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TRPM8 antagonist 2

Name: TRPM8 antagonist 2
Brand: TargetMol
SKU: T5698
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T5698Cas No. 259674-19-6

TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.

TRPM8 antagonist 2

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Purity: 98.1%

Catalog No. T5698Cas No. 259674-19-6

TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$30	In Stock	In Stock
5 mg	$64	In Stock	In Stock
10 mg	$106	In Stock	In Stock
25 mg	$179	In Stock	In Stock
50 mg	$289	In Stock	In Stock
100 mg	$463	In Stock	In Stock
200 mg	$666	-	In Stock
1 mL x 10 mM (in DMSO)	$71	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Purity:98.1%

Appearance:Solid

Color:White

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COA LCMS HNMR

Product Introduction

Bioactivity

Description	TRPM8 antagonist 2 is a potent and selective TRPM8 antagonist with an IC50 of 0.2 nM, used in the research of neuropathic pain syndromes.
Targets&IC50	TRPM8:0.2 nM
In vitro	TRPM8 antagonist 2 (Compound 14) is a potent and selective TRPM8 antagonist with an IC50 of 0.2 nM, used in neuropathic pain research. It effectively inhibits menthol-induced increases in intracellular Ca2+ levels in Ca2+ fluorimetric assays in HEK293 cells expressing the rat TRPM8 isoform (IC50, 40 nM).
In vivo	TRPM8 antagonist 2, administered subcutaneously at doses of 1, 10, and 30 mg/kg, demonstrates significant, dose-dependent antinociceptive effects and reduces wet-dog shakes (WDS)-like cold hypersensitivity in mice by 63% at the 30 mg/kg dosage. Additionally, at lower doses of 0.1 and 1 μg, it effectively mitigates Oxaliplatin (OXP)-induced cold allodynia in mice.

Chemical Properties

Molecular Weight	398.5
Formula	C₂₆H₂₆N₂O₂
Cas No.	259674-19-6
Smiles	COC(=O)[C@H](Cc1c[nH]c2ccccc12)N(Cc1ccccc1)Cc1ccccc1
Relative Density.	1.195 g/cm3 (Predicted)

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 160 mg/mL (401.51 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 4 mg/mL (10.04 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.5094 mL	12.5471 mL	25.0941 mL	125.4705 mL
5 mM	0.5019 mL	2.5094 mL	5.0188 mL	25.0941 mL
10 mM	0.2509 mL	1.2547 mL	2.5094 mL	12.5471 mL
20 mM	0.1255 mL	0.6274 mL	1.2547 mL	6.2735 mL
50 mM	0.0502 mL	0.2509 mL	0.5019 mL	2.5094 mL
100 mM	0.0251 mL	0.1255 mL	0.2509 mL	1.2547 mL

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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.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc