TRPA1 agonist-3
Based on 1 Customer Validation
TRPA1 agonist-3 is a selective and orally active TRPA1 agonist, with EC50 values of 50.05 μM and 314.04 μM for human and mouse TRPA1, respectively. TRPA1 agonist-3 does not activate hTRPV1, mTRPV2, hTRPV3, hTRPV4, hTRPC6, or hTRPM8 channels. TRPA1 agonist-3 alleviates inflammatory pain in mice through a channel desensitization mechanism.
For research use only. We do not sell to patients.
- Purity: 99.78%
- CAS No.: 3083086-77-2
- Formula: C14H18N2OS
- Molecular Weight:262.37
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Storage:Powder -20°C, 3 years , 4°C, 2 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
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Membrane Transporter/Ion Channel Compound Library
HY-L011
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Neuronal Signaling Compound Library
HY-L013
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Orally Active Compound Library
HY-L061
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Mechanoreceptors Compound Library
HY-L095
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Pain-Related Compound Library
HY-L139
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Membrane Protein-targeted Compound Library
HY-L149
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Membrane Receptor-targeted Compound Library
HY-L150
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Highly Selective Activators Library
HY-L159
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Ion Channel Compound Library
HY-L166
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
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TRPA1 50.50 μM (EC50, human) |
TRPA1 314.04 μM (EC50, mouse) |
TRPA1 agonist-3 (compound NMTA) (50 μM, 24 h) activates hTRPA1 channels in a concentration dependent manner, leading to Ca2+ inffux in HEK-293T cells[1].
TRPA1 agonist-3 exerts analgesic effects mediated through TRPA1 desensitization[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
TRPA1 agonist-3 (10-40 mg/kg, p.o. once) has selective desensitization of TRPA1 rather than direct inhibition of heat-sensitive channels in male C57BL/6J mice[1].
TRPA1 (10-40 mg/kg, p.o., once) agonist-3 has antinociceptive effect on cold-induced pain in male C57BL/6J mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CFA (p.i. 20 μL)-induced male C57BL/6J mice (6-8 weeks old, 18 g-20 g)[1].
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Dosage:10, 20, 40 mg/kg
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Administration:p.o. at a volume of 200 μL per 20 g body weight, once
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Result:Reduced the paw withdrawal mechanical threshold and paw withdrawal thermal threshold in the CFA model group.
Prolonged the thermal withdrawal latency with peak effect at 0.5 h and lasted for 1 h.
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Animal Model:Female C57BL/6J mice (6-8 weeks old, 18 g-20 g)[1]
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Dosage:10, 20, 40 mg/kg
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Administration:p.o., once
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Result:Prolonged the thermal withdrawal latency.
Reached peak effect at 0.5 h and lasted for 1 h.
Produced weak antinociceptive effects in 40 mg/kg with peak effect evidenced by prolonged withdrawal latency (23.15 ± 1.30 s) at 0.5 h postdosing.
Lasted for 1 h but completely lost at 2 and 4 h.
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Animal Model:Male C57BL/6J mice (6-8 weeks old, 18 g-20 g)[1]
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Dosage:10, 20, 40 mg/kg
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Administration:p.o., once
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Result:Prolonged the thermal withdrawal latency. All treatment groups reached peak effect at 0.5 h and lasted for 1 h in cold plate test.
Increased the tail-flick latency and reached a peak at 17.70 s at 1 h (40 mg/kg) in Cold Tail-Flick Test.
Chemical Information
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CAS No. 3083086-77-2
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Appearance Solid
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Molecular Weight 262.37
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Formula C14H18N2OS
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Color White to off-white
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SMILES
COCCCNC1=NC(C2=CC=C(C=C2)C)=CS1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (381.14 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 (9.53 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2.5 mg/mL.
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 (9.53 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 (274 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
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 | 3.8114 mL | 19.0571 mL | 38.1141 mL | 95.2853 mL |
| 5 mM | 0.7623 mL | 3.8114 mL | 7.6228 mL | 19.0571 mL | |
| 10 mM | 0.3811 mL | 1.9057 mL | 3.8114 mL | 9.5285 mL | |
| 15 mM | 0.2541 mL | 1.2705 mL | 2.5409 mL | 6.3524 mL | |
| 20 mM | 0.1906 mL | 0.9529 mL | 1.9057 mL | 4.7643 mL | |
| 25 mM | 0.1525 mL | 0.7623 mL | 1.5246 mL | 3.8114 mL | |
| 30 mM | 0.1270 mL | 0.6352 mL | 1.2705 mL | 3.1762 mL | |
| 40 mM | 0.0953 mL | 0.4764 mL | 0.9529 mL | 2.3821 mL | |
| 50 mM | 0.0762 mL | 0.3811 mL | 0.7623 mL | 1.9057 mL | |
| 60 mM | 0.0635 mL | 0.3176 mL | 0.6352 mL | 1.5881 mL | |
| 80 mM | 0.0476 mL | 0.2382 mL | 0.4764 mL | 1.1911 mL | |
| 100 mM | 0.0381 mL | 0.1906 mL | 0.3811 mL | 0.9529 mL |
TRPA1 agonist-3 Related Classifications
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