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Polyquaternium-1  (Synonyms: Polidronium chloride)

Cat. No.: HY-127032 Purity: ≥99.0%
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Polyquaternium-1 (Polidronium chloride; PQ-1) is an antimicrobial preservative and an activator of NF-κB. Polyquaternium-1 targets bacterial cell membranes, commonly used in ophthalmic surgery. Polyquaternium-1 adsorbs to the surface of microbial membranes through its polycationic properties, destroying membrane integrity and inducing potassium ion leakage, leading to bacterial death. Polyquaternium-1 exerts antimicrobial effects at a concentration of 0.001% and has low toxicity to mammalian cells. Polyquaternium-1 can be used to prepare products such as glaucoma eye drops (Travoprost preparations containing PQ-1), artificial tears, and contact lens solutions to reduce the ocular surface toxicity of traditional preservatives such as benzalkonium chloride (HY-B2232).

For research use only. We do not sell to patients.

Polyquaternium-1 Chemical Structure

Polyquaternium-1 Chemical Structure

CAS No. : 75345-27-6

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Based on 1 publication(s) in Google Scholar

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Description

Polyquaternium-1 (Polidronium chloride; PQ-1) is an antimicrobial preservative and an activator of NF-κB. Polyquaternium-1 targets bacterial cell membranes, commonly used in ophthalmic surgery. Polyquaternium-1 adsorbs to the surface of microbial membranes through its polycationic properties, destroying membrane integrity and inducing potassium ion leakage, leading to bacterial death. Polyquaternium-1 exerts antimicrobial effects at a concentration of 0.001% and has low toxicity to mammalian cells. Polyquaternium-1 can be used to prepare products such as glaucoma eye drops (Travoprost preparations containing PQ-1), artificial tears, and contact lens solutions to reduce the ocular surface toxicity of traditional preservatives such as benzalkonium chloride (HY-B2232)[1][2][3].

In Vitro

1. Cytotoxicity and inflammatory response:
Polyquaternium-1 (0.001%; ​​5-30 min + 24 h recovery) activates the NF-κB-related inflammatory pathway and reduces cell viability in HCE-2 human corneal epithelial cells (by about 50%), while 0.02% BAK (HY-B2232) induces all cell death. Polyquaternium-1 increases LDH release and activates the NF-κB pathway, enhances IL-6 and IL-8 secretion[1].
2. Comparison of preservative toxicity:
Compared with 0.015-0.02% BAK (HY-B2232), Polyquaternium-1 (0.001%; ​​25 min-2 h) has lower cytotoxicity in human corneal and conjunctival cells and does not cause significant cell damage or eye irritation[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: HCE-2 human corneal epithelial cells
Concentration: 0.001%
Incubation Time: 5, 15, 30 min exposure + 24 h recovery for viability; 6 h for NF-κB assay
Result: Showed 50% viability reduction at 30 min exposure, with LDH release increased 6-fold compared to control.
Moderately elevated Caspase-3 activity (1.5-fold) after 15 min exposure, but without statistically significant.
Increased IL-6 and IL-8 levels by 3-8-fold and 1.5-3.5-fold, respectively, with NF-κB DNA binding significantly upregulated in nuclear extracts after 30 min exposure.
In Vivo

1. Rabbit corneal toxicity test:
Compared with 0.02% BAK (HY-B2232), Polyquaternium-1 (0.001%; ​​single topical application; maintained for 24 h) has no significant effect on corneal transepithelial electrical resistance (TER) in the New Zealand white rabbit corneal model, and the corneal epithelial cells has normal morphology and intact microvilli, without inducing obvious inflammation or cell damage[3].
2. Rabbit eye long-term toxicity test:
Compared with BAK (HY-B2232), Polyquaternium-1 (0.001%; ​​single topical application; once a day; 30 days) has no significant effect on conjunctival goblet cell density in the Japanese white rabbit model, but reduces corneal fluorescein staining scores and prolongs tear film break-up time (TFBUT)[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: New Zealand White rabbits (male, 2.5-3.0 kg, 6-8 weeks old) with ex vivo corneal TER measurement and SEM analysis[3]
Dosage: 0.001%, in Travoprost/timolol solution (aqueous gel).
Administration: Topical application (1 mL), single 60-second exposure followed by 24 h recovery.
Result: Preserved corneal TER at 82.2% of baseline, comparable to HBSS control (101.3%), while 0.02% BAK in latanoprost/timolol reduced TER to 15.6%.
Reminded normal superficial corneal cells with intact microvilli in SEM results, whereas BAK group showed damaged cells with degenerated microvilli.
Animal Model: Japanese white rabbits (3.0-4.0 kg) with chronic topical dosing[3]
Dosage: 0.001%, in artificial tears or glaucoma formulations (aqueous solution).
Administration: Daily instillation for 30 days, 1 drop/eye, once daily.
Result: Preserved goblet cell density (18.8 cells/0.01 mm2) similar to control (21.6 cells), while 0.1% BAK reduced density to 6.0 cells.
Decreased corneal fluorescein staining scores from 4.93 to 3.27, and increased TFBUT from 6.74 to 8.92 seconds, indicating improved tear film stability.
Clinical Trial
Formula

C22H48Cl3N3O6

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OCC[N+](CCO)(C/C=C/C[N+](C)(C/C=C/C[N+](CCO)(CCO)CCO)C)CCO.[3 Cl-].[n]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 50 mg/mL (Need ultrasonic)

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This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: ≥99.0%

References
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Polyquaternium-1 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Polyquaternium-1
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HY-127032
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