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Polyquaternium-1  (Synonyms: Polidronium chloride)

目录号: HY-127032 纯度: ≥99.0%
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Polyquaternium-1 (Polidronium chloride; PQ-1) 是一种靶向细菌细胞膜的抗菌防腐剂和 NF-κB 通路激活剂。Polyquaternium-1 通过聚阳离子特性吸附于微生物膜表面,破坏膜完整性并诱导钾离子泄漏,导致细菌死亡。Polyquaternium-1 在 0.001% 浓度下即发挥抗菌作用,对哺乳动物细胞毒性较低。Polyquaternium-1 可用于制备如青光眼滴眼液 (含 PQ-1 的 Travoprost 制剂)、人工泪液及隐形眼镜护理液,以减少传统防腐剂 (如苯扎氯铵 (HY-B2232)) 的眼表毒性。

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Polyquaternium-1 Chemical Structure

Polyquaternium-1 Chemical Structure

CAS No. : 75345-27-6

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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].

体外研究
(In Vitro)

1. 细胞毒性与炎症反应
Polyquaternium-1 (0.001%;5-30 min+24 h 恢复) 可激活 NF-κB 相关炎症通路,在 HCE-2 人角膜上皮细胞中降低细胞活力 (下降 50% 左右),而 0.02% BAK (HY-B2232) 则引发全部细胞死亡。Polyquaternium-1 可增加 LDH 释放,并激活 NF-κB 通路,诱导 IL-6IL-8 分泌[1]
2. 防腐剂毒性对比
Polyquaternium-1 (0.001%;25 min-2 h) 与 0.015-0.02% BAK (HY-B2232) 相比,在人角膜和结膜细胞中,具有更低的细胞毒性,不会引起明显的细胞损伤或眼部刺激[2]

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.
体内研究
(In Vivo)

1. 兔角膜毒性实验
Polyquaternium-1 (0.001%;单次局部应用;保持 24 h) 与 0.02% BAK (HY-B2232) 相比,在新西兰白兔角膜模型中,对角膜跨上皮电阻 (TER) 无显著影响,角膜上皮细胞形态正常,微绒毛完整,未诱导明显炎症或细胞损伤[3]
2. 兔眼长期毒性实验
Polyquaternium-1 (0.001%;单次局部应用;每日 1 次;30 天) 与 BAK (HY-B2232) 相比,在日本白兔模型中对结膜杯状细胞密度无显著影响,角膜荧光素染色评分降低,泪膜破裂时间 (TFBUT) 延长[3]

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 号
性状

固体

颜色

Off-white to light yellow

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
细胞实验: 

H2O 中的溶解度 : 50 mg/mL (超声助溶)

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息:

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

由于实验过程有损耗,建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳,请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度,如有需要,请与 MCE 中国技术支持联系。
纯度 & 产品资料

纯度: ≥99.0%

参考文献

Polyquaternium-1 相关分类

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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