| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| Other Sizes |
| Targets |
Bacterial cell membrane. Brilacidin acts primarily on the bacterial cell membrane by depolarization. It does not target a specific protein receptor but disrupts membrane integrity through a mechanism similar to host defense peptides.
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| ln Vitro |
Among the bacterial species, Staphylococcus aureus (SA) and Staphylococcus epidermidis (SE) have the lowest minimum inhibitory concentrations. Brilacidin's MIC90s for Serratia marcescens (SM), Moraxella (MS), Haemophilus influenza (HI), Pseudomonas aeruginosa (PA), Streptococcus pneumonia (SP), and Streptococcus viridians (SV) are 128-fold higher than those of SA and SE, respectively, at 4, 32, 256, 32, 16, and 16. In vitro, brilacidin possesses Gram-positive activity. Topical application of brilacidin 0.5% causes minimal irritation. When the corneal epithelium is removed from a methicillin-resistant S. aureus (MRSA) keratitis model, brilacidin 0.5% proved to be just as effective as vancomycin (VAN). Brilacidin mainly depolarizes the bacterial cell membrane in order to affect it. Compared to Gram-negative bacteria, brinalacidin is more effective against Gram-positive bacteria (apart from SV)[2].
In vitro, Brilacidin shows MIC₉₀ values of 1 and 8 μg/mL for Gram-positive bacteria Streptococcus pneumoniae and Streptococcus viridans, and MIC₉₀ of 8 and 4 μg/mL for Gram-negative bacteria Haemophilus influenzae and Pseudomonas aeruginosa. It is more potent against Gram-positive bacteria (except S. viridans) than Gram-negative bacteria. Staphylococcus aureus and Staphylococcus epidermidis show the lowest MICs among tested bacteria. Topical Brilacidin 0.5% is minimally irritating. |
| ln Vivo |
In the NZW rabbit ocular toxicity model, brinalacidin exhibits dose-dependent ocular toxicity following seven topical instillations (every 30 minutes for three hours). Based on their Maximum mean total scores (MMTS) values, Brilacidin 1% is found to be Mildly Irritating (23.0), Brilacidin 0.5% (6.5), and Brilacidin 0.25% (4.0) to be Minimally Irritating, while Brilacidin 0.1% (2.0), TBS (1.0), and 0.01% Brilacidin (0.5) are found to be Practically Nonirritating and Nonirritating, respectively[2].
In a methicillin-resistant S. aureus (MRSA) keratitis model, topical Brilacidin 0.5% was equally efficacious as Vancomycin when the corneal epithelium was removed. This demonstrates in vivo efficacy against drug-resistant bacterial infections in a relevant ocular infection model. |
| Enzyme Assay |
Non-cell assays for Brilacidin focus on membrane disruption mechanisms rather than specific receptor binding. Artificial membrane models such as liposomes or planar lipid bilayers are used to assess membrane depolarization and permeability changes. Fluorescent dye leakage assays are performed using calcein-loaded liposomes incubated with Brilacidin at concentrations of 0.1-100 μg/mL. Membrane depolarization is measured using potential-sensitive dyes in a fluorometric plate reader.
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| Cell Assay |
Cellular assays are performed using standard broth microdilution methods. Bacterial strains are cultured in appropriate media, and inocula are prepared at 5×10⁵ CFU/mL. Two-fold serial dilutions of Brilacidin (0.125-256 μg/mL) are prepared in 96-well plates. After 18-24 hours of incubation at 37°C, MIC values are determined. Time-kill assays are performed to assess bactericidal kinetics. Eukaryotic cell cytotoxicity is evaluated using mammalian cell lines (e.g., HaCaT keratinocytes) with MTT assays.
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| Animal Protocol |
In vivo efficacy is evaluated in murine models of infection. For the MRSA keratitis model, mice are infected topically with MRSA and treated with Brilacidin 0.5% ophthalmic solution or Vancomycin control. Corneal opacity and bacterial burden are assessed. Other models include wound infections and systemic infection models where Brilacidin is administered intraperitoneally or intravenously. Survival and bacterial clearance are measured.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies have been conducted in animal models. Brilacidin is typically administered intravenously or topically. Following topical application, systemic absorption is minimal. After intravenous administration, the compound is distributed to tissues and eliminated primarily via renal excretion. The half-life is relatively short, requiring multiple daily dosing for systemic infections in preclinical studies.
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| Toxicity/Toxicokinetics |
In preclinical toxicology studies, Brilacidin shows a favorable safety profile. Topical Brilacidin 0.5% is minimally irritating to tissues. Systemic toxicity at high doses includes potential effects on renal function and electrolyte balance due to membrane activity. No significant genotoxicity has been reported. Standard toxicology studies would be required for therapeutic development.
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| References |
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| Additional Infomation |
Brilacidin is a synthetic antimicrobial peptide mimetic that has gained attention for its broad-spectrum activity against various pathogens, including drug-resistant bacteria. It is a promising candidate for the development of new antibiotics. The compound's mechanism involves bacterial membrane depolarization. Brilacidin has been investigated in clinical trials for the treatment of oral mucositis and bacterial infections. It is not yet approved for clinical use but has shown efficacy in Phase 2 trials.
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| Molecular Formula |
C40H54CL4F6N14O6
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|---|---|
| Molecular Weight |
1082.7494
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| Exact Mass |
1080.3
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| Elemental Analysis |
C, 44.37; H, 5.03; Cl, 13.10; F, 10.53; N, 18.11; O, 8.87
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| CAS # |
1224095-99-1
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| Related CAS # |
Brilacidin;1224095-98-0
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| PubChem CID |
45275360
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
11.687
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
70
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| Complexity |
1560
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| Defined Atom Stereocenter Count |
2
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| SMILES |
Cl[H].Cl[H].Cl[H].Cl[H].FC(C1C([H])=C(C(=C(C=1[H])N([H])C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])/N=C(\N([H])[H])/N([H])[H])=O)O[C@@]1([H])C([H])([H])N([H])C([H])([H])C1([H])[H])N([H])C(C1=C([H])C(C(N([H])C2=C([H])C(C(F)(F)F)=C([H])C(=C2O[C@@]2([H])C([H])([H])N([H])C([H])([H])C2([H])[H])N([H])C(C([H])([H])C([H])([H])C([H])([H])C([H])([H])/N=C(\N([H])[H])/N([H])[H])=O)=O)=NC([H])=N1)=O)(F)F
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| InChi Key |
QTHBCQCKYVOFDR-PIJQHSLXSA-N
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| InChi Code |
InChI=1S/C40H50F6N14O6.4ClH/c41-39(42,43)21-13-25(57-31(61)5-1-3-9-53-37(47)48)33(65-23-7-11-51-18-23)27(15-21)59-35(63)29-17-30(56-20-55-29)36(64)60-28-16-22(40(44,45)46)14-26(34(28)66-24-8-12-52-19-24)58-32(62)6-2-4-10-54-38(49)50;;;;/h13-17,20,23-24,51-52H,1-12,18-19H2,(H,57,61)(H,58,62)(H,59,63)(H,60,64)(H4,47,48,53)(H4,49,50,54);4*1H/t23-,24-;;;;/m1..../s1
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| Chemical Name |
N4,N6-bis(3-(5-guanidinopentanamido)-2-(((R)-pyrrolidin-3-yl)oxy)-5-(trifluoromethyl)phenyl)pyrimidine-4,6-dicarboxamide tetrahydrochloride
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| Synonyms |
PMX30063; PMX-30063; PMX 30063; Brilacidin; Brilacidin HCl; Brilacidin tetrahydrochloride;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~76.96 mM )
Methanol : ~10 mg/mL (~9.24 mM ) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (5.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (5.77 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 6.25 mg/mL (5.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 10% DMSO+40% PEG300+5% Tween-80+45% Saline: ≥ 6.25 mg/mL (5.77 mM) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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