TRPV3 antagonist 74a
Based on 1 Customer Validation
TRPV3 antagonist 74a is a potent and selective TRPV3 antagonist. TRPV3 antagonist 74a displays no significant activity against a panel of other ion channels. TRPV3 antagonist 74a can be used for the research of neuropathic pain.
For research use only. We do not sell to patients.
- Purity: 99.85%
- CAS No.: 1432051-63-2
- Formula: C17H17F3N2O2
- Molecular Weight:338.32
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Storage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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TRPV3 |
. TRPV3 antagonist 74a (10~100 mg/kg; p.o.) dose-dependently attenuates mechanical allodynia induced by von Frey hair stimulation to the ipsilateral (injured) hind paw. TRPV3 antagonist 74a exhibits anti-nociceptive activity in the reserpine model of central pain by increasing muscle pressure threshold[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:WT mice
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Dosage:150 μg
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Administration:Intradermal injection; 30 minutes
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Result:The number of scratches decreased significantly.
Chemical Information
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CAS No. 1432051-63-2
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Appearance Solid
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Molecular Weight 338.32
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Formula C17H17F3N2O2
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Color White to off-white
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SMILES
O[C@H](C1=CC=CC=N1)[C@@]2(C3=CC(C(F)(F)F)=CC=N3)C[C@@](O)(C2)C
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : ≥ 100 mg/mL (295.58 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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 (7.39 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.39 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 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.
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.
Purity & Documentation
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Data Sheet (278 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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Handling Instructions (2659 KB)
References
[1]. Gomtsyan A, et al. Synthesis and Pharmacology of (Pyridin-2-yl)methanol Derivatives as Novel and Selective Transient Receptor Potential Vanilloid 3 Antagonists. J Med Chem. 2016;59(10):4926-4947. [Content Brief]
[2]. Zhao J, et al. PAR2 Mediates Itch via TRPV3 Signaling in Keratinocytes. J Invest Dermatol. 2020;140(8):1524-1532. [Content Brief]
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 |
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| DMSO | 1 mM | 2.9558 mL | 14.7789 mL | 29.5578 mL | 73.8945 mL |
| 5 mM | 0.5912 mL | 2.9558 mL | 5.9116 mL | 14.7789 mL | |
| 10 mM | 0.2956 mL | 1.4779 mL | 2.9558 mL | 7.3895 mL | |
| 15 mM | 0.1971 mL | 0.9853 mL | 1.9705 mL | 4.9263 mL | |
| 20 mM | 0.1478 mL | 0.7389 mL | 1.4779 mL | 3.6947 mL | |
| 25 mM | 0.1182 mL | 0.5912 mL | 1.1823 mL | 2.9558 mL | |
| 30 mM | 0.0985 mL | 0.4926 mL | 0.9853 mL | 2.4632 mL | |
| 40 mM | 0.0739 mL | 0.3695 mL | 0.7389 mL | 1.8474 mL | |
| 50 mM | 0.0591 mL | 0.2956 mL | 0.5912 mL | 1.4779 mL | |
| 60 mM | 0.0493 mL | 0.2463 mL | 0.4926 mL | 1.2316 mL | |
| 80 mM | 0.0369 mL | 0.1847 mL | 0.3695 mL | 0.9237 mL | |
| 100 mM | 0.0296 mL | 0.1478 mL | 0.2956 mL | 0.7389 mL |
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