| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 100mg | |||
| 250mg | |||
| Other Sizes |
| Targets |
CX04328 targets the interaction between LEDGF/p75 (lens epithelium-derived growth factor) and HIV-1 integrase (IN). By binding to the integrase enzyme, it inhibits the protein-protein interaction, preventing the integration of the viral genome into the host chromosome. This allosteric mechanism of action is distinct from the active site inhibitors of integrase. In a cell-free assay, it exhibits an IC50 of 1.37 µM for inhibiting the LEDGF/p75-IN interaction.
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| ln Vitro |
In vitro, CX04328 functions as an allosteric inhibitor of HIV-1 integrase. It inhibits the LEDGF/p75-integrase interaction with an IC50 of 1.37 µM and shows antiviral activity with an EC50 of 2.35 µM. As a quinoline-based LEDGIN, it binds to the integrase enzyme at a site distinct from the active site, disrupting the functional interaction with LEDGF/p75 and impairing viral replication.
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| ln Vivo |
No specific in vivo activity data is publicly available for CX04328. As a research compound for HIV-1 inhibition, its in vivo efficacy, particularly in animal models of HIV-1 infection, has not been extensively reported. Further studies would be needed to establish its in vivo activity and potential as a therapeutic agent.
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| Enzyme Assay |
In cell-free enzymatic or receptor binding assays, CX04328's activity is evaluated by measuring its inhibition of the LEDGF/p75-IN protein-protein interaction. The assay typically involves incubating purified HIV-1 integrase protein with a LEDGF/p75-derived peptide in the presence of varying concentrations of the compound. The interaction is detected using techniques such as fluorescence polarization, AlphaScreen, or ELISA. The IC50 is calculated from the inhibition curve.
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| Cell Assay |
In vitro cell-based experiments with CX04328 typically involve HIV-1-infected cell lines, such as MT-4 or HeLa cells. Cells are infected with HIV-1 and treated with various concentrations of the compound. Viral replication is assessed by measuring the production of viral proteins (e.g., p24 antigen) or by quantifying viral RNA. The antiviral activity (EC50) is determined from the concentration-response curve.
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| Animal Protocol |
No specific in vivo animal protocols are publicly available for CX04328. If in vivo studies were to be conducted, typical protocols would involve HIV-1-infected humanized mouse models, where the compound would be administered orally or intraperitoneally, and viral load and CD4+ T cell counts would be monitored.
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| ADME/Pharmacokinetics |
No detailed pharmacokinetic data is publicly available for CX04328. As a research compound, its absorption, distribution, metabolism, and excretion (ADME) properties have not been extensively characterized. It is a small molecule (molecular weight 353.84) with a LogP of 5.831, indicating high lipophilicity. Solubility data shows it is soluble in DMSO at ≥100 mg/mL.
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| Toxicity/Toxicokinetics |
No specific toxicity data is publicly available for CX04328. In cell-based assays, it shows antiviral activity at micromolar concentrations, indicating a potential therapeutic window. The compound is for research use only and is not intended for human therapeutic applications. No systemic toxicity studies have been reported in the available literature.
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| Additional Infomation |
CX04328 is a quinoline-based inhibitor of the LEDGF/p75-HIV-1 integrase interaction. Its molecular formula is C21H20ClNO2 and its molecular weight is 353.84. It is also known as LEDGIN6 or CX-04328. The compound is a valuable research tool for studying HIV-1 replication and for developing allosteric integrase inhibitors as novel antiretroviral agents. It is not approved for clinical use and is available for research purposes only.
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| Molecular Formula |
C21H20CLNO2
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|---|---|
| Molecular Weight |
353.84
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| Exact Mass |
353.118
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| CAS # |
957890-42-5
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| Related CAS # |
HIV-1 integrase inhibitor;544467-07-4
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| PubChem CID |
24800940
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.831
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
25
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| Complexity |
451
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
XRPUJSGGRFQZPJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H20ClNO2/c1-3-7-16(21(24)25)19-13(2)23-18-11-10-15(22)12-17(18)20(19)14-8-5-4-6-9-14/h4-6,8-12,16H,3,7H2,1-2H3,(H,24,25)
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| Chemical Name |
2-(6-chloro-2-methyl-4-phenylquinolin-3-yl)pentanoic acid
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| Synonyms |
CX 04328; CX-04328; CX04328
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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 (~282.61 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.07 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 (7.07 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8261 mL | 14.1307 mL | 28.2614 mL | |
| 5 mM | 0.5652 mL | 2.8261 mL | 5.6523 mL | |
| 10 mM | 0.2826 mL | 1.4131 mL | 2.8261 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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