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TRPM8 antagonist 3

Name: TRPM8 antagonist 3
Brand: TargetMol
SKU: T9709
Price: 34 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T9709Cas No. 2102179-29-1

TRPM8 antagonist 3 is a blocker of TRPM8 (IC50 = 11 nM).

TRPM8 antagonist 3

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Purity: 99.74%

Catalog No. T9709Cas No. 2102179-29-1

TRPM8 antagonist 3 is a blocker of TRPM8 (IC50 = 11 nM).

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$34	In Stock	In Stock
5 mg	$82	In Stock	In Stock
10 mg	$128	In Stock	In Stock
25 mg	$212	In Stock	In Stock
50 mg	$309	In Stock	In Stock
100 mg	$435	In Stock	In Stock
1 mL x 10 mM (in DMSO)	$91	In Stock	In Stock

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

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Purity:99.74%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

TRPM8 antagonist 3 AI Summary

TRPM8 antagonist 3 is a bioactive compound that exhibits inhibitory activity against human TRPM8 receptors expressed in HEK293 cells. It has demonstrated potent IC50 values of 11.0 nM for reducing Ca2+ efflux induced by ethyl 4-methoxy-2-phenylthiazole-5-carboxylate, 4.5 nM for icilin-induced Ca2+ efflux, and 5.5 nM for cold-stimulated Ca2+ efflux. Additionally, the compound showed moderate apparent permeability in human corneal epithelial cells at 0.1%, with high solubility at pH 7.4 measured at 9700000.0 nM. In a metabolic stability assay using human liver S9 fraction, it had a half-life of 0.8833 hours. Furthermore, TRPM8 antagonist 3 displayed a pKa value of 9.3 and a logD of 0.77 at pH 7.4..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	TRPM8 antagonist 3 is a blocker of TRPM8 (IC50 = 11 nM).
Targets&IC50	TRPM8:11 nM

Chemical Properties

Molecular Weight	292.31
Formula	C₁₃H₁₂N₂O₄S
Cas No.	2102179-29-1
Smiles	Oc1nc(sc1C(=O)N1CCCO1)-c1ccccc1O
Relative Density.	1.517 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: 50 mg/mL (171.05 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	3.4210 mL	17.1051 mL	34.2103 mL	171.0513 mL
5 mM	0.6842 mL	3.4210 mL	6.8421 mL	34.2103 mL
10 mM	0.3421 mL	1.7105 mL	3.4210 mL	17.1051 mL
20 mM	0.1711 mL	0.8553 mL	1.7105 mL	8.5526 mL
50 mM	0.0684 mL	0.3421 mL	0.6842 mL	3.4210 mL
100 mM	0.0342 mL	0.1711 mL	0.3421 mL	1.7105 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