1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel
  3. CIM0216

CIM0216, a synthetic TRPM3 ligand, acts as a potent and selective agonist of TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts in a TRPM3-dependent manner to induce pain and evoke neuropeptide release from sensory nerve terminals in vitro. CIM0216 is a powerful tool for studies of the physiological functions of TRPM3, and can be used for neurogenic inflammation research.

For research use only. We do not sell to patients.

CIM0216 Chemical Structure

CIM0216 Chemical Structure

CAS No. : 1031496-06-6

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 115 In-stock
Solution
10 mM * 1 mL in DMSO USD 115 In-stock
Solid
1 mg USD 50 In-stock
5 mg USD 105 In-stock
10 mg USD 182 In-stock
25 mg USD 380 In-stock
50 mg USD 605 In-stock
100 mg USD 1045 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

CIM0216, a synthetic TRPM3 ligand, acts as a potent and selective agonist of TRPM3. CIM0216 exhibits selectivity for TRPM3 over TRPM1, TRPM2 and TRPM4-8. CIM0216 acts in a TRPM3-dependent manner to induce pain and evoke neuropeptide release from sensory nerve terminals in vitro. CIM0216 is a powerful tool for studies of the physiological functions of TRPM3, and can be used for neurogenic inflammation research[1].

IC50 & Target[1]

TRPM3

 

In Vitro

CIM0216 elicits a dose-dependent Ca2+ response [pEC50=0.77±0.1 μM] in HEK-TRPM3 cells, which is not observed in nontransfected HEK293 cells. CIM0216 induces a robust increase in intracellular Ca2+ concentration (1,145±26 nM) in single-cell FURA2-ratiometric Ca2+ imaging in HEK-TRPM3 cells. These responses are not observed in nontransfected HEK cells or in the absence of extracellular Ca2+[1].
CIM0216 (10 μM) has no stimulating/blocking effect on TRPM1, TRPM4, TRPM6, or TRPM7 currents; however, a small blocking effect of CIM0216 is observed after activation of TRPM2 (16.6% block) and TRPM5 (33.5% block). CIM0216 also has no detectable effect on human TRPV1 and TRPM8 channel activation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Molecular Weight

347.41

Formula

C21H21N3O2

CAS No.
Appearance

Solid

SMILES

CC1=CC(NC(C(C2=CC=CC=C2)N3C4=CC=CC=C4CCC3)=O)=NO1

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 : 35 mg/mL (100.75 mM; Need ultrasonic and warming; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 17 mg/mL (48.93 mM; Need ultrasonic and warming)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8784 mL 14.3922 mL 28.7844 mL
5 mM 0.5757 mL 2.8784 mL 5.7569 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)

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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

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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: ≥ 2.08 mg/mL (5.99 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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(per animal)

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Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
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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
Ethanol / DMSO 1 mM 2.8784 mL 14.3922 mL 28.7844 mL 71.9611 mL
5 mM 0.5757 mL 2.8784 mL 5.7569 mL 14.3922 mL
10 mM 0.2878 mL 1.4392 mL 2.8784 mL 7.1961 mL
15 mM 0.1919 mL 0.9595 mL 1.9190 mL 4.7974 mL
20 mM 0.1439 mL 0.7196 mL 1.4392 mL 3.5981 mL
25 mM 0.1151 mL 0.5757 mL 1.1514 mL 2.8784 mL
30 mM 0.0959 mL 0.4797 mL 0.9595 mL 2.3987 mL
40 mM 0.0720 mL 0.3598 mL 0.7196 mL 1.7990 mL
DMSO 50 mM 0.0576 mL 0.2878 mL 0.5757 mL 1.4392 mL
60 mM 0.0480 mL 0.2399 mL 0.4797 mL 1.1994 mL
80 mM 0.0360 mL 0.1799 mL 0.3598 mL 0.8995 mL
100 mM 0.0288 mL 0.1439 mL 0.2878 mL 0.7196 mL
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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.

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CIM0216
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