PQ-10
(Synonyms: 6,7-二甲氧基-4-[(3R)-3-(2-喹喔啉基氧基)-1-吡咯烷基]喹唑啉) 目录号 : GC44673
A selective PDE10 inhibitor
Cas No.:927691-21-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PQ-10 is a potent and selective inhibitor of phosphodiesterase type 10 (PDE10; Ki = 4 nM). It has >38-fold selectivity for PDE10 over a panel of 60 CNS-associated receptors, enzymes, and ion channels in vitro. Subcutaneous injection of PQ-10 (32 mg/kg) leads to increases in striatal cGMP and phosphorylation of cAMP response element binding protein (CREB) in murine striatum, known markers of in vivo PDE10 inhibition. PQ-10 at a dose of 0.3 mg/kg, p.o., reduces scopolamine- and MK-801-induced memory deficits in rats. PQ-10 also inhibits tumor cell growth with IC50 values of 0.29 and 0.22 mM for HCT116 and SW480 colon cancer cells, respectively.
| Cas No. | 927691-21-2 | SDF | |
| 别名 | 6,7-二甲氧基-4-[(3R)-3-(2-喹喔啉基氧基)-1-吡咯烷基]喹唑啉 | ||
| Canonical SMILES | COC1=CC2=C(C(N3CC[C@@H](OC4=NC(C=CC=C5)=C5N=C4)C3)=NC=N2)C=C1OC | ||
| 分子式 | C22H21N5O3 | 分子量 | 403.4 |
| 溶解度 | DMF: 25 mg/mL,DMF:PBS (pH 7.2) (1:20): 0.04 mg/mL,DMSO: 16 mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4789 mL | 12.3946 mL | 24.7893 mL |
| 5 mM | 0.4958 mL | 2.4789 mL | 4.9579 mL |
| 10 mM | 0.2479 mL | 1.2395 mL | 2.4789 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Detecting Levels of Polyquaternium-10 (PQ-10) via Potentiometric Titration with Dextran Sulphate and Monitoring the Equivalence Point with a Polymeric Membrane-Based Polyion Sensor
Anal Methods 2016 Aug 7;8(29):5806-5811.PMID:28018490DOI:10.1039/C6AY01748G.
Polymeric quaternary ammonium salts (polyquaterniums) have found increasing use in industrial and cosmetic applications in recent years. More specifically, polyquaternium-10 (PQ-10) is routinely used in cosmetic applications as a conditioner in personal care product formulations. Herein, we demonstrate the use of potentiometric polyion-sensitive polymeric membrane-based electrodes to quantify PQ-10 levels. Mixtures containing both PQ-10 and sodium lauryl sulfate (SLS) are used as model samples to illustrate this new method. SLS is often present in cosmetic samples that contain PQ-10 (e.g., shampoos, etc.) and this surfactant species interferes with the polyion sensor detection chemistry. However, it is shown here that SLS can be readily separated from the PQ-10/SLS mixture by use of an anion-exchange resin and that the PQ-10 can then be titrated with dextran sulphate (DS). This titration is monitored by potentiometric polyanion sensors to provide equivalence points that are directly proportional to PQ-10 concentrations.
Adsorption isotherms of Polyquaternium-10 polymers by activated sludge solids
Chemosphere 2022 Nov;307(Pt 2):135891.PMID:35926742DOI:10.1016/j.chemosphere.2022.135891.
Polymeric quaternary ammonium salts (polyquaternium-10 polymers, PQ-10) are extensively used as components of hair care products, lotions, and makeup and, therefore, are present in domestic sewage. Adsorption of these polymers by activated sludge was assessed to evaluate their removal by a commonly used wastewater treatment process. Activated sludge solids (ASS) were dosed with PQ-10 polymers with relatively high molecular mass (JR-125 and JR-30 M) and relatively low molecular mass (LR-400 and LR-30 M) and equilibrated for 2 h at 20 ± 2 °C. After equilibration, the vessels with the mixtures were centrifuged and the supernatants were analyzed with a phenol method. The relationships between dosed amounts and equilibrium concentrations in the aqueous phase (dose-response curves) for each tested polymer indicated that at relatively low dosing solution concentrations were negligible ("total adsorption" region of the dose-response curve). Light absorbance of the samples prepared for determination of polymer concentration using a phenol method within this region was close to the absorbance of the blank (0 μg (a.i.)/mL) or below absorbance of the blank, resulting in calculated concentrations apparently below zero. At some level of dosing, a subsequent increase in polymer dosage resulted in a quantifiable increase in solution concentration ("solution concentration rising" region). The relationships between concentrations of the polymers in the aqueous phase and concentrations of adsorbed polymers (adsorption isotherms) were non-linear. The ability of activated sludge solids to bind tested polymers may be characterized by apparent "threshold values" of the loading for each polymer. Below the "threshold value," solution concentration of the polymer is close to zero and above this value it becomes measurable. "Threshold loading" for all polymers was from 50 to 100 mg (a.i.)/g, far above concentrations of these compounds expected to be present in the sewage.
Inhibition of phoshodiesterase type 2 or type 10 reverses object memory deficits induced by scopolamine or MK-801
Behav Brain Res 2013 Jan 1;236(1):16-22.PMID:22951181DOI:10.1016/j.bbr.2012.08.019.
The objective of this study was to assess the effects of phosphodiesterase type 2 (PDE2) and type 10 (PDE10) inhibition on memory function in the object recognition task using the scopolamine- and MK-801-induced memory deficit model. The effects of the PDE2 inhibitor BAY 60-7550 and the PDE10 inhibitor PQ-10 on object recognition performance were investigated in the scopolamine (0.1mg/kg, i.p.) or MK-801 (0.125 mg/kg, i.p.) model. BAY 60-7550 was tested at a dose of 0.3-3mg/kg (p.o.) in both models; PQ-10 was tested at doses of 0.1-1mg/kg (p.o.) in the scopolamine model and 0.3-3mg/kg in the MK-801 model. All compounds were injected 30 min before the learning trial. Both BAY 60-7550 (1mg/kg) and PQ-10 (0.3mg/kg) attenuated the scopolamine-induced memory deficit. The MK-801-induced memory deficit was reversed after treatment with each PDE inhibitor at a dose of 1mg/kg or higher. PQ10 was highly brain penetrant, whereas 60-7550 levels in the brain were very low after oral treatment. We concluded that since BAY 60-7550 and PQ10 reversed both scopolamine- and MK-801-induced memory deficits, this supports the notion that dual substrate PDE inhibitors might be suitable candidates for cognition enhancement.
Understanding Ecotoxicological Responses of Fish Embryos and Gill Cells to Cationic Polymers
Environ Toxicol Chem 2022 Sep;41(9):2259-2272.PMID:35703088DOI:10.1002/etc.5410.
Cationic polymers are considered by the scientific and regulatory communities as a group of greater interest amongst the polymers in commerce. As a category, relatively little hazard information is available in the public literature. Very few examples exist of published, high-quality polymer characterization and quantification of exposure. In the present study we describe a series of fish embryo toxicity (FET) and fish gill cytotoxicity assays used to establish a baseline understanding of several representative polyquaternium categories (PQ-6, PQ-10, PQ-16) in animal alternative models, accompanied by high-quality analytical characterization. Materials were chosen to encompass a range of molecular weights and charge densities to determine the influence of test material characteristics on toxicity. Both chorionated and dechorionated FET assays were generally similar to published acute fish toxicity data. Toxicity was correlated with cationic polymer charge density, and not with molecular weight, and was a combination of physical effects and likely toxicity at the site of action. Toxicity could be ameliorated by humic acid in a dose-dependent manner. Fish gill cytotoxicity results were orders of magnitude less sensitive than FET test responses. Environ Toxicol Chem 2022;41:2259-2272. © 2022 SETAC.
Physicochemical and transfection properties of cationic Hydroxyethylcellulose/DNA nanoparticles
Biomacromolecules 2006 Oct;7(10):2856-62.PMID:17025362DOI:10.1021/bm060474b.
In this study the physicochemical and transfection properties of cationic hydroxyethylcellulose/plasmid DNA (pDNA) nanoparticles were investigated and compared with the properties of DNA nanoparticles based on polyethylene imine (PEI), which is widely investigated as a gene carrier. The two types of cationic hydroxyethylcelluloses studied, polyquaternium-4 (PQ-4) and polyquaternium-10 (PQ-10), are already commonly used in cosmetic and topical drug delivery devices. Both PQ-4 and PQ-10 spontaneously interact with pDNA with the formation of nanoparticles approximately 200 nm in size. Gel electrophoresis and fluorescence dequenching experiments indicated that the interactions between pDNA and the cationic celluloses were stronger than those between pDNA and PEI. The cationic cellulose/pDNA nanoparticles transfected cells to a much lesser extent than the PEI-based pDNA nanoparticles. The low transfection property of the PQ-4/pDNA nanoparticles was attributed to their neutrally charged surface, which does not allow an optimal binding of PQ-4/pDNA nanoparticles to cellular membranes. Although the PQ-10/pDNA nanoparticles were positively charged and thus expected to be taken up by cells, they were also much less efficient in transfecting cells than were PEI/pDNA nanoparticles. Agents known to enhance the endosomal escape were not able to improve the transfection properties of PQ-10/pDNA nanoparticles, indicating that a poor endosomal escape is, most likely, not the major reason for the low transfection activity of PQ-10/pDNA nanoparticles. We hypothesized that the strong binding of pDNA to PQ-10 prohibits the release of pDNA from PQ-10 once the PQ-10/pDNA nanoparticles arrive in the cytosol of the cells. Tailoring the nature and extent of the cationic side chains on this type of cationic hydroxyethylcellulose may be promising to further enhance their DNA delivery properties.