| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Biotin protein ligase[1]
Bio-AMS TFA targets bacterial biotin protein ligase (BPL), an enzyme essential for biotin metabolism in bacteria. By inhibiting this enzyme, the compound disrupts biotinylation of key carboxylases involved in fatty acid and lipid biosynthesis. This target is selective for bacterial BPL, making it an attractive candidate for antitubercular drug development. The compound does not inhibit human biotin-dependent enzymes at relevant concentrations. |
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| ln Vitro |
Bio-AMS exhibits outstanding antitubercular action against MDR/XDR-TB and Mtb H37Rv strains, with MICs ranging from 0.16 to 0.625 μM, and is unaffected by modifications to the main carbon source[1]. In mouse macrophages infected with Mtb, Bio-AMS (2.5, 5 and 10 μM; 24 h) reduces Mtb development in a concentration-dependent manner without causing any damage to the mitochondria[2].
In vitro, Bio-AMS exhibits excellent antitubercular activity against Mtb H37Rv and MDR/XDR-TB strains with minimum inhibitory concentrations (MICs) ranging from 0.16 to 0.625 microM. Its activity is not affected by changes to the primary carbon source. Bio-AMS (2.5, 5, and 10 microM; 24 hours) inhibits growth of Mtb in a concentration-dependent manner in Mtb-infected mouse macrophages. Additionally, it shows no signs of mitochondrial toxicity in these assays. |
| ln Vivo |
In vivo efficacy data for Bio-AMS TFA have not been extensively reported in standard product literature, as the compound is primarily characterized in in vitro and cell-based assays. The primary focus has been on demonstrating its selective activity against mycobacterial strains in culture and in infected macrophage models. Further in vivo animal model studies would be required to evaluate its therapeutic potential and pharmacokinetic properties.
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| Enzyme Assay |
Binding assays for Bio-AMS TFA typically involve biochemical inhibition studies using purified bacterial biotin protein ligase enzyme. The compound is incubated with the enzyme, biotin, and ATP, and the inhibition of biotinyl-AMP formation is measured. IC50 values can be determined from dose-response curves. Competitive binding studies may also be performed to confirm the mechanism of inhibition at the biotin binding site.
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| Cell Assay |
Cellular assays for Bio-AMS TFA utilize Mtb-infected mouse macrophage models. Macrophages are infected with Mtb H37Rv or MDR strains, then treated with varying concentrations of Bio-AMS (e.g., 2.5, 5, and 10 microM for 24 hours). Bacterial growth is assessed by colony-forming unit (CFU) counts or metabolic activity assays. Cytotoxicity is evaluated in uninfected control cells using standard viability assays such as MTT.
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| Animal Protocol |
Detailed in vivo animal protocols for Bio-AMS TFA are not extensively reported in available product literature. As the compound is currently characterized in in vitro and cell-based systems, standard mouse models of tuberculosis infection could be employed for future efficacy studies, typically involving intravenous or oral administration of the compound followed by measurement of bacterial burden in lung and spleen tissues.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Bio-AMS TFA are not extensively detailed in standard product literature. The compound is primarily characterized for its antitubercular activity in vitro. As a biotin protein ligase inhibitor, its physicochemical properties would need to be evaluated in dedicated PK studies to determine oral bioavailability, half-life, plasma protein binding, and tissue distribution for potential therapeutic applications.
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| Toxicity/Toxicokinetics |
Toxicological data for Bio-AMS TFA are limited in available product literature. In vitro studies in Mtb-infected mouse macrophages show no signs of mitochondrial toxicity. However, comprehensive toxicology assessments including acute and repeated-dose toxicity, genotoxicity, and safety pharmacology have not been described. Standard precautions for handling research-use chemical compounds should be followed.
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| References | |
| Additional Infomation |
Bio-AMS TFA (CAS 1393881-52-1) has the molecular formula C22H30F3N9O9S2 and a molecular weight of 685.65. It is available as a TFA salt. The compound has been studied for its selective antitubercular activity against MDR and XDR-TB strains. It represents a novel approach targeting bacterial biotin metabolism, a pathway distinct from current frontline TB drugs. The compound is for research use only and not for human therapy.
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| Molecular Formula |
C22H30F3N9O9S2
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| Molecular Weight |
685.65
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| Related CAS # |
Bio-AMS;1393881-52-1
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| Appearance |
Typically exists as solid at room temperature
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 1.4585 mL | 7.2924 mL | 14.5847 mL | |
| 5 mM | 0.2917 mL | 1.4585 mL | 2.9169 mL | |
| 10 mM | 0.1458 mL | 0.7292 mL | 1.4585 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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