Obefazimod
Based on 1 Customer Validation
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.
- Purity: 99.85%
- CAS No.: 1258453-75-6
- Formula: C16H10ClF3N2O
- Molecular Weight:338.71
-
Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocol
- Purity & Documentation
- References
-
Help & FAQs
-
Orally Active Compound Library
HY-L061
-
Heterocyclic Compound Library
HY-L138
-
Highly Selective Inhibitors Library
HY-L158
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
High-Throughput Bioactive Compound Library
HY-L205
-
Anti-Infection Compound Library
HY-L002
-
Clinical Compound Library
HY-L026
-
Antiviral Compound Library
HY-L027
-
Drug Repurposing Compound Library
HY-L035
Biological Activity
|
HIV-1 0.1-0.5 μM (IC50, in PBMCs) |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 1258453-75-6
-
Appearance Solid
-
Molecular Weight 338.71
-
Formula C16H10ClF3N2O
-
Color White to off-white
-
SMILES
FC(F)(F)OC1=CC=C(NC2=NC3=C(Cl)C=CC=C3C=C2)C=C1
-
Synonyms
ABX464
-
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
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
-
Data Sheet (273 KB)
-
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
-
Handling Instructions (2659 KB)
References
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.
| 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 |
Obefazimod Related Classifications
HY-100870 Related Classifications
Powered by Bioz