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

Brilacidin tetrahydrochloride (Synonyms: PMX 30063 tetrahydrochloride)

Cat. No.: HY-19892A Purity: 99.35%
Handling Instructions

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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1 mg USD 300 In-stock
Estimated Time of Arrival: December 31
5 mg USD 620 In-stock
Estimated Time of Arrival: December 31
10 mg USD 980 In-stock
Estimated Time of Arrival: December 31
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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].

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].

Molecular Weight

1082.75

Formula

C₄₀H₅₄Cl₄F₆N₁₄O₆

CAS No.

1224095-99-1

SMILES

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

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 : 83.33 mg/mL (76.96 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
10 mM 0.0924 mL 0.4618 mL 0.9236 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

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

*All of the co-solvents are provided by MCE.
References
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Keywords:

Brilacidin tetrahydrochloridePMX 30063 tetrahydrochlorideBacterialAntibioticInhibitorinhibitorinhibit

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Brilacidin tetrahydrochloride
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