1. Anti-infection
  2. Bacterial
  3. Antimicrobial agent-8

Antimicrobial agent-8 (Compound 15) is a potent antimicrobial agent, and shows potent antimicrobial activity with an MIC range of 2-8 μg/mL against Gram-negative and Gram-positive bacteria. Antimicrobial agent-8 shows anti-inflammatory activity against lipopolysaccharide-induced inflammation.

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Antimicrobial agent-8 Chemical Structure

Antimicrobial agent-8 Chemical Structure

CAS No. : 2978694-22-1

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Based on 1 publication(s) in Google Scholar

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Description

Antimicrobial agent-8 (Compound 15) is a potent antimicrobial agent, and shows potent antimicrobial activity with an MIC range of 2-8 μg/mL against Gram-negative and Gram-positive bacteria. Antimicrobial agent-8 shows anti-inflammatory activity against lipopolysaccharide-induced inflammation.

In Vitro

Antimicrobial agent-8 (2.8-56.4 μM; 24 h) inhibits Gram-negative bacteria and Gram-positive bacteria growth[1].
Antimicrobial agent-8 (5 and 20 μg/mL; 18 h) inhibits the production of nitric oxide (NO) and tumor necrosis factor-α (TNF-α) by lipopolysaccharide-stimulated in RAW 264.7 cells[1].
Antimicrobial agent-8 (1-32 μg/mL, 16 h; 8-128 μg/mL; 24 h) shows potent biofilm inhibitory (MBIC50=1 μg/mL) and eradicating activities (MBEC50=8 μg/mL) by MDRPA bacteria[1].
Antimicrobial agent-8 exhibits proteolytic resistance and salt/serum stability[1].
Antimicrobial agent-8 displays synergistic or additive effects when combined with selected clinically used antibiotics[1].

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

Cell Viability Assay[1]

Cell Line: E. coli [KCTC 1682], P. aeruginosa [KCTC 1637], S. epidermidis [KCTC 1917] and S. aureus [KCTC1621]
Concentration: 2.8-56.4 μM
Incubation Time: 24 hours
Result: Inhibited Gram-negative bacteria with MIC values of 5.4 μM for E. coli [KCTC 1682] and P. aeruginosa [KCTC 1637].
Inhibited Gram- positive bacteria with MIC values of 2.7 μM and 5.4 μM for S. epidermidis [KCTC 1917] and S. aureus [KCTC1621], respectively.

Cell Viability Assay[1]

Cell Line: RAW 264.7 macrophages
Concentration: 5 and 20 μg/mL
Incubation Time: 18 hours
Result: Observed LPS-stimulated production of NO with an inhibitory rate of 90.79% at 5 μg/mL.
Exhibited inhibitory effects on the LPS-stimulated production of TNF-α with an inhibitory rate of 95.4% at 20 μg/mL.
Molecular Weight

746.95

Formula

C39H54N16

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NCCN(C1=NC(NCC2=CC=CC=C2)=NC(N3CCN(C4=NC(NCC5=CC=CC=C5)=NC(N(CCN)CCN)=N4)C(CC6=CC=CC=C6)C3)=N1)CCN

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (133.88 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.3388 mL 6.6939 mL 13.3878 mL
5 mM 0.2678 mL 1.3388 mL 2.6776 mL
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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Volume (start)

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C2

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Volume (final)

V2

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.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: 2.5 mg/mL (3.35 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (3.35 mM); Clear solution; Need ultrasonic

    This protocol yields a clear solution of 2.5 mg/mL.

    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:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation
References

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
DMSO 1 mM 1.3388 mL 6.6939 mL 13.3878 mL 33.4694 mL
5 mM 0.2678 mL 1.3388 mL 2.6776 mL 6.6939 mL
10 mM 0.1339 mL 0.6694 mL 1.3388 mL 3.3469 mL
15 mM 0.0893 mL 0.4463 mL 0.8925 mL 2.2313 mL
20 mM 0.0669 mL 0.3347 mL 0.6694 mL 1.6735 mL
25 mM 0.0536 mL 0.2678 mL 0.5355 mL 1.3388 mL
30 mM 0.0446 mL 0.2231 mL 0.4463 mL 1.1156 mL
40 mM 0.0335 mL 0.1673 mL 0.3347 mL 0.8367 mL
50 mM 0.0268 mL 0.1339 mL 0.2678 mL 0.6694 mL
60 mM 0.0223 mL 0.1116 mL 0.2231 mL 0.5578 mL
80 mM 0.0167 mL 0.0837 mL 0.1673 mL 0.4184 mL
100 mM 0.0134 mL 0.0669 mL 0.1339 mL 0.3347 mL
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Antimicrobial agent-8 Related Classifications

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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Antimicrobial agent-8
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