| 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 |
IC50: 22 µM (1,4-dihydroxy-2-naphthoate prenyltransferase, MenA)[1]
MenA-IN-2 targets the bacterial enzyme MenA (1,4-dihydroxy-2-naphthoate prenyltransferase), which is essential for the production of menaquinone in most Gram-positive bacteria, including Mycobacterium tuberculosis (Mtb). This pathway is absent in humans, making it a promising and selective target for developing new antibiotics with a low risk of off-target effects on human cells. |
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| ln Vitro |
MenA-IN-2 demonstrates potent enzymatic inhibition, with an IC₅0 of 22 microM against the MenA enzyme. It also exhibits significant antibacterial activity against Mycobacterium tuberculosis (Mtb), with a GIC₅0 (growth inhibition concentration 50%) of 10 microM. These data indicate that it effectively stops the growth of Mtb by disrupting its ability to produce a critical component of its respiratory chain.
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| ln Vivo |
Not available. The standard literature does not provide in vivo efficacy data for MenA-IN-2, such as its ability to clear Mtb infection in a murine model. The compound has been reported to have an inhibitory effect on the continuous transmission of Mtb, indicating its potential to limit bacterial spread.
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| Enzyme Assay |
A standard radiometric MenA enzyme assay protocol involves incubating purified MenA protein with its substrate, 1,4-dihydroxy-2-naphthoate (DHNA) and a prenyl donor like solanesyl diphosphate, in a Tris-HCl buffer (pH 7.5). The reaction is initiated by adding the enzyme and the compound is tested at various concentrations. After termination, the product is extracted with an organic solvent and quantified by HPLC or liquid scintillation counting if radiolabeled substrates are used, to determine the IC₅0.
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| Cell Assay |
A standard protocol for testing antibacterial activity involves growing Mycobacterium tuberculosis (Mtb) in Middlebrook 7H9 broth. The bacteria are then exposed to a 2-fold dilution series of MenA-IN-2 in a 96-well plate for 5-7 days. Bacterial growth is measured by adding a metabolic indicator dye (e.g., resazurin or Alamar Blue), which changes color in the presence of live bacteria. The well with the lowest concentration of compound that prevents this color change is the MIC (minimum inhibitory concentration).
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| Animal Protocol |
A standard in vivo protocol for testing a new anti-tuberculosis drug would involve infecting mice with aerosolized Mycobacterium tuberculosis. After the infection is established, the mice would be treated with MenA-IN-2, often by oral gavage, daily for several weeks. The primary endpoint is the reduction of bacterial load (colony forming units, CFU) in the lungs and spleen compared to a vehicle-treated control group.
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| ADME/Pharmacokinetics |
MenA-IN-2 has an IC₅0 of 22 microM against the MenA enzyme. It has moderate solubility in DMSO (225 mg/mL, ~581.46 mM). For in vivo use, it can be formulated in various vehicles, such as 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline.
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| Toxicity/Toxicokinetics |
As a specific inhibitor of a bacterial enzyme, the direct toxicity to mammalian cells is expected to be low. The compound's safety profile is not provided, but selective antibacterial agents are designed to target bacterial pathways not present in humans, reducing the potential for toxic effects.
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| References |
[1]. Berg K, et al. SAR study of piperidine derivatives as inhibitors of 1,4-dihydroxy-2-naphthoate isoprenyltransferase (MenA) from Mycobacterium tuberculosis. Eur J Med Chem. 2023 Jan 18;249:115125.
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| Additional Infomation |
It should be noted that this compound is a potent inhibitor of the MenA enzyme, which is essential for menaquinone biosynthesis in Mtb, making it a promising lead for new antitubercular agents. This product is for laboratory research use only and not for human or therapeutic applications.
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| Molecular Formula |
C23H31CLN2O
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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) |
DMSO :~250 mg/mL (~646.06 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.38 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 20.8 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.) |
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.
Products are for research use only; We do not sell to patients
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