| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Exeporfinium targets bacterial cell membranes through a membrane-active mechanism. It acts as a membrane-perturbing agent that weakens bacterial cell walls without causing lysis. The compound is equally effective against antibiotic-resistant isolates as antibiotic-sensitive isolates, indicating that its mechanism of action is not affected by common resistance mechanisms. Exeporfinium has a low propensity for engendering bacterial resistance, which is a significant advantage over conventional antibiotics. The compound's dicationic porphyrin structure facilitates interaction with bacterial membranes, leading to disruption of membrane integrity and cell death.
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| ln Vitro |
In vitro, exeporfinium demonstrates potent bactericidal activity against Staphylococcus aureus, including both methicillin-sensitive and methicillin-resistant strains. The minimum inhibitory concentration (MIC) of exeporfinium is determined using broth microdilution methods following Clinical and Laboratory Standards Institute (CLSI) guidelines. The compound is rapidly bactericidal, with activity observed within minutes of exposure. Exeporfinium is equally effective against antibiotic-resistant isolates as antibiotic-sensitive isolates, with no significant difference in MIC values. The compound also shows activity against Clostridium difficile. The low resistance potential of exeporfinium has been demonstrated in serial passage experiments, where resistance development was not observed.
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| ln Vivo |
In vivo, exeporfinium chloride nasal gel has been evaluated in a randomized, placebo-controlled Phase 2 study in cardiac surgery patients. The study demonstrated that exeporfinium nasal gel significantly reduces Staphylococcus aureus nasal carriage throughout surgery and the early recovery period. The compound's rapid bactericidal activity and low resistance potential make it particularly attractive for prophylaxis in high-risk patient populations. Exeporfinium is also being evaluated for the treatment of Clostridium difficile infection. The compound's topical formulation allows for targeted delivery to the site of infection.
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| Enzyme Assay |
Exeporfinium's antibacterial activity is assessed using MIC determination by broth microdilution methods. Bacterial cultures are incubated with varying concentrations of exeporfinium; growth inhibition is measured by optical density or colony counting. Time-kill assays are performed to characterize the bactericidal kinetics of the compound. Membrane disruption is assessed using fluorescent dyes or by measuring leakage of intracellular contents. These assays provide mechanistic insights into the antibacterial activity of exeporfinium.
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| Cell Assay |
Exeporfinium is tested on cultured bacterial cells, including Staphylococcus aureus (both MSSA and MRSA) and Clostridium difficile. Bacterial cells are treated with varying concentrations of exeporfinium; growth inhibition is measured by optical density; viability is assessed by colony counting; membrane integrity is assessed using fluorescent probes (e.g., SYTOX Green, propidium iodide). These cell-based assays demonstrate the potent bactericidal activity and membrane-disrupting mechanism of exeporfinium.
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| Animal Protocol |
Exeporfinium has been evaluated in animal models and human clinical trials. In preclinical studies, exeporfinium was tested in mouse models of MRSA infection, demonstrating dose-dependent reduction in bacterial burden. The compound has been evaluated in a Phase 2 clinical trial as a nasal gel for reducing S. aureus nasal carriage in cardiac surgery patients. In this study, exeporfinium significantly reduced nasal carriage compared to placebo. Additional clinical trials are ongoing to evaluate the compound in other indications including C. difficile infection.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of exeporfinium have been conducted in preclinical species and humans. When administered topically as a nasal gel, exeporfinium achieves high local concentrations at the site of application with minimal systemic absorption. This pharmacokinetic profile is advantageous for topical antimicrobial therapy, as it allows for potent local activity while minimizing systemic exposure and potential toxicity. The compound's systemic pharmacokinetics following other routes of administration have not been extensively reported.
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| Toxicity/Toxicokinetics |
In clinical studies, exeporfinium nasal gel has been shown to be well-tolerated. Local adverse effects are mild and transient, including nasal irritation and discomfort. Systemic adverse effects are uncommon due to minimal systemic absorption. The safety profile of exeporfinium is consistent with its mechanism of action as a topical antimicrobial agent. Long-term safety data is being collected as part of ongoing clinical development.
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| References |
:Antimicrob Agents Chemother. 2011 Mar;55(3):1177-81.
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| Additional Infomation |
Exeporfinium (XF-73) is a dicationic porphyrin derivative with potent bactericidal activity against Gram-positive pathogens including MRSA and C. difficile. The compound has a novel mechanism of action—membrane perturbation without lysis—and a low propensity for engendering bacterial resistance. Exeporfinium has been evaluated in a Phase 2 clinical trial as a nasal gel for reducing S. aureus nasal carriage in cardiac surgery patients. The compound is also being developed for the treatment of C. difficile infection. Exeporfinium represents a promising new class of antimicrobial agents for addressing the growing problem of antibiotic-resistant infections. The compound's rapid bactericidal activity, broad spectrum of activity, and low resistance potential make it a valuable addition to the antimicrobial armamentarium.
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| Molecular Formula |
C44H50BR2N6O2
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|---|---|
| Molecular Weight |
854.73
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| Exact Mass |
694.3984
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| Elemental Analysis |
C, 61.83; H, 5.90; Br, 18.70; N, 9.83; O, 3.74
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| CAS # |
943326-71-4
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| Related CAS # |
756818-36-7 (cation);718638-68-7 (Cl);943326-71-4 (bromide);
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| Appearance |
Solid powder
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| InChi Key |
OOOQIWWDNZLZQQ-XRFOENPRSA-L
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| InChi Code |
InChI=1S/C44H50N6O2.2BrH/c1-49(2,3)25-7-27-51-37-17-9-31(10-18-37)43-39-21-13-33(45-39)29-35-15-23-41(47-35)44(42-24-16-36(48-42)30-34-14-22-40(43)46-34)32-11-19-38(20-12-32)52-28-8-26-50(4,5)6/h9-24,29-30,45,48H,7-8,25-28H2,1-6H32*1H/q+2/p-2/b33-29-,34-30-,35-29-,36-30-,43-39-,43-40-,44-41-,44-42-
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| Chemical Name |
3,3'-((porphyrin-5,15-diylbis(4,1-phenylene))bis(oxy))bis(N,N,N-trimethylpropan-1-aminium) dibromide
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| Synonyms |
XF73 XF 73 XF-73
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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 |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1700 mL | 5.8498 mL | 11.6996 mL | |
| 5 mM | 0.2340 mL | 1.1700 mL | 2.3399 mL | |
| 10 mM | 0.1170 mL | 0.5850 mL | 1.1700 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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