| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Bacterial ribosome - inhibitor of trans-translation.
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| ln Vitro |
Some features of MBX-4132, which blocks trans translation to disrupt protein synthesis, may indicate that it is a potential Neisseria gonorrhoeae (N. gonorrhoeae) match[1].
In vitro studies demonstrate that MBX-4132 is an oxadiazole that inhibits trans-translation by binding to bacterial ribosomes. Trans-translation is a bacterial ribosome-mediated process that rescues stalled ribosomes and targets proteins for degradation, playing a critical role in bacterial survival under stress conditions. By inhibiting trans-translation, MBX-4132 disrupts bacterial protein quality control and leads to bacterial cell death. The compound is bactericidal against Neisseria gonorrhoeae at concentrations ≥ 4X MIC, including multiple-antibiotic resistant strains. |
| ln Vivo |
In vivo studies have demonstrated that MBX-4132 (10 mg/kg) clears infection by a multiple-antibiotic resistant N. gonorrhoeae strain. The compound's ability to target trans-translation, a pathway essential for bacterial survival but absent in mammalian cells, makes it a promising therapeutic agent for combating antibiotic-resistant bacterial infections, particularly gonorrhea. The compound's bactericidal activity against N. gonorrhoeae, including drug-resistant strains, suggests potential for the treatment of gonorrhea, a sexually transmitted infection for which new antibiotics are urgently needed due to increasing antibiotic resistance.
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| Enzyme Assay |
For antibacterial susceptibility testing, minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC) assays are performed against a panel of bacterial strains including N. gonorrhoeae. Serial dilutions of MBX-4132 are prepared and incubated with standardized bacterial cultures. MIC is determined as the lowest concentration showing no visible growth after incubation. MBC is determined by subculturing wells with no visible growth onto agar plates. Time-kill assays are performed to assess the bactericidal kinetics of the compound. For mechanistic studies, ribosome binding assays are performed using purified bacterial ribosomes and radiolabeled or fluorescently labeled MBX-4132.
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| Cell Assay |
Cellular assays for MBX-4132 typically involve culturing bacterial strains and treating them with the compound at various concentrations. Bacterial viability is assessed by colony counting or by measuring optical density. The compound's effects on bacterial protein synthesis and trans-translation are assessed by measuring the incorporation of radiolabeled amino acids or by using reporter systems for trans-translation activity. Cytotoxicity against mammalian cells is assessed using MTT or CellTiter-Glo assays to evaluate selectivity. The compound's activity against drug-resistant clinical isolates is assessed to determine its spectrum of activity.
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| Animal Protocol |
In vivo efficacy of MBX-4132 is evaluated in animal models of bacterial infection, such as mouse models of N. gonorrhoeae infection. Mice are infected with a multiple-antibiotic resistant N. gonorrhoeae strain and then treated with MBX-4132 via oral or intraperitoneal administration (e.g., 10 mg/kg). Bacterial burden in the infection site (e.g., genital tract) is determined by colony counting. The compound's ability to clear infection is assessed. Pharmacokinetic studies are conducted to determine the compound's bioavailability and tissue distribution. The compound's efficacy against drug-resistant strains supports its potential for further development as a treatment for gonorrhea.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MBX-4132 have been characterized to support its use as a research tool. The compound has a molecular weight of 338.34 and the molecular formula C18H15FN4O2. Key PK parameters including half-life, clearance, volume of distribution, and oral bioavailability are determined using LC-MS/MS analysis of plasma and tissue samples following administration. The compound's ability to reach the site of infection (e.g., the genital tract) is important for its efficacy in vivo. The compound should be stored as a powder at -20°C.
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| Toxicity/Toxicokinetics |
Toxicological evaluation of MBX-4132 is typically conducted in parallel with efficacy studies in animal models. Standard toxicology assessments include in vitro cytotoxicity assays against a panel of mammalian cell lines to determine the compound's selectivity index. In vivo toxicity studies in rodents include acute and repeated-dose toxicity testing, observation of clinical signs and body weight changes, and histopathological examination of major organs. As an antibacterial agent that targets bacterial trans-translation, a pathway absent in mammalian cells, MBX-4132 is expected to have a favorable safety profile with minimal off-target effects on host cells.
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| References | |
| Additional Infomation |
MBX-4132 is a research tool compound and potential therapeutic agent used for studying bacterial trans-translation and for developing new antibiotics against drug-resistant bacterial infections. The compound is not approved for clinical use and is intended for laboratory research purposes only. Its mechanism of action involves inhibition of trans-translation by binding to bacterial ribosomes, disrupting bacterial protein quality control and leading to bacterial cell death. MBX-4132 is bactericidal against N. gonorrhoeae, including multiple-antibiotic resistant strains, and clears infection in animal models. This compound is valuable for validating trans-translation as a therapeutic target and for developing new antibiotics for gonorrhea and other bacterial infections.
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| Molecular Formula |
C18H15FN4O2
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|---|---|
| Molecular Weight |
338.3424
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| Exact Mass |
338.117
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| Elemental Analysis |
C, 63.90 H, 4.47 F, 5.62 N, 16.56 O, 9.46
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| CAS # |
2286411-30-9
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| PubChem CID |
134691207
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| Appearance |
White to off-white solid powder
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| Density |
1.382±0.06 g/cm3(Predicted)
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
25
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| Complexity |
472
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| Defined Atom Stereocenter Count |
0
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| SMILES |
FC1C=CC(=CC=1)C1=NN=C(NC(N2CC3=CC=CC=C3CC2)=O)O1
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| InChi Key |
OZHWSOOZCIJFQN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C18H15FN4O2/c19-15-7-5-13(6-8-15)16-21-22-17(25-16)20-18(24)23-10-9-12-3-1-2-4-14(12)11-23/h1-8H,9-11H2,(H,20,22,24)
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| Chemical Name |
N-(5-(4-fluorophenyl)-1,3,4-oxadiazol-2-yl)-3,4-dihydroisoquinoline-2(1H)-carboxamide
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| Synonyms |
MBX-4132; MBX 4132; MBX4132;
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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 : ~25 mg/mL (~73.89 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 | 2.9556 mL | 14.7780 mL | 29.5561 mL | |
| 5 mM | 0.5911 mL | 2.9556 mL | 5.9112 mL | |
| 10 mM | 0.2956 mL | 1.4778 mL | 2.9556 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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