2-PPA

Name: 2-PPA
Brand: MedChemExpress
SKU: HY-33878
Rating: 4.5 (1 reviews)

Cat. No.: HY-33878 Purity: 99.98%: Data Sheet
COA

SDS
Handling Instructions
FAQs
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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.

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

2-PPA Chemical Structure

CAS No. : 21203-86-1

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	In-stock	Estimated Time of Arrival: December 31
5 g	In-stock	Estimated Time of Arrival: December 31
10 g	In-stock	Estimated Time of Arrival: December 31
50 g	Get quote

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Based on 1 publication(s) in Google Scholar

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References
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Description

IC₅₀ & Target^[1]

TMEM175

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	6.9 μM Compound: 12	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	[PMID: 21257308]

In Vitro

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.

In Vivo

2-PPA (130 mg/kg; i.p.; single dose) administration to rats results in covalent binding to hepatic protein that is increased by 25% with Clofibric acid (HY-B1415) pretreatment, and decreased by 25% and 29% with Fenofibrate (HY-17356) and Gemfibrozil (HY-B0258) pretreatment, respectively, due to differential modulation of hepatic reactive metabolite levels^[2].

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

Molecular Weight

170.22

Formula

C₁₁H₁₀N₂

CAS No.

21203-86-1

Appearance

Solid

Color

White to off-white

SMILES

NC1=CC(C2=CC=CC=C2)=NC=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility

In Vitro:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	5.8748 mL	29.3738 mL	58.7475 mL
5 mM	1.1750 mL	5.8748 mL	11.7495 mL
10 mM	0.5875 mL	2.9374 mL	5.8748 mL

View the 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (14.69 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

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).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Purity & Documentation

Purity: 99.98%

Select Batch:

Data Sheet (273 KB) SDS (394 KB)

COA (246 KB) HNMR (131 KB) RP-HPLC (213 KB)

Handling Instructions (2659 KB)

References

[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.

Complete Stock Solution Preparation Table

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

2-PPA Related Classifications

Neurological Disease

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.

Keywords:

2-PPA21203-86-1Potassium ChannelProton PumpKcsAMEFsMIA PaCa-2SH-SY5YPANC-1HeLaInhibitorinhibitorinhibit

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2-PPA

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