SMT-738
Based on 1 Customer Validation
SMT-738 is a bacterial bactericide. SMT-738 targets the small molecules responsible for lipoprotein transport in Enterobacteriaceae, causing abnormal lipoprotein localization and bacterial cell death. SMT-738 inhibits the growth of E. coli and K. pneumoniae. SMT-738 reduces bacterial loads in mouse models of urinary tract infection, bloodstream infection, and pulmonary infection caused by Enterobacterales. SMT-738 can be used in the research of Enterobacteriaceae infections, urinary tract infections, bloodstream infections, and pneumonia.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.13%
- CAS. Nr.: 2862851-15-6
- Formel: C21H24N6O2
- Molecular Weight:392.45
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Speicherung:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Biologische Aktivität
Beschreibung
In Vitro
SMT-738 potently inhibits the growth of E. coli NCTC 13441 and K. pneumoniae NCTC 13438 with MIC values of 0.39 μM (0.15 μg/mL) and 1.56 μM (0.61 μg/mL), respectively[1].
SMT-738 inhibits the growth of two cefiderocol-resistant E. coli and K. pneumoniae respiratory isolates with MIC values of 0.25 μg/mL and 0.5 μg/mL, respectively[1].
SMT-738 potently inhibits the growth of 15 NDM-carrying E. coli isolates with an MIC range of 0.25-1 μg/mL and 15 NDM-carrying K. pneumoniae isolates with an MIC range of 0.5-1 μg/mL[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | C0 | Vss | CL |
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| Mice[1] | 20 mg/kg | i.v. | 18386 ng/mL | 4.3 L/kg | 59 mL/min/kg |
In Vivo
SMT-738 (5-20 mg/kg; i.v. infusion over 60 min; twice daily) reduces the bloodstream infection burden of *E. coli* BAA2469 in CD-1 mice by 4 log10, and the infection burden falls below the limit of detection at doses of 10 mg/kg BID or 20 mg/kg BID[1].
SMT-738 (20 mg/kg; i.v. infusion over 60 min; once daily; twice daily) reduces the stagnant level of pulmonary infection burden caused by K. pneumoniae ATCC 43816 in neutropenic CD-1 mice by 1-2 log10[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C3H/HeN (female, E. coli UTI89 infection)[1]
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Dosage:20 mg/kg
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Administration:i.v. infusion over 60 min; once daily for 3 days; twice daily for 3 days
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Result:Achieved a 5-6 log10 reduction in bacterial burden compared to pre-treatment.
Reached levels below the limit of detection in both urine and kidney.
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Animal Model:CD-1 (male, E. coli BAA2469 infection)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.v. infusion over 60 min; twice daily
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Result:Showed a dose-dependent reduction in blood bacterial burden.
Achieved a 4 log10 reduction compared to pre-treatment at 10 mg/kg BID and 20 mg/kg BID doses.
Reached bacterial levels below the limit of detection at 10 mg/kg BID and 20 mg/kg BID doses.
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Animal Model:CD-1 (male; K. pneumoniae ATCC 43816 infection)[1]
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Dosage:20 mg/kg
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Administration:i.v. infusion over 60 min; once daily; twice daily
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Result:Achieved a 1-2 log10 reduction in lung bacterial burden compared to pre-treatment stasis levels.
Chemical Information
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CAS. Nr. 2862851-15-6
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Appearance Solid
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Molecular Weight 392.45
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Formel C21H24N6O2
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Color Light yellow to yellow
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SMILES
CC1=CN=CC=C1C2=C(N=C(N2)N)C3=CC4=C(OCCN4C(C(C)(N)C)=O)C=C3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 100 mg/mL (254.81 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.37 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protokoll
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Mammalian live/dead viability and cytotoxicity staining
Live/dead viability and cytotoxicity staining assays are based on the simultaneous detection of intracellular esterase activity in metabolically active (viable) cells and membrane integrity loss in non-viable cells. In commonly used dual-staining approaches, membrane-permeant fluorogenic substrates are converted by intracellular esterases into fluorescent products in live cells, while impermeant DNA-binding dyes selectively enter cells with compromised plasma membranes and label nucleic acids in dead or dying cells, enabling discrimination between viable and non-viable populations by fluorescence microscopy or flow cytometry.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
Reinheit & Dokumentation
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.5481 mL | 12.7405 mL | 25.4810 mL | 63.7024 mL |
| 5 mM | 0.5096 mL | 2.5481 mL | 5.0962 mL | 12.7405 mL | |
| 10 mM | 0.2548 mL | 1.2740 mL | 2.5481 mL | 6.3702 mL | |
| 15 mM | 0.1699 mL | 0.8494 mL | 1.6987 mL | 4.2468 mL | |
| 20 mM | 0.1274 mL | 0.6370 mL | 1.2740 mL | 3.1851 mL | |
| 25 mM | 0.1019 mL | 0.5096 mL | 1.0192 mL | 2.5481 mL | |
| 30 mM | 0.0849 mL | 0.4247 mL | 0.8494 mL | 2.1234 mL | |
| 40 mM | 0.0637 mL | 0.3185 mL | 0.6370 mL | 1.5926 mL | |
| 50 mM | 0.0510 mL | 0.2548 mL | 0.5096 mL | 1.2740 mL | |
| 60 mM | 0.0425 mL | 0.2123 mL | 0.4247 mL | 1.0617 mL | |
| 80 mM | 0.0319 mL | 0.1593 mL | 0.3185 mL | 0.7963 mL | |
| 100 mM | 0.0255 mL | 0.1274 mL | 0.2548 mL | 0.6370 mL |
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