ICILIN CAS NO.36945-98-9

icilin(ag 3-5) is a synthetic super-agonist of trpm8 ion channel.
ic50 value:
target: trpm8
in vitro: icilin, a super-cooling agent, down-regulated the expression of cell cycle signature genes and caused g1 arrest in pc-3 prostate cancer cells. icilin affected cell cycle-related transcriptional modules and identified e2f1 transcription factor as a target master regulator of icilin. icilin reduced the activity and expression levels of e2f1 [1]. icilin concentration-response curves were significantly shifted to the right when ph was lowered from 7.3 to 6.9, whereas those with menthol were unaltered in solutions of ph 6.1 [2]. icilin modulated the expression level of various cell cycle regulators at transcription or post-translational levels. in addition, icilin activated jnk and p38 kinase pathways, but not erk [4].
in vivo: rats injected with icilin (0.5, 1, 2.5, 5mg/kg, i.p.) displayed dose-related wds that were inhibited by pretreatment with a fixed dose of clonidine (0.15 mg/kg, s.c.). shaking behavior caused by a fixed dose (2.5mg/kg) of icilin was also inhibited in a dose-related manner by clonidine pretreatment (0.03-0.15 mg/kg, s.c.) and reduced by clonidine posttreatment (0.15 mg/kg, s.c.) [3].