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Purity: ≥98%
Icilin (also known as AG-3-5 or AG 3-5) is a synthetic CMR1/TRPM8 (transient receptor potential M8) super-cooling agent/agonist that is 2.5-fold more efficacious and nearly 200-fold more potent than the reference cold thermosensory agonist, l-menthol. Icilin induces sensations of intense cold when applied orally in humans, and induces 'wet dog shakes', a behavioral marker of cold sensation, when given to rats. Icilin should serve as the reference cold nociceptive agonist For TRP-type ion channels in the future. Icilin down-regulated the expression of cell cycle signature genes and caused G1 arrest in PC-3 prostate cancer cells. Icilin inactivates a small regulatory module controlling the cell cycle in prostate cancer cells. This study might provide insight into the development of cell cycle-targeted cancer therapeutics.
| ln Vitro |
Icilin-evoked TRPM8 currents demonstrate very varied latencies with substantial desensitization. They also have variable activation kinetics and Ca2+ dependence[1].
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| ln Vivo |
Rats and mice are behaviorally activated by iscilin, a transient receptor potential cation channel subfamily M (TRPM8) agonist. Mice are given the "Wet dog shake" when given icin (3 mg/kg; sc)[2].
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| Cell Assay |
Cell Viability Assay[1]
Cell Types: TRPM8-expressing oocytes or HEK293 cells Tested Concentrations: 10 μM Incubation Duration: 3 minutes for TRPM8-expressing oocytes; 1 minute for HEK293 cells Experimental Results: Activated membrane currents with variable delay of onset in voltage-clamped TRPM8-expressing oocytes or HEK293 cells. |
| Animal Protocol |
Animal/Disease Models: The C57BL/ 6 mice 9–10 weeks (adult, 26-30 g) or 24 months (aged, 35-42g)[2].
Doses: 3 mg/kg Route of Administration: Injected sc Experimental Results: Produced vivid and quantifiable shaking behaviors (“wet- dog shakes”), which were TRPM8-dependent. |
| 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.
[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. [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. |
| Molecular Formula |
C16H13N3O4
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| Molecular Weight |
311.29
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| CAS # |
36945-98-9
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| Related CAS # |
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| SMILES |
O=C1NC(C2=CC=CC([N+]([O-])=O)=C2)=CCN1C3=CC=CC=C3O
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (8.03 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 + to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Clonidine pretreatment reduces WDS induced by a fixed dose of icilin.Brain Res.2011 Apr 12;1384:110-7. |
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Pretreatment with a fixed dose of clonidine (0.15 mg/kg) reduces WDS evoked by graded doses of icilin.Brain Res.2011 Apr 12;1384:110-7. |
ST-91 pretreatment reduces WDS induced by a fixed dose of icilin.Brain Res.2011 Apr 12;1384:110-7. |
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