VKT-17-P4-23
Based on 1 Customer Validation
VKT-17-P4-23 is a blood-brain barrier-permeable DksA inhibitor. DksA is a highly conserved transcriptional regulator in Gram-negative bacteria, with a Kd of 124 μM. Through the DksA-regulated, SPI-2-dependent survival pathway, VKT-17-P4-23 exhibits antibacterial activity against both planktonic and intracellular pathogens such as Salmonella, and also effectively combats persistent bacteria that are difficult to eliminate. VKT-17-P4-23 can be used in studies of Salmonella infection.
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- Pureté : 98.13%
- CAS No.: 2411865-57-9
- Formule: C13H16N4O
- Masse moléculaire:244.29
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
In Vitro
VKT-17-P4-23 (16 μg/mL; 20 h) inhibits growth of S. Typhimurium ATCC strain 14028s in EG minimal medium with an MIC of 16 μg/mL[1].
VKT-17-P4-23 (≥4 μg/mL; 20 h) inhibits growth of intracellular S. Typhimurium in J774 macrophage-like cells in a dose-dependent manner, with significant activity at concentrations ≥4 μg/mL[1].
VKT-17-P4-23 (16 μg/mL; 20 h) significantly reduces survival of in vitro-selected persistent S. Typhimurium cells exposed to DNA synthesis inhibitors[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
In Vivo
VKT-17-P4-23 (10 mg/kg; i.p.; every 12 hours; 12 hours pre-infection plus 3 total post-infection doses) significantly reduces Salmonella burden in systemic murine infection, eliminates liver histopathological lesions, and normalizes plasma liver enzyme levels[1].
VKT-17-P4-23 (10 mg/kg; i.p.; every 12 hours; 12 hours pre-infection plus 3 total post-infection doses) significantly reduces Salmonella burden in both gastrointestinal and systemic tissues during oral murine salmonellosis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (6 to 8 weeks old, 5 males, 5 females, intraperitoneal inoculation with Salmonella enterica serovar Typhimurium)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every 12 hours; 12 hours pre-infection plus 3 total post-infection doses
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Result:Reduced Salmonella burdens in livers, spleens, and cecal contents significantly compared to vehicle controls.
Eliminated measurable histopathological liver lesions, reducing inflammatory foci counts to near zero.
Normalized plasma alanine aminotransferase (ALT) and aspartate aminotransferase (AST) levels to basal levels matching uninfected naïve mice.
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Animal Model:C57BL/6 (6 to 8 weeks old, streptomycin pretreatment, oral inoculation with Salmonella enterica serovar Typhimurium)[1]
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Dosage:10 mg/kg
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Administration:i.p.; every 12 hours; 12 hours pre-infection plus 3 total post-infection doses
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Result:Reduced Salmonella burdens in cecal contents significantly compared to vehicle controls.
Reduced Salmonella burdens in Peyer’s patches significantly compared to vehicle controls.
Reduced Salmonella burdens in mesenteric lymph nodes significantly compared to vehicle controls.
Reduced Salmonella burdens in livers significantly compared to vehicle controls.
Chemical Information
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CAS No. 2411865-57-9
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Appearance Solid
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Masse moléculaire 244.29
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Formule C13H16N4O
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Color White to off-white
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SMILES
O=C(C1=NNC=N1)NCCCCC2=CC=CC=C2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (409.35 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (10.23 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.
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.
Protocole
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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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Gram Staining of Tissue Sections
Gram staining of tissue sections is a histochemical technique used to differentiate Gram-positive and Gram-negative bacteria within histological specimens based on differences in bacterial cell wall structure and dye retention, adapted from classical bacteriological Gram staining into tissue-compatible “histological Gram stain” variants. In tissue applications, modifications of the Brown-Hopps and Brown-Brenn methods are commonly used to improve differentiation of microorganisms embedded within host connective tissue and to reduce overstaining or loss of Gram-negative signal, which are known limitations of earlier approaches. The principle relies on crystal violet-iodine complex retention in Gram-positive organisms and subsequent decolorization and counterstaining steps that allow contrast visualization of Gram-negative organisms against tissue background.
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Bacterial live/dead nucleic-acid viability staining
The LIVE/DEAD bacterial viability staining method is based on differential permeability of nucleic-acid-binding fluorescent dyes, most commonly SYTO 9 and propidium iodide (PI), which enables discrimination of bacterial populations with intact versus compromised cytoplasmic membranes. SYTO 9 penetrates both intact and damaged bacterial membranes and binds nucleic acids to produce green fluorescence, whereas propidium iodide penetrates only cells with compromised membranes and fluoresces red while also reducing SYTO 9 signal through competitive binding and fluorescence interactions. The resulting fluorescence pattern is interpreted as a proxy for membrane integrity, which is widely used as an indicator of bacterial viability in microscopy, flow cytometry, and spectroscopic platforms. However, mechanistic studies show that SYTO 9 and PI interactions involve displacement and fluorescence resonance energy transfer effects, which can influence signal interpretation depending on dye ratios a
Pureté et documentation
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Fiche technique (272 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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Instruction de manipulation (2659 KB)
Références
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. 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 | 4.0935 mL | 20.4675 mL | 40.9350 mL | 102.3374 mL |
| 5 mM | 0.8187 mL | 4.0935 mL | 8.1870 mL | 20.4675 mL | |
| 10 mM | 0.4093 mL | 2.0467 mL | 4.0935 mL | 10.2337 mL | |
| 15 mM | 0.2729 mL | 1.3645 mL | 2.7290 mL | 6.8225 mL | |
| 20 mM | 0.2047 mL | 1.0234 mL | 2.0467 mL | 5.1169 mL | |
| 25 mM | 0.1637 mL | 0.8187 mL | 1.6374 mL | 4.0935 mL | |
| 30 mM | 0.1364 mL | 0.6822 mL | 1.3645 mL | 3.4112 mL | |
| 40 mM | 0.1023 mL | 0.5117 mL | 1.0234 mL | 2.5584 mL | |
| 50 mM | 0.0819 mL | 0.4093 mL | 0.8187 mL | 2.0467 mL | |
| 60 mM | 0.0682 mL | 0.3411 mL | 0.6822 mL | 1.7056 mL | |
| 80 mM | 0.0512 mL | 0.2558 mL | 0.5117 mL | 1.2792 mL | |
| 100 mM | 0.0409 mL | 0.2047 mL | 0.4093 mL | 1.0234 mL |
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