2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. Icilin

Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC50=1.4 μM). Icilin is a "super-cooling agent" . Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response.

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Icilin Chemical Structure

Icilin Chemical Structure

CAS No. : 36945-98-9

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Icilin Related Antibodies

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1 Publications Citing Use of MCE Icilin

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Description

Icilin (AG-3-5) is a super-agonist of the transient receptor potential M8 (TRPM8) ion channel. Icilin activates TRPM8 in EGTA in a dose-dependent manner (EC50=1.4 μM). Icilin is a "super-cooling agent" [1][2]. Icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response[3].

IC50 & Target[1]

TRPM8

 

Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
0.058 μM
Compound: 3
Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins before icilin stimulation by Fluo-4-AM dye based spectrofluorimetry
Antagonist activity against rat TRPM8 expressed in HEK293 cells assessed as inhibition of icilin-induced intracellular Ca2+ level pre-treated 5 mins before icilin stimulation by Fluo-4-AM dye based spectrofluorimetry
[PMID: 25935641]
HEK293 EC50
0.11 μM
Compound: 3
Agonist activity at rat TRPM8 expressed in HEK293 cells assessed as induction of intracellular Ca2+ level by Fluo-4-AM dye based spectrofluorimetry
Agonist activity at rat TRPM8 expressed in HEK293 cells assessed as induction of intracellular Ca2+ level by Fluo-4-AM dye based spectrofluorimetry
[PMID: 25935641]
HEK293 EC50
0.19 μM
Compound: icilin
Agonist activity at rat recombinant TRPM8 receptor expressed in HEK293 cells assessed as increase in intracellular calcium concentration by fluorimetric test
Agonist activity at rat recombinant TRPM8 receptor expressed in HEK293 cells assessed as increase in intracellular calcium concentration by fluorimetric test
[PMID: 19162486]
HEK293 EC50
300 nM
Compound: Icilin
Inhibition of human TRPM8 (unknown origin) expressed in HEK293 cells assessed as inhibition of WS12-induced Ca2+ elevation by FLIPR assay
Inhibition of human TRPM8 (unknown origin) expressed in HEK293 cells assessed as inhibition of WS12-induced Ca2+ elevation by FLIPR assay
[PMID: 24080460]
In Vitro

Icilin-evoked TRPM8 currents show variable activation kinetics and Ca2+ dependence.Icilin-evoked currents exhibit highly variable latencies with pronounced desensitization[1].

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

Icilin Related Antibodies

Cell Viability Assay[1]

Cell Line: TRPM8-expressing oocytes or HEK293 cells
Concentration: 10 μM
Incubation Time: 3 minutes for TRPM8-expressing oocytes; 1 minute for HEK293 cells
Result: Activated membrane currents with variable delay of onset in voltage-clamped TRPM8-expressing oocytes or HEK293 cells.
In Vivo

Icilin is a transient receptor potential cation channel subfamily M (TRPM8) agonist that produces behavioral activation in rats and mice. Icilin (3 mg/kg; s.c.) induces "Wet dog shake" in mice[2].

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

Animal Model: The C57BL/6 mice 9–10 weeks (adult, 26-30 g) or 24 months (aged, 35-42g)[2].
Dosage: 3 mg/kg
Administration: Injected s.c.
Result: Produced vivid and quantifiable shaking behaviors (“wet-dog shakes”), which were TRPM8-dependent. 
Molecular Weight

311.29

Formula

C16H13N3O4
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N(C2=CC=CC=C2O)CC=C(C3=CC=CC([N+]([O-])=O)=C3)N1
Shipping

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

DMSO : ≥ 54 mg/mL (173.47 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.2124 mL 16.0622 mL 32.1244 mL
5 mM 0.6425 mL 3.2124 mL 6.4249 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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

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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: ≥ 2.5 mg/mL (8.03 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.
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

Purity: 99.26%

SDS (393 KB)

COA (257 KB) HNMR (179 KB) RP-HPLC (169 KB) LCMS (228 KB)

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2124 mL 16.0622 mL 32.1244 mL 80.3110 mL
5 mM 0.6425 mL 3.2124 mL 6.4249 mL 16.0622 mL
10 mM 0.3212 mL 1.6062 mL 3.2124 mL 8.0311 mL
15 mM 0.2142 mL 1.0708 mL 2.1416 mL 5.3541 mL
20 mM 0.1606 mL 0.8031 mL 1.6062 mL 4.0155 mL
25 mM 0.1285 mL 0.6425 mL 1.2850 mL 3.2124 mL
30 mM 0.1071 mL 0.5354 mL 1.0708 mL 2.6770 mL
40 mM 0.0803 mL 0.4016 mL 0.8031 mL 2.0078 mL
50 mM 0.0642 mL 0.3212 mL 0.6425 mL 1.6062 mL
60 mM 0.0535 mL 0.2677 mL 0.5354 mL 1.3385 mL
80 mM 0.0402 mL 0.2008 mL 0.4016 mL 1.0039 mL
100 mM 0.0321 mL 0.1606 mL 0.3212 mL 0.8031 mL
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Icilin 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:

Icilin36945-98-9AG-3-5TRP ChannelTransient receptor potential channelssupertransientreceptorpotentialTRPM8ionchannel ,coolingautoimmuneneuroinflammationT-cellresponseInhibitorinhibitorinhibit

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