.o. 0.66 h 0.33 h 317.02 ng/mL 352.24 ng·h/mL 376.68 ng·h/mL 0.81 h 1 h 10.42 % / / /
Mice[1] 2 mg/kg i.v. 1.95 h 0.08 h 0533 ng/mL 720 ng·h/mL 723 ng·h/mL 0.54 h 0.57 h / 2159 ng/mL 4699 mL/kg 2806 mL/h/kg
In Vivo

CAB7-3 (15 mg/kg, p.o., once daily for 18 days) inhibits the secretion of viral DNA containing particles by repressing HBV capsid assembly in the HBV carrier mouse model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: pAAVHBV1.2 plasmid (6 μg, hydrodynamic injection ) induced-male C57BL/6J (6 weeks)[1]
Dosage: 15 mg/kg
Administration: p.o., once daily for 18 days
Result: Significantly reduced serum HBV DNA levels from the vehicle baseline of 1.02 × 105 IU/mL to 1.06 × 104 IU/mL.
Displayed enhanced anti-HBV activity, reducing hepatic HBcAg expression despite not noticeably affecting serum HBsAg expression.
Showed no significant change in the Serum ALT and AST levels, as well as HE staining of liver tissue.
Molecular Weight

656.33

Formula

C28H28BBrFN5O5S
CAS No.
SMILES

FC1=CC(Br)=C(C=C1)[C@H]2C(C(OCC)=O)=C(NC(C3=NC=CS3)=N2)CN4[C@H](CCC4)C(NC5=CC=C(C=C5)B(O)O)=O
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Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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CAB7-3 Related Classifications

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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:

CAB7-33014372-17-6HBVHepatitis B viruscapsid assembly modulatorviral replicationHepatitis B VirusInhibitorinhibitorinhibit

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