1. Anti-infection
  2. HIV
  3. ABX464

ABX464 

Cat. No.: HY-100870 Purity: 99.81%
Handling Instructions

ABX464 is a potent anti-HIV agent. ABX464 inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) with an IC50 ranging between 0.1 μM and 0.5 μM.

For research use only. We do not sell to patients.

ABX464 Chemical Structure

ABX464 Chemical Structure

CAS No. : 1258453-75-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 261 In-stock
Estimated Time of Arrival: December 31
1 mg USD 150 In-stock
Estimated Time of Arrival: December 31
5 mg USD 350 In-stock
Estimated Time of Arrival: December 31
10 mg USD 550 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1100 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1600 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

ABX464 is a potent anti-HIV agent. ABX464 inhibits HIV-1 replication in stimulated peripheral blood mononuclear cells (PBMCs) with an IC50 ranging between 0.1 μM and 0.5 μM.

IC50 & Target[1]

HIV-1

0.1-0.5 μM (IC50, in PBMCs)

In Vitro

ABX464 inhibits HIV-1 production in PBMC- and macrophages-infected cells. ABX464 has a strong inhibitory effect for all HIV-1 subtypes tested including subtype B, C and recombinant viruses. ABX464 also very efficiently inhibits the replication of viral strains harbouring mutations that confer resistance to different therapeutic agents in vitro. While the antiviral drug 3TC is not highly active on K65R and M184V mutant strains, both strains are inhibited by ABX464. To generalize the effect of ABX464 on HIV-1 replication in other primary cells, cells are treated with between 0.01 μM up to 30 μM concentrations of ABX464 and p24 antigen levels are monitored in culture supernatants over a 12 days period. ABX464 efficiently blocks virus replication in a dose-dependent manner with an IC50 ranging between 0.1 μM and 1 μM[1].

In Vivo

Humanized mice reconstituted with human lymphoid cells provide rapid, reliable, reproducible experimental systems for testing the efficacy of ABX464 in vivo. In the initial setting, SCID mice are reconstituted with PBMCs and then infected with the HIV-1 strain JR-CSF. Mice are treated twice a day (b.i.d) for 15 days by oral gavage with 20 mg/kg of ABX464. Measures of viral RNA show that the oral treatment with ABX464 is able to significantly reduce the viral load over a period of 15 days of treatment. FACS analysis of blood samples show that treatment with ABX464 prevents depletion of CD4+ cells following infection of reconstituted mice and thereby restores the CD8+/CD4+ ratio back to that of non-infected mice[1].

Clinical Trial
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (295.24 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9524 mL 14.7619 mL 29.5238 mL
5 mM 0.5905 mL 2.9524 mL 5.9048 mL
10 mM 0.2952 mL 1.4762 mL 2.9524 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.75 mg/mL (11.07 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 3.75 mg/mL (11.07 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Cell Assay
[1]

The concentration of ABX464 with minimal side effects on cell viability is determined using an MTS test. PBMCs are treated with ABX464 (2, 4, 8, 16, 31, 63, 125, and 250 μM). Cell viability is measured by MTS assay after 6 days of incubation and cytotoxicity is indicated as percentage as compared with untreated cells[1].

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

Animal Administration
[1]

Mice[1]
SCID mice are reconstituted with fresh human PBMCs for two weeks and the reconstitution rates are estimated by human IgG titration. Reconstituted SCID mice are infected with JRCSF HIV-1 strain by intraperitoneal injection. Control group receive labrafil and 5% DMSO by gavage (n=15) and the treated group receive 20 mg/kg b.i.d of ABX464 (n=14) for 15 days[1].

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

References
Molecular Weight

338.71

Formula

C₁₆H₁₀ClF₃N₂O

CAS No.

1258453-75-6

SMILES

FC(F)(F)OC1=CC=C(NC2=NC3=C(Cl)C=CC=C3C=C2)C=C1

Shipping

Room temperature in continental US; may vary elsewhere

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Cat. No.: HY-100870