2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. TRPA1 agonist-3

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.

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TRPA1 agonist-3

TRPA1 agonist-3 Chemical Structure

CAS No. : 3083086-77-2

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

TRPA1 agonist-3 Related Antibodies

Top Publications Citing Use of Products

View All TRP Channel Isoform Specific Products:

View All Isoforms
TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

  • Biological Activity

  • Purity & Documentation

  • References

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Description

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[1].

IC50 & Target[1]

TRPA1

50.50 μM (EC50, human)

TRPA1

314.04 μM (EC50, mouse)

In Vitro

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 Related Antibodies
In Vivo

TRPA1 agonist-3 (compound NMTA) (10-40 mg/kg, p.o., once) alleviates CFA (Complete Freund’s Adjuvant) (HY-153808B) (plantar injection p.i., 20 μL)-induced inflammatory pain in male C57BL/6J mice[1].
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.

Animal Model: CFA (p.i. 20 μL)-induced male C57BL/6J mice (6-8 weeks old, 18 g-20 g)[1].
Dosage: 10, 20, 40 mg/kg
Administration: p.o. at a volume of 200 μL per 20 g body weight, once
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.
Animal Model: Female C57BL/6J mice (6-8 weeks old, 18 g-20 g)[1]
Dosage: 10, 20, 40 mg/kg
Administration: p.o., once
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.
Animal Model: Male C57BL/6J mice (6-8 weeks old, 18 g-20 g)[1]
Dosage: 10, 20, 40 mg/kg
Administration: p.o., once
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.
Molecular Weight

262.37

Formula

C14H18N2OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

COCCCNC1=NC(C2=CC=C(C=C2)C)=CS1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.8114 mL 19.0571 mL 38.1141 mL
5 mM 0.7623 mL 3.8114 mL 7.6228 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, 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

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: 2.5 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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

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
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
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TRPA1 agonist-3 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TRPA1 agonist-33083086-77-2TRP ChannelTransient receptor potential channelsInflammatory painNMTATRPA1analgesicantinociceptionInhibitorinhibitorinhibit

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