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

Icilin (Synonyms: AG-3-5)

Cat. No.: HY-11062 Purity: ≥95.0%
Handling Instructions

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.

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

Icilin Chemical Structure

Icilin Chemical Structure

CAS No. : 36945-98-9

Size Price Stock Quantity
Solution
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
USD 66 In-stock
Estimated Time of Arrival: December 31
Solid
10 mg USD 60 In-stock
Estimated Time of Arrival: December 31
50 mg USD 220 In-stock
Estimated Time of Arrival: December 31
100 mg USD 380 In-stock
Estimated Time of Arrival: December 31
500 mg USD 1150 In-stock
Estimated Time of Arrival: December 31
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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

 

In Vitro

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

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

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].

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.
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 : ≥ 54 mg/mL (173.47 mM)

*"≥" 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
10 mM 0.3212 mL 1.6062 mL 3.2124 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

*All of the co-solvents are provided by MCE.
References
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Icilin
Cat. No.:
HY-11062
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