TRPM2-IN-2

Name: TRPM2-IN-2
Brand: TargetMol
SKU: T213658
Rating: 4.5 (1 reviews)

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TRPM2-IN-2 is a potent and selective TRPM2 inhibitor (IC50= 0.66 μM) with minimal activity against TRPM8 and TRPV1 (IC50> 10 μM). It demonstrates significant neuroprotective effects in both an in vitro oxygen-glucose deprivation/reperfusion (OGD/R) model and an in vivo transient middle cerebral artery occlusion (tMCAO) mouse model. TRPM2-IN-2 can be used for research related to ischemic stroke.

TRPM2-IN-2

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For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Product Introduction

Bioactivity

Description	TRPM2-IN-2 is a potent and selective TRPM2 inhibitor (IC50= 0.66 μM) with minimal activity against TRPM8 and TRPV1 (IC50> 10 μM). It demonstrates significant neuroprotective effects in both an in vitro oxygen-glucose deprivation/reperfusion (OGD/R) model and an in vivo transient middle cerebral artery occlusion (tMCAO) mouse model. TRPM2-IN-2 can be used for research related to ischemic stroke.
Targets & IC50	TRPM2:0.66 μM
In vitro	TRPM2-IN-2 (LC4) demonstrates protective effects as an adamantane derivative in an OGD/R cell model, at concentrations ranging from 0.03 to 10 μM over 6 to 24 hours, and exhibits low cytotoxicity towards SH-SY5Y cells. At a concentration of 10 μM, TRPM2-IN-2 shows minimal inhibitory activity on TRPV1 and TRPM8, with inhibition rates of 20.5% and 23.2%, respectively. Additionally, it inhibits the hERG channel in CHO cells with an IC50 value of 21.61 μM.
In vivo	In a tMCAO mouse model, TRPM2-IN-2 administered intravenously at doses of 0.3, 1, and 3 mg/kg as a single dose demonstrated significant neuroprotective effects at 3 hours post-infusion.

Chemical Properties

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Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.