Icilin is a synthetic super-agonist of the transient receptor potential M8 (TRPM8) ion channel.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 Induces currents in CMR1-expressing HEK 293 cells (EC50 = 0.36 μM) more potently than menthol or low temperatures. 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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO 15 mg/ml|
Icilin inhibits E2F1-mediated cell cycle regulatory programs in prostate cancer.
Lee S,et al. Biochem Biophys Res Commun. 2013 Nov 29;441(4):1005-10. PMID: 24239550.
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