Propoxur
Based on 1 Customer Validation
Propoxur is a reversible, competitive, orally active AChE inhibitor that can cross the blood-brain barrier. Propoxur inhibits AChE activity to induce neurotoxicity, while promoting MMP-2 expression and enhancing tumor cell migration and invasion by inducing intracellular ROS generation and activating the ERK/Nrf2 signaling pathway. On the one hand, Propoxur inhibits AChE, leading to acetylcholine accumulation and causing neurological dysfunction; on the other hand, it promotes Nrf2 nuclear translocation through ROS-dependent ERK1/2 phosphorylation, and upregulates MMP-2 and other invasion-related proteins. Propoxur is also a carbamate insecticide used to combat turf, forestry, and household pests.
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity: 99.43%
- CAS No.: 114-26-1
- 화학식: C11H15NO3
- 분자량:209.24
-
보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biological Activity
-
Chemical Information
-
용액&용해도
- 순도&문서
- References
-
Help & FAQs
Biological Activity
|
MMP-2 |
AChE |
Propoxur (0.01-100 μM; 48 h) promotes cell migration and invasion in human breast cancer MCF-7 and MDA-MB-231 cells in a concentration-dependent manner, enhances MMP-2 protein expression, increases intracellular ROS levels, and activates ERK1/2 phosphorylation and Nrf2 nuclear translocation[1]. The intracellular regulatory activity of Propoxur could be reversed by PD98059 (HY-12028)[1].
Propoxur (10 μg/mL; 24 h) induces lipid peroxidation in hamster ovary CHO-K1 cells, significantly increases MDA production, decreases GSH content and GSH/GSSG ratio, and activates GR, GPx, and GST antioxidant enzyme activities. BSO pretreatment further aggravated oxidative damage[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:Human breast cancer MCF-7 and MDA-MB-231 cells
-
Concentration:0, 0.01, 1, 100 μM
-
Incubation Time:48 h
-
Result:Unchanged cell viability across concentrations, and reduced migration/invasion.
Dose-dependent increases in migration and invasion in Wound healing and Transwell assays, with 110.8-406.0% higher invasion compared to control.
-
Cell Line:Human breast cancer MCF-7 and MDA-MB-231 cells
-
Concentration:0, 0.01, 1, 100 μM
-
Incubation Time:48 h
-
Result:Increased MMP-2 protein expression without changes in MMP-9.
Dose-dependently increased phosphorylated ERK1/2 and nuclear Nrf2 levels, and the effects reversed by PD98059 (HY-12028), which suppressed MMP-2 overexpression.
-
Cell Line:MCF-7 & MDA-MB-231cells
-
Concentration:0, 0.01, 1, 100 μM
-
Incubation Time:48 h
-
Result:Resulted significant ROS accumulation in Flow cytometry and immunofluorescence.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Male Sprague-Dawley rats (250-300 g) with propoxur-induced neurotoxicity model[3]
-
Dosage:8.51 mg/kg
-
Administration:Oral gavage, daily for 30 days
-
Result:Significantly decreased body weight and weights of cerebellum, cortex, and hippocampus by 24%, 24%, 44%, respectively. AChE activity was reduced by 50% in cerebellum, 39% in cortex, and 54% in hippocampus.
Significantly decreased activities of superoxide dismutase (SOD), catalase (CAT), glutathione peroxidase (GSH-Px), and glutathione-S-transferase (GST).
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 114-26-1
-
Appearance Solid
-
분자량 209.24
-
화학식 C11H15NO3
-
Color White to off-white
-
SMILES
CC(C)OC1=CC=CC=C1OC(NC)=O
-
선적
Room temperature in continental US; may vary elsewhere.
-
보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
용액&용해도
DMSO : ≥ 100 mg/mL (477.92 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (9.94 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (9.94 mM); Suspended solution
This protocol yields a suspended solution of ≥ 2.08 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
-
Data Sheet (282 KB)
-
SDS (623 KB)
- English - EN (623 KB)
- Français - FR (623 KB)
- Deutsch - DE (623 KB)
- Norwegian - NO (623 KB)
- Español - ES (623 KB)
- Swedish - SV (623 KB)
- Italian - IT (623 KB)
- Korean - KR (623 KB)
- Portuguese - PT (623 KB)
-
Handling Instructions (2659 KB)
References
[1]. Shi Y, et al. Propoxur enhances MMP-2 expression and the corresponding invasion of human breast cancer cells via the ERK/Nrf2 signaling pathway. Oncotarget. 2017 Jul 7;8(50):87107-87123. [Content Brief]
[2]. Maran E, et al. Effects of aldicarb and propoxur on cytotoxicity and lipid peroxidation in CHO-K1 cells. Food Chem Toxicol. 2010 Jun;48(6):1592-6. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 4.7792 mL | 23.8960 mL | 47.7920 mL | 119.4800 mL |
| 5 mM | 0.9558 mL | 4.7792 mL | 9.5584 mL | 23.8960 mL | |
| 10 mM | 0.4779 mL | 2.3896 mL | 4.7792 mL | 11.9480 mL | |
| 15 mM | 0.3186 mL | 1.5931 mL | 3.1861 mL | 7.9653 mL | |
| 20 mM | 0.2390 mL | 1.1948 mL | 2.3896 mL | 5.9740 mL | |
| 25 mM | 0.1912 mL | 0.9558 mL | 1.9117 mL | 4.7792 mL | |
| 30 mM | 0.1593 mL | 0.7965 mL | 1.5931 mL | 3.9827 mL | |
| 40 mM | 0.1195 mL | 0.5974 mL | 1.1948 mL | 2.9870 mL | |
| 50 mM | 0.0956 mL | 0.4779 mL | 0.9558 mL | 2.3896 mL | |
| 60 mM | 0.0797 mL | 0.3983 mL | 0.7965 mL | 1.9913 mL | |
| 80 mM | 0.0597 mL | 0.2987 mL | 0.5974 mL | 1.4935 mL | |
| 100 mM | 0.0478 mL | 0.2390 mL | 0.4779 mL | 1.1948 mL |
Propoxur Related Classifications
HY-B0916 Related Classifications
Powered by Bioz