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Icilin

Cat. No. M2591
Icilin Structure
Synonym:

AG 3-5

Size Price Availability Quantity
10mM*1mL in DMSO USD 57.6  USD64 In stock
10mg USD 52.2  USD58 In stock
50mg USD 189  USD210 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 311.29
Formula C16H13N3O4
CAS Number 36945-98-9
Purity >98%
Solubility DMSO 15 mg/ml
Storage at -20°C
References

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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Keywords: Icilin, AG 3-5 supplier, TRP Channel, inhibitors

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