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Chemical Structure| 36945-98-9 Chemical Structure| 36945-98-9

Structure of Icilin
CAS No.: 36945-98-9

Chemical Structure| 36945-98-9

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Icilin is an agonist of TRPM8 ion channel with EC50 of 0.36 μM in HEK 293 cells.

Synonyms: AG-3-5

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Product Details of Icilin

CAS No. :36945-98-9
Formula : C16H13N3O4
M.W : 311.29
SMILES Code : O=C1NC(C2=CC=CC([N+]([O-])=O)=C2)=CCN1C3=CC=CC=C3O
Synonyms :
AG-3-5
MDL No. :MFCD01689072
InChI Key :RCEFMOGVOYEGJN-UHFFFAOYSA-N
Pubchem ID :161930

Safety of Icilin

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H312-H332
Precautionary Statements:P280

Isoform Comparison

Biological Activity

In Vitro:

Cell Line
Concentration Treated Time Description References
HEK293 cells 20 µM To study the activation effect of Icilin on TRPM8 FA_AG channels, results showed that Icilin elicits robust currents in the presence of Ca2+ Science. 2019 Mar 1;363(6430):eaav9334
human primary brown adipocytes 1 µM and 10 µM 6 hours To evaluate the effect of Icilin on UCP1 expression and oxygen consumption rate in human brown adipocytes, results showed that Icilin did not significantly increase Ucp1 transcription or oxygen consumption. Nat Commun. 2018 Oct 23;9(1):4304
mouse primary brown adipocytes 1 µM and 10 µM 6 hours To evaluate the effect of Icilin on UCP1 expression and oxygen consumption rate in brown adipocytes, results showed that Icilin did not significantly increase Ucp1 transcription or oxygen consumption. Nat Commun. 2018 Oct 23;9(1):4304
HEK cells 30 μM TRPM8 activation by icilin blocked TRPV1-mediated calcium signaling Proc Natl Acad Sci U S A. 2013 Apr 30;110(18):7476-81
human iPSC-derived TG neurons 1 μM 30 seconds To assess the response of trigeminal neurons to cold stimuli, results showed that approximately 15% of cells responded to icilin at day 30 of differentiation. Proc Natl Acad Sci U S A. 2018 Sep 11;115(37):E8775-E8782

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice Diet-induced obese (DIO) mice Subcutaneous injection 0.6 mg/kg and 6 mg/kg Once daily for 14 days To evaluate the effect of Icilin on energy expenditure and body weight, results showed that Icilin dose-dependently lowered body weight and increased energy expenditure without affecting food intake. Nat Commun. 2018 Oct 23;9(1):4304
Mice VAMP7−/− mice Left hind paw injection 5 mM icilin solution Single injection, measured at 15 and 30 minutes post-injection To evaluate the effect of VAMP7 deficiency on icilin-induced cold hypersensitivity, results showed a significant blunting of cold hypersensitivity in VAMP7?/? mice. Nat Commun. 2016 Feb 4;7:10489
Mice CGRP α-DTR+/− mice Plantar injection 2.4 μg/μl Single injection To study the behavioral responses of CGRP α DRG neurons to cold stimuli, it was found that DTX-treated mice showed significantly enhanced behavioral responses to icilin. Neuron. 2013 Apr 10;78(1):138-51

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.21mL

0.64mL

0.32mL

16.06mL

3.21mL

1.61mL

32.12mL

6.42mL

3.21mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1

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