| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
HIV-1 inhibitor-6 targets HIV-1 pre-mRNA alternative splicing. By inhibiting this process, the compound blocks HIV replication. It is active against wild-type HIV-1IIIB (subtype B, X4-tropic) with an EC50 of 0.6 µM and against HIV-1 97USSN54 (subtype A, R5-tropic) with an EC50 of 0.9 µM.
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| ln Vitro |
In vitro, HIV-1 inhibitor-6 is a potent inhibitor of HIV-1 pre-mRNA alternative splicing. It blocks HIV replication. The compound shows activity against wild-type HIV-1IIIB with an EC50 of 0.6 µM and against HIV-1 97USSN54 with an EC50 of 0.9 µM. It also inhibits HIV strains resistant to drugs targeting reverse transcriptase, protease, integrase, and CCR5 with EC50s ranging from 0.9 to 1.5 µM.
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| ln Vivo |
In vivo, HIV-1 inhibitor-6 is expected to show efficacy in animal models of HIV infection by inhibiting viral replication. However, specific in vivo efficacy data and detailed animal study results are not extensively reported in the available literature. The compound is primarily used as a research tool.
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| Enzyme Assay |
In vitro antiviral assays for HIV-1 inhibitor-6 are performed using HIV-1 infected cell lines. Cells are infected with HIV-1 and treated with various concentrations of the compound. Viral replication is quantified by measuring viral RNA levels (RT-qPCR), p24 antigen production (ELISA), or by using reporter viruses. EC50 values are determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for HIV-1 inhibitor-6 are performed using cell lines susceptible to HIV-1 infection. Cells are treated with the compound and then infected with HIV-1. The inhibition of viral replication is measured as described above. Cytotoxicity is assessed in parallel using standard assays like MTT to determine the selectivity index.
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| Animal Protocol |
In vivo animal studies with HIV-1 inhibitor-6 would typically be conducted in humanized mouse models of HIV infection. The compound would be administered, and its effects on viral load and CD4+ T cell counts would be assessed. However, specific protocols are not detailed in the available literature.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of HIV-1 inhibitor-6 are not extensively reported. The compound is typically stored as a powder at -20°C for up to 3 years. Specific parameters such as oral bioavailability, half-life, and tissue distribution are not detailed.
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| Toxicity/Toxicokinetics |
The toxicity profile of HIV-1 inhibitor-6 is not extensively reported in the available literature. As a research compound, it is for research use only and not for human therapeutic use. No specific toxicity data are detailed.
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| References | |
| Additional Infomation |
HIV-1 inhibitor-6 (compound 9) is a potent inhibitor of HIV-1 pre-mRNA alternative splicing that blocks HIV replication. It is active against wild-type and drug-resistant HIV-1 strains. The compound is used in HIV research and is available for research purposes only.
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| Molecular Formula |
C14H10N4O4S
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|---|---|
| Molecular Weight |
330.32
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| Exact Mass |
330.042
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| CAS # |
1821309-39-0
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| PubChem CID |
92045028
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
1.9
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
23
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| Complexity |
600
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN1C=CC(=O)C(=C1)C(=O)NC2=NSC3=C2C=C(C=C3)[N+](=O)[O-]
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| InChi Key |
CPKUAABJFWRBSN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C14H10N4O4S/c1-17-5-4-11(19)10(7-17)14(20)15-13-9-6-8(18(21)22)2-3-12(9)23-16-13/h2-7H,1H3,(H,15,16,20)
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| Chemical Name |
1-methyl-N-(5-nitro-1,2-benzothiazol-3-yl)-4-oxopyridine-3-carboxamide
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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 : ~3.33 mg/mL (~10.08 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0274 mL | 15.1368 mL | 30.2737 mL | |
| 5 mM | 0.6055 mL | 3.0274 mL | 6.0547 mL | |
| 10 mM | 0.3027 mL | 1.5137 mL | 3.0274 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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