TRPM8 antagonist 2

Name: TRPM8 antagonist 2
Brand: MedChemExpress
SKU: HY-112430
Rating: 4.5 (1 reviews)

Cat. No.: HY-112430 Purity: 98.01%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

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.

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

TRPM8 antagonist 2 Chemical Structure

CAS No. : 259674-19-6

Size	Price	Stock	Quantity

Free Sample (0.1 - 0.5 mg)		Apply Now
Solid + Solvent
10 mM * 1 mL in DMSO ready for reconstitution	USD 109	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 109	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	USD 99	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 462	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 770	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE TRPM8 antagonist 2

•bioRxiv. 2023 Jun 20.

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

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.

IC₅₀ & Target

IC50: 0.2 nM (TRPM8)^[1]

In Vitro

TRPM8 antagonist 2 (Compound 14) 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 potently inhibits menthol-induced increase in intracellular Ca²⁺ levels in Ca²⁺ fluorimetric assays in HEK293 cells stably expressing the rat isoform of TRPM8 channels (IC₅₀, 40 nM)^[1].

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

In Vivo

TRPM8 antagonist 2 (1, 10, and 30 mg/kg, s.c.) shows a marked, dose-dependent antinociceptive activity, and inhibits wet-dog shakes (WDS)-like cold hypersensitivity in mice by 63% at 30 mg/kg. In addition, TRPM8 antagonist 2 (0.1 and 1 μg, s.c.) attenuates Oxaliplatin (OXP)-induced cold allodynia in mice^[1].

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

Molecular Weight

398.50

Formula

C₂₆H₂₆N₂O₂

CAS No.

259674-19-6

Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C([C@@H](N(CC1=CC=CC=C1)CC2=CC=CC=C2)CC3=CNC4=CC=CC=C43)OC

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (250.94 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.5094 mL	12.5471 mL	25.0941 mL
5 mM	0.5019 mL	2.5094 mL	5.0188 mL
10 mM	0.2509 mL	1.2547 mL	2.5094 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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: ≥ 2.67 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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: ≥ 2.67 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.67 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (26.7 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: ≥ 2.67 mg/mL (6.70 mM); Clear solution

This protocol yields a clear solution of ≥ 2.67 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 (26.7 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).

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: 98.01%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (262 KB) HNMR (259 KB) RP-HPLC (245 KB) MS (70 KB)

Handling Instructions (2659 KB)

References

[1]. Bertamino A, et al. Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity. J Med Chem. 2018 Jul 10. doi: 10.1021/acs.jmedchem.8b00545. [Content Brief]

Animal Administration
^[1]

Mice^[1]
Icilin, a TRPM8 agonist, is dissolved in 20% DMSO and 1% Tween 80 in distilled water and injected intraperitoneally (i.p.) in a volume of 10 mL/kg. Each animal is acclimatized for 30 min for two consecutive days before icilin administration. TRPM8 antagonist 2 (compound 14) stock is prepared in DMSO and diluted in saline for injections. Gabapentin is dissolved in saline and administered s.c. at the dose of 25 mg/kg 60 min prior to icillin injection. Control animals receive the vehicle injection^[1].

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

References

[1]. Bertamino A, et al. Identification of a Potent Tryptophan-Based TRPM8 Antagonist With in Vivo Analgesic Activity. J Med Chem. 2018 Jul 10. doi: 10.1021/acs.jmedchem.8b00545. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.5094 mL	12.5471 mL	25.0941 mL	62.7353 mL
	5 mM	0.5019 mL	2.5094 mL	5.0188 mL	12.5471 mL
	10 mM	0.2509 mL	1.2547 mL	2.5094 mL	6.2735 mL
	15 mM	0.1673 mL	0.8365 mL	1.6729 mL	4.1824 mL
	20 mM	0.1255 mL	0.6274 mL	1.2547 mL	3.1368 mL
	25 mM	0.1004 mL	0.5019 mL	1.0038 mL	2.5094 mL
	30 mM	0.0836 mL	0.4182 mL	0.8365 mL	2.0912 mL
	40 mM	0.0627 mL	0.3137 mL	0.6274 mL	1.5684 mL
	50 mM	0.0502 mL	0.2509 mL	0.5019 mL	1.2547 mL
	60 mM	0.0418 mL	0.2091 mL	0.4182 mL	1.0456 mL
	80 mM	0.0314 mL	0.1568 mL	0.3137 mL	0.7842 mL
	100 mM	0.0251 mL	0.1255 mL	0.2509 mL	0.6274 mL