TRPM8 antagonist 2
Based on 2 publication(s) in Google Scholar
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.
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- Pureté : 98.09%
- CAS No.: 259674-19-6
- Formule: C26H26N2O2
- Masse moléculaire:398.50
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TRPM8 antagonist 2
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Activité biologique
Description
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
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 259674-19-6
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Appearance Solid
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Masse moléculaire 398.50
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Formule C26H26N2O2
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Color Light yellow to yellow
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SMILES
O=C([C@@H](N(CC1=CC=CC=C1)CC2=CC=CC=C2)CC3=CNC4=CC=CC=C43)OC
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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Biomolecules
Up-Regulation of the TRPM8 Channel Attenuates TRPC1-Mediated Store-Operated Calcium Entry in Abdominal Aortic Aneurysm. [Abstract]2026 May 19;16(5):741. PMID: 42194089 -
Solvant et solubilité
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)
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.
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.
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.
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.
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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureté et documentation
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Fiche technique (283 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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.
| 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 |
TRPM8 antagonist 2 Related Classifications
HY-112430 Related Classifications
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