Icilin
Based on 1 publication(s) in Google Scholar
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.
- Purity: 99.26%
- CAS No.: 36945-98-9
- Formula: C16H13N3O4
- Molecular Weight:311.29
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Icilin
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Biological Activity
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TRPM8 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | EC50 |
0.11 μM
Compound: 3
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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
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[PMID: 25935641] |
| HEK293 | EC50 |
0.19 μM
Compound: icilin
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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
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[PMID: 19162486] |
| HEK293 | EC50 |
100 μM
Compound: 52
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Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx
Agonist activity at human TRPA1 channel expressed in HEK293 cells assessed as increase in intracellular calcium influx
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[PMID: 20356305] |
| HEK293 | EC50 |
300 nM
Compound: Icilin
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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
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[PMID: 24080460] |
| HEK293 | IC50 |
0.058 μM
Compound: 3
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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
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[PMID: 25935641] |
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.
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Cell Line:TRPM8-expressing oocytes or HEK293 cells
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Concentration:10 μM
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Incubation Time:3 minutes for TRPM8-expressing oocytes; 1 minute for HEK293 cells
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Result:Activated membrane currents with variable delay of onset in voltage-clamped TRPM8-expressing oocytes or HEK293 cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:The C57BL/6 mice 9–10 weeks (adult, 26-30 g) or 24 months (aged, 35-42g)[2].
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Dosage:3 mg/kg
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Administration:Injected s.c.
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Result:Produced vivid and quantifiable shaking behaviors (“wet-dog shakes”), which were TRPM8-dependent.
Chemical Information
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CAS No. 36945-98-9
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Appearance Solid
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Molecular Weight 311.29
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Formula C16H13N3O4
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Color Light yellow to yellow
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SMILES
O=C1N(C2=CC=CC=C2O)CC=C(C3=CC=CC([N+]([O-])=O)=C3)N1
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Synonyms
AG-3-5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Int J Biol Macromol
Neuregulin 1 mitigated prolactin deficiency through enhancing TRPM8 signaling under the influence of melatonin in senescent pituitary lactotrophs. [Abstract]2024 Jul 3:133659. PMID: 38969045
Icilin purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2024 Jul 3:133659. [Abstract]
The effects of varying concentrations of Icilin (1-10 μM) on the Nrg1-TRPM8 axis and protein levels of PRL in GH3 cells after 48 h of treatment. The results indicated increased phosphorylation levels of ErbB4 and Akt1, along with a marked upregulation of PRL expression after treatment with the TRPM8 agonist Icilin.
Icilin purchased from MedChemExpress. Usage Cited in: Int J Biol Macromol. 2024 Jul 3:133659. [Abstract]
The effect of varying concentrations of Icilin on the secretion of soluble PRL into the conditioned medium of GH3 cells. The results showed that Icilin (1-10 μM; 48 h) significantly enhance the secretion of a soluble form of PRL into the conditioned culture.
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (282 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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
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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