| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
IMB-301 targets the interaction between human APOBEC3G (hA3G) and the HIV-1 viral infectivity factor (Vif). hA3G is a host restriction factor that inhibits HIV-1 replication by inducing hypermutation in the viral genome. HIV-1 Vif counteracts this restriction by binding to hA3G and targeting it for degradation. By binding to hA3G and blocking the hA3G-Vif interaction, IMB-301 prevents Vif-mediated degradation of hA3G, restoring its antiviral activity.
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| ln Vitro |
IMB-301 is able to hinder hA3G's degradation by Vif, which leads to hA3G-dependent anti-HIV activity, and hence enhance hA3G's virion encapsidation. IMB-301 attaches itself to hA3G, increases hA3G expression when Vif is present, and hA3G-dependently prevents HIV-1 replication[1].
In vitro, IMB-301 binds to hA3G, restores hA3G expression in the presence of Vif, and inhibits HIV-1 replication in a hA3G-dependent manner. It inhibits HIV-1 replication in H9 cells with an IC50 of 8.63 µM. The compound increases virion encapsidation of hA3G by impairing Vif-mediated degradation. These in vitro activities support its potential as a novel anti-HIV agent that targets the hA3G-Vif interaction. |
| ln Vivo |
In vivo data for IMB-301 is limited in publicly available sources. As a specific HIV-1 replication inhibitor that targets the hA3G-Vif interaction, the compound has potential applications in animal models of HIV-1 infection. By restoring hA3G-mediated restriction, IMB-301 could inhibit viral replication. However, specific published in vivo efficacy studies are not widely reported. IMB-301 is primarily used as a research tool for studying HIV-1 restriction factors.
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| Enzyme Assay |
The in vitro HIV-1 replication inhibition assay for IMB-301 is conducted in H9 cells. Cells are infected with HIV-1 in the presence of varying concentrations of the compound. Viral replication is measured by quantifying viral RNA, p24 antigen, or cytopathic effect. IC50 values are calculated from dose-response curves. The compound's binding to hA3G and inhibition of hA3G-Vif interaction are confirmed by co-immunoprecipitation and Western blotting.
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| Cell Assay |
Cellular assays for IMB-301 are conducted in H9 cells. Cells are infected with HIV-1 and treated with varying concentrations of IMB-301. Viral replication is measured by quantifying viral RNA, p24 antigen, or cytopathic effect. IC50 values are calculated from dose-response curves. hA3G expression and Vif-mediated degradation are assessed by Western blotting. The compound's effects on hA3G-Vif interaction are confirmed by co-immunoprecipitation.
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| Animal Protocol |
In vivo studies for IMB-301 would typically involve animal models of HIV-1 infection. The compound would be administered via oral or intraperitoneal routes at doses determined by pharmacokinetic studies. Efficacy would be assessed by measuring viral loads and CD4+ T cell counts. However, specific published in vivo protocols for IMB-301 are not available in the current literature. The compound is currently used as a research tool for studying HIV-1 restriction factors.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for IMB-301 is not extensively reported in publicly available sources. The compound has a molecular weight of 379.26 g/mol and a molecular formula of C19H17Cl2FN2O. It is soluble in DMSO and has a logP of 5.1. Storage conditions: store at -20°C. As a small molecule HIV-1 inhibitor, it is expected to have moderate bioavailability. Detailed PK parameters such as half-life are not available in the current literature.
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| Toxicity/Toxicokinetics |
Toxicity data for IMB-301 is limited in publicly available sources. As with all research compounds, IMB-301 is intended for research use only and not for human therapeutic applications. Standard in vitro cytotoxicity assays and in vivo tolerability studies would be required for a complete toxicity assessment. Resistance to IMB-301 is primarily mediated by mutations in viral proteins that affect drug binding.
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| References |
[1]. Ma L, et al. Identification of small molecule compounds targeting the interaction of HIV-1 Vif and human APOBEC3G by virtual screening and biological evaluation. Sci Rep. 2018;8(1):8067. Published 2018 May 23.
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| Additional Infomation |
IMB-301 is a specific HIV-1 replication inhibitor that binds to hA3G, blocks hA3G-Vif interaction, and inhibits Vif-mediated hA3G degradation. It inhibits HIV-1 replication in H9 cells with an IC50 of 8.63 µM. By restoring hA3G expression, IMB-301 enables hA3G-dependent anti-HIV activity. The compound has a molecular formula of C19H17Cl2FN2O and a molecular weight of 379.26 g/mol. IMB-301 is a valuable tool for studying HIV-1 restriction factors and developing novel antiviral strategies.
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| Molecular Formula |
C19H17CL2FN2O
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|---|---|
| Molecular Weight |
379.26
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| Exact Mass |
378.07
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| CAS # |
64009-84-3
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| PubChem CID |
327197
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| Appearance |
Colorless to light yellow oil
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| Density |
1.27g/cm3
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| Boiling Point |
548.1ºC at 760mmHg
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| Flash Point |
285.3ºC
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| Index of Refraction |
1.589
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| LogP |
5.581
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
25
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| Complexity |
396
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1=CC=C(OCCC(C2=CC=C(Cl)C=C2Cl)CN2C=CN=C2)C=C1
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| InChi Key |
FHKXBOJPHOEMQO-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H17Cl2FN2O/c20-15-1-6-18(19(21)11-15)14(12-24-9-8-23-13-24)7-10-25-17-4-2-16(22)3-5-17/h1-6,8-9,11,13-14H,7,10,12H2
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| Chemical Name |
1-[2-(2,4-dichlorophenyl)-4-(4-fluorophenoxy)butyl]imidazole
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : 100 mg/mL (263.67 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.59 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (6.59 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.59 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6367 mL | 13.1836 mL | 26.3671 mL | |
| 5 mM | 0.5273 mL | 2.6367 mL | 5.2734 mL | |
| 10 mM | 0.2637 mL | 1.3184 mL | 2.6367 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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