Obefazimod (Synonyms: ABX464)

Cat. No.: HY-100870 Purity: 99.61%: FAQs
Data Sheet SDS COA Handling Instructions

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Obefazimod (ABX464) is a potent anti-HIV agent. Obefazimod 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.

Obefazimod Chemical Structure

CAS No. : 1258453-75-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 127	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 127	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 115	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 185	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 400	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 640	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 1025	In-stock	Estimated Time of Arrival: December 31
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Biological Activity
Protocol
Purity & Documentation
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Description

IC₅₀ & Target

IC50: 0.1-0.5 μM (HIV-1, in PBMCs)^[1]

In Vitro

Obefazimod inhibits HIV-1 production in PBMC- and macrophages-infected cells. Obefazimod has a strong inhibitory effect for all HIV-1 subtypes tested including subtype B, C and recombinant viruses. Obefazimod 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 Obefazimod. To generalize the effect of Obefazimod on HIV-1 replication in other primary cells, cells are treated with between 0.01 μM up to 30 μM concentrations of Obefazimod and p24 antigen levels are monitored in culture supernatants over a 12 days period. Obefazimod efficiently blocks virus replication in a dose-dependent manner with an IC₅₀ ranging between 0.1 μM and 1 μM^[1].

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

In Vivo

Humanized mice reconstituted with human lymphoid cells provide rapid, reliable, reproducible experimental systems for testing the efficacy of Obefazimod 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 Obefazimod. Measures of viral RNA show that the oral treatment with Obefazimod 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 Obefazimod 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].

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

Clinical Trial

Molecular Weight

338.71

Formula

C₁₆H₁₀ClF₃N₂O

CAS No.

1258453-75-6

Appearance

Solid

Color

White to off-white

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.

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; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 3.75 mg/mL (11.07 mM); Clear solution

This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.61%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (246 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.9524 mL	14.7619 mL	29.5238 mL	73.8095 mL
	5 mM	0.5905 mL	2.9524 mL	5.9048 mL	14.7619 mL
	10 mM	0.2952 mL	1.4762 mL	2.9524 mL	7.3809 mL
	15 mM	0.1968 mL	0.9841 mL	1.9683 mL	4.9206 mL
	20 mM	0.1476 mL	0.7381 mL	1.4762 mL	3.6905 mL
	25 mM	0.1181 mL	0.5905 mL	1.1810 mL	2.9524 mL
	30 mM	0.0984 mL	0.4921 mL	0.9841 mL	2.4603 mL
	40 mM	0.0738 mL	0.3690 mL	0.7381 mL	1.8452 mL
	50 mM	0.0590 mL	0.2952 mL	0.5905 mL	1.4762 mL
	60 mM	0.0492 mL	0.2460 mL	0.4921 mL	1.2302 mL
	80 mM	0.0369 mL	0.1845 mL	0.3690 mL	0.9226 mL
	100 mM	0.0295 mL	0.1476 mL	0.2952 mL	0.7381 mL

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:

Obefazimod1258453-75-6ABX464ABX 464ABX-464Inhibitorinhibitorinhibit

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