1. Anti-infection
  2. Bacterial
  3. Antibacterial agent 302

Antibacterial agent 302 is an antibacterial agent. Antibacterial agent 302 shows a potent and broad-spectrum antibacterial activity. Antibacterial agent 302 has no significant hemolytic toxicity and cytotoxicity, and a low tendency to induce resistance. Antibacterial agent 302 exerts its antibacterial mechanism by disrupting the integrity of the bacterial cell membranes. Antibacterial agent 302 can be used for the study of bacterial keratitis.

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Antibacterial agent 302

Antibacterial agent 302 Chemical Structure

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Description

Antibacterial agent 302 is an antibacterial agent. Antibacterial agent 302 shows a potent and broad-spectrum antibacterial activity. Antibacterial agent 302 has no significant hemolytic toxicity and cytotoxicity, and a low tendency to induce resistance. Antibacterial agent 302 exerts its antibacterial mechanism by disrupting the integrity of the bacterial cell membranes. Antibacterial agent 302 can be used for the study of bacterial keratitis[1].

IC50 & Target

HIF-1α

 

In Vitro

Antibacterial agent 302 (Compound 27) shows good antibacterial activity against both Gram-positive (S. epidermidis CMCC 26069, MIC = 0.39 μg/mL) and Gram-negative (K. pneumoniae ATCC 10031, MIC = 1.56 μg/mL) bacteria[1].
Antibacterial agent 302 exhibits low hemolytic toxicity to rabbit red blood cells (RBCs) and high safety[1].
Antibacterial agent 302 (24 h) shows a CC50 of 62.44 μg/mL against HEK 293 cells, 84.46 μg/mL against NCTC clone 929 cells, and 60.99 μg/mL and 61.17 μg/mL against THLE-2 and HSC-T6 cells, respectively[1].
Antibacterial agent 302 (21 days) maintains stable MIC values against Staphylococcus aureus ATCC 29213 and Escherichia coli ATCC 25922 over 20 generations, and is not prone to inducing drug resistance[1].
Antibacterial agent 302 (8 × MIC, 2 h) exerts its bactericidal effect by disrupting the cell membranes of Staphylococcus aureus ATCC 29213, MRSA NCTC 10442, and Escherichia coli ATCC 25922 and causes bacterial morphological damage[1].
Antibacterial agent 302 (1-8 × MIC, 1 h) increases the permeability of the bacterial membranes of MRSA NCTC 10442 and Pseudomonas aeruginosa ATCC 9027, leading to leakage of contents[1].
Antibacterial agent 302 (1-2 × MIC, 1 h) can increase the outer membrane permeability of E. coli in a concentration-dependent manner[1].
Antibacterial agent 302 (4 × MIC, 90 min) upregulates the dltB, mprF, and vraG genes in Staphylococcus aureus ATCC 29213 by 3.9-fold, 3.1-fold, and 4.9-fold, respectively[1].
Antibacterial agent 302 (0.39-12.5 μg/mL, 24 h) effectively inhibits biofilm formation in Staphylococcus aureus ATCC 29213 and Escherichia coli ATCC 25922[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: Caco-2 cells
Concentration: 2.07 μM
Incubation Time: 72 h
Result: Suppressed Caco-2 cell migration with 56.29 % wound closure.

Cell Cycle Analysis[1]

Cell Line: Caco-2 cells
Concentration:
Incubation Time: 24 h and 48 h
Result: Increased of % Caco-2 cells in G0 / G1 phase from 62.07 % in the control to 86.36 %.
Reduced nearly 3-fold in % Caco-2 cells in both S phase and G2 / M phase.

Apoptosis Analysis[1]

Cell Line: Caco-2 cells
Concentration:
Incubation Time: 24 h and 48 h
Result: Increased 42 fold in total apoptosis
Increased the ratio of annexin V-FITC positive early apoptotic cells from 0.54 % to 20.26 %, whilst the percentage of late apoptotic cells rose from 0.22 % to 11 %.
Resulted in a combined percentage of early and late apoptotic cells that significantly exceeded the percentage of necrotic cells. (Early apoptotic cells is 20.26%, late apoptotic cells is 11.32%, necrotic cells is 3.61%).
In Vivo

Antibacterial agent 302 (Compound 27) (5 mg/mL, topical application, 4-6 times daily ) shows significant efficacy in vivo against keratitis induced by Gram-positive (S. aureus) and Gram-negative (P. aeruginosa) mice, with no significant toxic symptoms observed in the mice[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: The left corneas of the C57BL/6 mice aged 6-8 weeks (with a weight of 16-18 g) were scratched with a sterile needle. The bacterial suspensions of S. aureus ATCC 29213 or P. aeruginosa ATCC 9027 were adjusted to a bacterial cell concentration of approximately 5× 107 CFU/mL and then dropped onto the injured corneas to establish a corneal infection model[1].
Dosage: 5 mg/mL
Administration: For S. aureus infection: Topical application, starting 24 hours after infection, four times daily (2-hour intervals) for three consecutive days.
For P. aeruginosa infection: Topical application, once every 20 minutes for the first hour after the first dose, then once every 2 hours (a total of six times daily) for two consecutive days.
Result: For S. aureus infection, corneal bacterial load decreased by 5.56 log.
For P. aeruginosa infection, bacterial load decreased by 2.20 log.
Molecular Weight

847.10

Formula

C44H70N12O5

SMILES

O=C(C1=CN(CCCCNC([C@@H](N)CCCNC(N)=N)=O)C2=C(C=CC=C2)C1=O)NC3=CC(OCCCCNC([C@@H](N)CCCNC(N)=N)=O)=C(C(C)(C)C)C=C3C(C)(C)C

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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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.

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Product Name:
Antibacterial agent 302
Cat. No.:
HY-179438
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