2. Anti-infection
  3. Bacterial
  4. VKT-17-P4-23

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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VKT-17-P4-23

VKT-17-P4-23 Chemical Structure

CAS No. : 2411865-57-9

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VKT-17-P4-23 Related Antibodies

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Description

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[1].

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.

VKT-17-P4-23 Related Antibodies
Parmacokinetics
Species Dose Route AUC0-24 Cmax Tmax T1/2
Rat[1] 1.0 mg/kg i.p. 6979 ng·h/mL 798 ng/mL 2.0 h /
Rat[1] 10.0 mg/kg p.o. 1271 ng·h/mL 447 ng/mL 0.5 h /
Rat[1] 1.0 mg/kg i.v. / / / 2.68 h
Rat[1] 10.0 mg/kg p.o. / 950 ng/mL 2.02 h /
In Vivo

VKT-17-P4-23 (1-10 mg/kg; i.v., i.p., p.o.; single dose) exhibits favorable pharmacokinetic properties in healthy male Sprague-Dawley rats, with measurable tissue distribution including passage across the blood-brain barrier, and an intravenous half-life of 2.68 hours[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 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.

Animal Model: C57BL/6 (6 to 8 weeks old, 5 males, 5 females, intraperitoneal inoculation with Salmonella enterica serovar Typhimurium)[1]
Dosage: 10 mg/kg
Administration: i.p.; every 12 hours; 12 hours pre-infection plus 3 total post-infection doses
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.
Animal Model: C57BL/6 (6 to 8 weeks old, streptomycin pretreatment, oral inoculation with Salmonella enterica serovar Typhimurium)[1]
Dosage: 10 mg/kg
Administration: i.p.; every 12 hours; 12 hours pre-infection plus 3 total post-infection doses
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.
Molecular Weight

244.29

Formula

C13H16N4O
CAS No.
SMILES

O=C(C1=NNC=N1)NCCCCC2=CC=CC=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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VKT-17-P4-23 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

VKT-17-P4-232411865-57-9BacterialGreBSalmonella enterica serovar TyphimuriumC57BL/6 micerpsM promoterDksAE. coliSPI-2Sprague-Dawley ratsJ774 macrophage-like cellsGreAInhibitorinhibitorinhibit

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