Icilin (Synonyms: AG-3-5)

Name: Icilin
Brand: MedChemExpress
SKU: HY-11062
Rating: 4.5 (1 reviews)

Cat. No.: HY-11062 Purity: 99.26%: FAQs
Data Sheet
SDS

COA
Handling Instructions Technical Support

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

CAS No. : 36945-98-9

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 1 publication(s) in Google Scholar

1 Publications Citing Use of MCE Icilin

•Int J Biol Macromol. 2024 Jul 3:133659. [Abstract]

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TRPC TRPM TRPV TRPA TRPML

Biological Activity
Purity & Documentation
References
Customer Review

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.

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.

36945-98-9

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 : 100 mg/mL (321.24 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	3.2124 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

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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

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In Vivo Dissolution Calculator

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.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.26%

Select Batch:

Data Sheet (282 KB) SDS (393 KB)

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

Handling Instructions (2659 KB)

References

[1]. Huai-hu Chuang, et al. The super-cooling agent icilin reveals a mechanism of coincidence detection by a temperature-sensitive TRP channel. Neuron. 2004 Sep 16;43(6):859-69. [Content Brief]

[2]. Viktor V Feketa,et al. Transient receptor potential melastatin 8 channel inhibition potentiates the hypothermic response to transient receptor potential vanilloid 1 activation in the conscious mouse. Crit Care Med. 2014 May;42(5):e355-63. [Content Brief]

[3]. Benjamin W Ewanchuk, et al. The cooling compound icilin attenuates autoimmune neuroinflammation through modulation of the T-cell response. FASEB J. 2018 Mar;32(3):1236-1249. [Content Brief]

Complete Stock Solution Preparation Table

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

Icilin Related Classifications

Neurological Disease Inflammation/Immunology

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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Icilin (Synonyms: AG-3-5)

Customer Review

Icilin Related Antibodies

1 Publications Citing Use of MCE Icilin

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All TRP Channel Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Icilin Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Icilin Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

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