2. Anti-infection
  3. Bacterial Antibiotic
  4. Brilacidin tetrahydrochloride

Brilacidin tetrahydrochloride  (Synonyms: PMX 30063 tetrahydrochloride)

Cat. No.: HY-19892A Purity: 98.75%
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Brilacidin tetrahydrochloride (PMX 30063 tetrahydrochloride) is an anti-infective antimicrobial with MIC90s of 1 and 8 μg/mL for Gram-positive bacteria Streptococcus pneumonia and Streptococcus viridans, and MIC90 of 8 and 4 μg/mL for Gram-negative bacteria Haemophilus influenza and Pseudomonas aeruginosa. Brilacidin tetrahydrochloride is a defensin mimetic antibiotic compound.

For research use only. We do not sell to patients.

Brilacidin tetrahydrochloride Chemical Structure

Brilacidin tetrahydrochloride Chemical Structure

CAS No. : 1224095-99-1

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Based on 1 publication(s) in Google Scholar

Other Forms of Brilacidin tetrahydrochloride:

Brilacidin tetrahydrochloride Related Antibodies

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Description

Brilacidin tetrahydrochloride (PMX 30063 tetrahydrochloride) is an anti-infective antimicrobial with MIC90s of 1 and 8 μg/mL for Gram-positive bacteria Streptococcus pneumonia and Streptococcus viridans, and MIC90 of 8 and 4 μg/mL for Gram-negative bacteria Haemophilus influenza and Pseudomonas aeruginosa. Brilacidin tetrahydrochloride is a defensin mimetic antibiotic compound[1][2].

In Vitro

Both Staphylococcus aureus (SA) and Staphylococcus epidermidis (SE) have the lowest minimum inhibitory concentrations among the bacterial groups. The MIC90s to Brilacidin for Streptococcus pneumonia (SP), Streptococcus viridians (SV), Moraxella (MS), Haemophilus influenza (HI), Pseudomonas aeruginosa (PA), and Serratia marcescens (SM) are 4, 32, 256, 32, 16, and 128-fold higher, respectively, than SA and SE. Brilacidin has Gram-positive in vitro activity; topical Brilacidin 0.5% is minimally irritating; and Brilacidin 0.5% was equally efficacious as Vancomycin (VAN) in a methicillin-resistant S. aureus (MRSA) keratitis model when the corneal epithelium is removed. Brilacidin acts primarily on the bacterial cell membrane by depolarization. Brilacidin is more potent for Gram-positive bacteria (except SV) than Gram-negative bacteria[2].

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

Brilacidin tetrahydrochloride Related Antibodies
In Vivo

Brilacidin demonstrates dose-dependent ocular toxicity after 7 topical instillations (every 30 min for 3 h) in the NZW rabbit ocular toxicity model. Brilacidin 1% is determined to be Mildly Irritating (23.0), Brilacidin 0.5% (6.5), and Brilacidin 0.25% (4.0) are determined to be Minimally Irritating, while Brilacidin 0.1% (2.0) and TBS (1.0) are determined to be Practically Nonirritating and 0.01% Brilacidin (0.5) is determined to be Nonirritating based on their Maximum mean total scores (MMTS) values[2].

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

1082.75

Formula

C40H54Cl4F6N14O6
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

O=C(C1=NC=NC(C(NC2=CC(C(F)(F)F)=CC(NC(CCCCNC(N)=N)=O)=C2O[C@H]3CNCC3)=O)=C1)NC4=CC(C(F)(F)F)=CC(NC(CCCCNC(N)=N)=O)=C4O[C@H]5CNCC5.Cl.Cl.Cl.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 83.33 mg/mL (76.96 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Methanol : 10 mg/mL (9.24 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.9236 mL 4.6179 mL 9.2357 mL
5 mM 0.1847 mL 0.9236 mL 1.8471 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
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: ≥ 6.25 mg/mL (5.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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: ≥ 6.25 mg/mL (5.77 mM); Clear solution

    This protocol yields a clear solution of ≥ 6.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (62.5 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).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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 (sealed storage, away from moisture). 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
Methanol / DMSO 1 mM 0.9236 mL 4.6179 mL 9.2357 mL 23.0894 mL
5 mM 0.1847 mL 0.9236 mL 1.8471 mL 4.6179 mL
DMSO 10 mM 0.0924 mL 0.4618 mL 0.9236 mL 2.3089 mL
15 mM 0.0616 mL 0.3079 mL 0.6157 mL 1.5393 mL
20 mM 0.0462 mL 0.2309 mL 0.4618 mL 1.1545 mL
25 mM 0.0369 mL 0.1847 mL 0.3694 mL 0.9236 mL
30 mM 0.0308 mL 0.1539 mL 0.3079 mL 0.7696 mL
40 mM 0.0231 mL 0.1154 mL 0.2309 mL 0.5772 mL
50 mM 0.0185 mL 0.0924 mL 0.1847 mL 0.4618 mL
60 mM 0.0154 mL 0.0770 mL 0.1539 mL 0.3848 mL
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Brilacidin tetrahydrochloride 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.

Keywords:

Brilacidin tetrahydrochloride1224095-99-1PMX 30063 tetrahydrochlorideBacterialAntibioticInhibitorinhibitorinhibit

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