TRPM8-IN-1
Based on 1 Customer Validation
TRPM8-IN-1 (example 14) is an inhibitor of transient receptor potential melastatin-8 (TRPM8) channels, IC50<5 μM.
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- Pureté: 99.44%
- CAS No.: 1159996-20-9
- Formule: C23H18F4N2O
- Masse moléculaire:414.40
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
Activité biologique
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TRPM8 <5 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
53 nM
Compound: 68
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Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin induction by flash luminometry
Antagonist activity at rat TRPM8 expressed in CHO cells assessed as inhibition of icilin-induced Ca2+ influx incubated 2.5 mins prior icilin induction by flash luminometry
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[PMID: 22329507] |
Chemical Information
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CAS No. 1159996-20-9
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Appearance Solid
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Masse moléculaire 414.40
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Formule C23H18F4N2O
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Color White to off-white
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SMILES
O=C(N1C(C2=CC=C(C(F)(F)F)C=C2)C3=C(C=CC=C3)CC1)NC4=CC=C(F)C=C4
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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 6 months -20°C 1 month
Solvant et solubilité
DMSO : 100 mg/mL (241.31 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.5 mg/mL (6.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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 (273 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.4131 mL | 12.0656 mL | 24.1313 mL | 60.3282 mL |
| 5 mM | 0.4826 mL | 2.4131 mL | 4.8263 mL | 12.0656 mL | |
| 10 mM | 0.2413 mL | 1.2066 mL | 2.4131 mL | 6.0328 mL | |
| 15 mM | 0.1609 mL | 0.8044 mL | 1.6088 mL | 4.0219 mL | |
| 20 mM | 0.1207 mL | 0.6033 mL | 1.2066 mL | 3.0164 mL | |
| 25 mM | 0.0965 mL | 0.4826 mL | 0.9653 mL | 2.4131 mL | |
| 30 mM | 0.0804 mL | 0.4022 mL | 0.8044 mL | 2.0109 mL | |
| 40 mM | 0.0603 mL | 0.3016 mL | 0.6033 mL | 1.5082 mL | |
| 50 mM | 0.0483 mL | 0.2413 mL | 0.4826 mL | 1.2066 mL | |
| 60 mM | 0.0402 mL | 0.2011 mL | 0.4022 mL | 1.0055 mL | |
| 80 mM | 0.0302 mL | 0.1508 mL | 0.3016 mL | 0.7541 mL | |
| 100 mM | 0.0241 mL | 0.1207 mL | 0.2413 mL | 0.6033 mL |