2-PPA
Based on 1 Customer Validation
2-PPA is a lysosomal potassium and proton channel TMEM175 pore blocker. 2-PPA binds at a TMEM175 pore site to occlude potassium and proton ion permeation pathways. 2-PPA increases lysosomal macromolecule catabolism, accelerates macropinocytosis. 2-PPA binds to hepatic protein in covalent. 2-PPA can be used for the research of Parkinson's disease.
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- Pureza: 99.98%
- No. CAS: 21203-86-1
- Fòrmula: C11H10N2
- Peso molecular:170.22
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Almacenamiento:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Anti-Alzheimer's Disease Compound Library
HY-L069
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Anti-Parkinson's Disease Compound Library
HY-L085
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Neurodegenerative Disease-related Compound Library
HY-L086
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Potassium Channel Compound Library
HY-L119
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Ion Channel Compound Library
HY-L166
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
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Membrane Transporter/Ion Channel Compound Library
HY-L011
Actividad biológica
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TMEM175 |
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Cell Line
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Type | Value | Description | References |
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| HEK293 | IC50 |
6.9 μM
Compound: 12
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Inhibition of human ASIC3 expressed in HEK293 cells assessed as inhibition of acid-evoked current by manual patch-clamp electrophysiology assay
Inhibition of human ASIC3 expressed in HEK293 cells assessed as inhibition of acid-evoked current by manual patch-clamp electrophysiology assay
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[PMID: 21257308] |
2-PPA (1-1000 μM) potently inhibits human TMEM175-mediated K+ flux, with an IC50 of 31 μM[1].
2-PPA binds as a pore blocker to the cytosolic region of the open-state human TMEM175 pore, occluding the ion permeation pathway via specific interactions with channel residues Ser45 and Ala42[1].
2-PPA (3-1000 μM) potently and selectively inhibits human TMEM175-mediated Kv3.1 currents in HEK293T cells, with an IC50 of 32 μM[1].
2-PPA (3-1000 μM) inhibits human TMEM175-mediated proton flux in HEK293T cells with an IC50 of 30 μM at pH 4.5[1].
2-PPA (300 μM; 1 h) accelerates lysosomal catabolism and macropinocytosis in wild-type MEFs, MIA PaCa-2, SH-SY5Y, PANC-1, and HeLa cells via specific inhibition of TMEM175[1].
2-PPA (300 μM; 1 h) stimulates lysosomal cathepsin B activity in wild-type MEFs via indirect modulation of lysosomal function, without directly altering cathepsin enzymatic activity[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 21203-86-1
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Appearance Solid
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Peso molecular 170.22
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Fòrmula C11H10N2
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Color White to off-white
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SMILES
NC1=CC(C2=CC=CC=C2)=NC=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvente y solubilidad
DMSO : ≥ 100 mg/mL (587.48 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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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: ≥ 2.5 mg/mL (14.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (14.69 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. Oh S, et al. Discovery of Selective Inhibitors for the Lysosomal Parkinson's Disease Channel TMEM175. J Am Chem Soc. 2024;146(33):23230-23239. [Content Brief]
[2]. Li C, et al. Differential effects of fibrates on the metabolic activation of 2-phenylpropionic acid in rats. Drug Metab Dispos. 2008;36(4):682-687. [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, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 5.8748 mL | 29.3738 mL | 58.7475 mL | 146.8688 mL |
| 5 mM | 1.1750 mL | 5.8748 mL | 11.7495 mL | 29.3738 mL | |
| 10 mM | 0.5875 mL | 2.9374 mL | 5.8748 mL | 14.6869 mL | |
| 15 mM | 0.3917 mL | 1.9583 mL | 3.9165 mL | 9.7913 mL | |
| 20 mM | 0.2937 mL | 1.4687 mL | 2.9374 mL | 7.3434 mL | |
| 25 mM | 0.2350 mL | 1.1750 mL | 2.3499 mL | 5.8748 mL | |
| 30 mM | 0.1958 mL | 0.9791 mL | 1.9583 mL | 4.8956 mL | |
| 40 mM | 0.1469 mL | 0.7343 mL | 1.4687 mL | 3.6717 mL | |
| 50 mM | 0.1175 mL | 0.5875 mL | 1.1750 mL | 2.9374 mL | |
| 60 mM | 0.0979 mL | 0.4896 mL | 0.9791 mL | 2.4478 mL | |
| 80 mM | 0.0734 mL | 0.3672 mL | 0.7343 mL | 1.8359 mL | |
| 100 mM | 0.0587 mL | 0.2937 mL | 0.5875 mL | 1.4687 mL |
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