| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
Ki: 48 nM (ANAT)[1]
ANAT inhibitor-4 dilithium targets N-acetyltransferase (ANAT), an enzyme involved in acetyl-CoA-dependent acetylation reactions. The compound inhibits ANAT with a Ki value of 48 nM. By blocking ANAT function, the compound may modulate various biological processes such as cell growth, inflammation, or protein synthesis. It has potential applications in Canavan disease (CD) research. |
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| ln Vitro |
In vitro studies demonstrate that ANAT inhibitor-4 dilithium is a potent inhibitor of N-acetyltransferase (ANAT) with a Ki value of 48 nM. This high affinity for the enzyme indicates strong inhibitory activity. The compound's inhibition of ANAT may modulate acetylation-dependent biological processes. It has been investigated for its potential in Canavan disease research. Detailed cellular activity data, including IC50 values in cell-based systems, are not extensively documented in the available literature.
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| ln Vivo |
In vivo activity of ANAT inhibitor-4 dilithium is inferred from its potential use in Canavan disease research. As an ANAT inhibitor, it may modulate acetylation pathways involved in the pathogenesis of this genetic disorder. The dilithium salt form is designed to improve solubility and bioavailability for in vivo applications. Detailed in vivo efficacy data from animal models are not extensively documented in the available literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for ANAT inhibitor-4 dilithium involves measuring its inhibitory activity against N-acetyltransferase (ANAT). The assay typically uses purified recombinant ANAT enzyme incubated with the compound at varying concentrations and acetyl-CoA as the acetyl donor. Enzyme activity is measured by quantifying the transfer of acetyl groups to a suitable acceptor substrate using methods such as radiometric detection, HPLC, or spectrophotometric assays. The Ki value of 48 nM is determined from the inhibition kinetics.
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| Cell Assay |
In vitro cell-based assays for ANAT inhibitor-4 dilithium are conducted using cell lines relevant to Canavan disease or acetylation research. Cells are treated with the compound at various concentrations, and ANAT activity is measured by quantifying acetylation levels of target proteins or metabolites. Cellular effects such as proliferation, apoptosis, or differentiation are assessed. Cytotoxicity is evaluated using standard cell viability assays. The compound's ability to modulate acetylation-dependent biological processes is investigated.
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| Animal Protocol |
In vivo animal studies for ANAT inhibitor-4 dilithium are typically conducted using mouse models of Canavan disease or other conditions where ANAT inhibition may be beneficial. Animals are administered the compound via appropriate routes, and efficacy is evaluated by measuring disease-relevant biomarkers, behavioral outcomes, and histopathological changes. Pharmacokinetic parameters are determined from plasma samples. The dilithium salt form is used to enhance solubility and bioavailability.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of ANAT inhibitor-4 dilithium include formulation as a dilithium salt to improve solubility and bioavailability. The compound has a molecular weight of 966.55 and a molecular formula of C28H43Li2N8O21P3S. It appears as a white to off-white solid. Storage recommendations include 4°C, protect from light, stored under nitrogen, with in solvent stability of -80°C for 6 months or -20°C for 1 month.
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| Toxicity/Toxicokinetics |
Toxicity information for ANAT inhibitor-4 dilithium is limited in the available literature. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human therapeutic applications. Cytotoxicity should be evaluated in cell-based assays to determine appropriate concentrations. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
ANAT inhibitor-4 dilithium (compound BA2) is a potent N-acetyltransferase (ANAT) inhibitor with a Ki value of 48 nM. It has potential for Canavan disease (CD) research. By blocking ANAT function, the compound may modulate cell growth, inflammation, or protein synthesis. The dilithium salt form improves solubility and bioavailability. It is intended for research use only and is not for human therapeutic applications.
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| Molecular Formula |
C28H43LI2N8O21P3S
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|---|---|
| Molecular Weight |
966.55
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| Appearance |
White to off-white solid powder
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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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture. |
| 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) |
H2O :≥ 100 mg/mL (~103.46 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 | 1.0346 mL | 5.1730 mL | 10.3461 mL | |
| 5 mM | 0.2069 mL | 1.0346 mL | 2.0692 mL | |
| 10 mM | 0.1035 mL | 0.5173 mL | 1.0346 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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