| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Polidronium chloride targets bacterial cell membranes. As a polycationic polymer, it adsorbs to the microbial membrane surface via electrostatic interactions. This binding disrupts membrane integrity and induces potassium ion leakage, leading to bacterial cell death. It is also an activator of the NF-κB pathway. Its mechanism is physical rather than specific receptor-mediated, which reduces the risk of resistance development.
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| ln Vitro |
Polidronium chloride demonstrates antimicrobial activity in vitro against a broad spectrum of bacteria and fungi. Its activity is assessed by standard antimicrobial susceptibility testing methods. The compound's polycationic nature and membrane-disrupting mechanism contribute to its broad-spectrum activity. It is used as a preservative in ophthalmic formulations to prevent microbial contamination.
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| ln Vivo |
Polidronium chloride is used as an ophthalmic preservative in multiple-dose topical medications. It is effective in suppressing the growth of microbial contaminants in eye drops and other ophthalmic products. It is commonly used in ophthalmic surgery. Its in vivo efficacy has been established through its use in commercial ophthalmic formulations. No systemic pharmacological effects are observed as it acts locally in the eye.
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| Enzyme Assay |
Antimicrobial activity assays are performed using standard broth microdilution or agar diffusion methods according to CLSI or USP guidelines. Bacterial and fungal strains (e.g., Pseudomonas aeruginosa, Staphylococcus aureus, Candida albicans) are cultured in appropriate media. Polidronium chloride is serially diluted and tested against the microorganisms. Minimum inhibitory concentrations (MICs) are determined. Time-kill assays are performed to assess bactericidal activity. Preservative efficacy testing is conducted according to USP <51> Antimicrobial Effectiveness Testing. Each assay includes appropriate quality control strains.
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| Cell Assay |
Polidronium chloride's antimicrobial activity is evaluated in cell-based assays using bacterial and fungal cultures. Standard microbiological methods are used to assess its ability to inhibit growth. The compound's mechanism of action on bacterial membranes can be studied using fluorescent membrane integrity probes (e.g., propidium iodide) and potassium leakage assays. For NF-κB activation studies, mammalian cell lines (e.g., HEK-293, macrophages) are treated with Polidronium chloride and NF-κB activation is measured by reporter assays or Western blotting for phosphorylated IκBα. Cell viability is assessed using MTT or LDH assays.
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| Animal Protocol |
In vivo studies with Polidronium chloride are primarily conducted as part of ophthalmic product safety and efficacy evaluations. The compound is formulated in eye drops and tested in animal models (rabbits) for ocular tolerance and preservative efficacy. Ocular irritation and toxicity are assessed by slit-lamp examination. Antimicrobial efficacy is evaluated by challenging the preserved formulation with microorganisms. The compound is also used in clinical ophthalmic products.
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| ADME/Pharmacokinetics |
Polidronium chloride has a molecular formula of C22H48Cl3N3O6. It is supplied as a solution with 46.5% active ingredients in H2O. Storage: typically at room temperature. As an ophthalmic preservative, it is not systemically absorbed in significant amounts. No systemic pharmacokinetic data are available. It acts locally in the eye.
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| Toxicity/Toxicokinetics |
Polidronium chloride is generally well-tolerated as an ophthalmic preservative. Ocular irritation may occur in sensitive individuals. It is not intended for systemic use. Standard toxicology studies have demonstrated an acceptable safety profile for ophthalmic use. It is approved for use as a preservative in ophthalmic formulations in many countries.
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| References | |
| Additional Infomation |
Polidronium chloride is a quaternary ammonium salt.
See also: Chlorinated polyphosphonic acid (note moved to). Polidronium chloride is also known as Polyquaternium-1 and PQ-1. It is a polycationic ophthalmic preservative that suppresses microbial growth in multiple-dose topical medications. It targets bacterial cell membranes and is an activator of NF-κB. It is commonly used in ophthalmic products and surgery. No clinical trials as a therapeutic agent have been reported. It is approved for use as a preservative. |
| Molecular Formula |
(C6H12N)NC16H36N2O6.3CL
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|---|---|
| Molecular Weight |
0.00000
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| Exact Mass |
555.26
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| CAS # |
75345-27-6
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| Related CAS # |
75345-27-6 (chloride);741204-38-6 (cation);
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| PubChem CID |
5282453
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
20
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| Heavy Atom Count |
34
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| Complexity |
424
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C[N+](C)(CC=CC[N+](CCO)(CCO)CCO)CC=CC[N+](CCO)(CCO)CCO.[Cl-].[Cl-].[Cl-]
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| InChi Key |
OTIWYSKRSMXGNK-VHJGTCNUSA-K
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| InChi Code |
InChI=1S/C22H48N3O6.3ClH/c1-23(2,7-3-5-9-24(11-17-26,12-18-27)13-19-28)8-4-6-10-25(14-20-29,15-21-30)16-22-31;;;/h3-6,26-31H,7-22H2,1-2H3;3*1H/q+3;;;/p-3/b5-3+,6-4+;;;
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| Chemical Name |
dimethyl-bis[(E)-4-[tris(2-hydroxyethyl)azaniumyl]but-2-enyl]azanium;trichloride
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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) |
H2O : ~100 mg/mL
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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.) |
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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