| Field | Specification |
|---|---|
| Alternative names | PMX 30063 tetrahydrochloride |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C40H54Cl4F6N14O6 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
Brilacidin tetrahydrochloride (PMX 30063 tetrahydrochloride) is an anti-infective antimicrobial with MIC90 values of 1 μg/mL against the Gram-positive bacterium Streptococcus pneumonia and 8 μg/mL against Streptococcus viridans, and MIC90 values of 8 μg/mL against the Gram-negative bacterium Haemophilus influenza and 4 μg/mL against Pseudomonas aeruginosa. It is a defensin-mimetic antibiotic compound[1][2]. It is supplied as an off-white to light yellow solid (C40H54Cl4F6N14O6, MW 1082.75) at 99.10% purity.
Physical & Chemical Properties
| CAS Number | 1224095-99-1 |
|---|---|
| Molecular Formula | C40H54Cl4F6N14O6 |
| Molecular Weight | 1082.75 g/mol |
| Purity | 99.10% |
| 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 |
| Signaling Pathway | Anti-infection |
| Solubility | In Vitro: DMSO: 83.33 mg/mL (76.96 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) Methanol: 10 mg/mL (9.24 mM; Requires sonication) |
| Storage | 4°C, sealed storage, away from moisture. In solvent: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 83.33 mg/mL (76.96 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
| Methanol | 10 mg/mL (9.24 mM) | requires sonication |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); sealed storage, away from moisture; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline |
|---|---|
| Result | ≥ 6.25 mg/mL (5.77 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 6.25 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (62.5 mg/mL) to 400 μL PEG300; then 50 μL Tween-80; then 450 μL saline to bring the volume to 1 mL. Saline: dissolve 0.9 g sodium chloride in ddH2O and make up to 100 mL. |
Protocol 2
| Composition | 10% DMSO + 90% (20% SBE-β-CD in saline) |
|---|---|
| Result | ≥ 6.25 mg/mL (5.77 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 6.25 mg/mL (saturation not determined). For 1 mL of working solution: add 100 μL DMSO stock (62.5 mg/mL) to 900 μL 20% SBE-β-CD in saline. 20% SBE-β-CD in saline: dissolve 2 g SBE-β-CD powder in 10 mL saline until clear (4°C, store up to one week). |
Protocol 3
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | ≥ 6.25 mg/mL (5.77 mM); clear solution |
| How to prepare | Gives a clear solution at ≥ 6.25 mg/mL (saturation not determined). Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (62.5 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
The lowest minimum inhibitory concentrations among the bacterial groups belong to both Staphylococcus aureus (SA) and Staphylococcus epidermidis (SE). Compared with SA and SE, the MIC90s of Brilacidin are 4, 32, 256, 32, 16, and 128-fold higher, respectively, against Streptococcus pneumonia (SP) and Streptococcus viridians (SV), Moraxella (MS) and Haemophilus influenza (HI), as well as Pseudomonas aeruginosa (PA) and Serratia marcescens (SM). Brilacidin has Gram-positive in vitro activity, and topical Brilacidin 0.5% is minimally irritating. In a methicillin-resistant S. aureus (MRSA) keratitis model with the corneal epithelium removed, Brilacidin 0.5% showed efficacy equal to that of Vancomycin (VAN). Brilacidin acts mainly on the bacterial cell membrane through depolarization. Brilacidin is more potent against Gram-positive bacteria (except SV) than against Gram-negative bacteria[2].
In Vivo
In the NZW rabbit ocular toxicity model, Brilacidin shows dose-dependent ocular toxicity after 7 topical instillations (every 30 min for 3 h). Based on Maximum mean total scores (MMTS), Brilacidin 1% (23.0) is rated Mildly Irritating; Brilacidin 0.5% (6.5) and Brilacidin 0.25% (4.0) are rated Minimally Irritating; Brilacidin 0.1% (2.0) and TBS (1.0) are rated Practically Nonirritating; and 0.01% Brilacidin (0.5) is rated Nonirritating[2].
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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A novel peptide mimetic, brilacidin, for combating multidrug-resistant Neisseria gonorrhoeae. PLoS One 2025 Jun 5;20(6):e0325722. PMID: 40471977
