AMG-517

Short Summary : TRPV1 antagonist,potent and highly selective

Category : Membrane Transporter/Ion Channel|TRPV1

Purity : 0.98

CAS Number : 659730-32-2

Formula : C20H13F3N4O2S

Molecular Weight : 430.4

SMILE : CC(=O)NC1=NC2=C(C=CC=C2S1)OC3=NC=NC(=C3)C4=CC=C(C=C4)C(F)(F)F

Solubility : >21.5mg/mL in DMSO

Storage : Store at -20°C

Description : AMG-517 is an antagonist of TRPV1 channel with IC50 value of 1-2 nM [1].TRP1, transient receptor potential cation channel subfamily V member 1, is a subfamily of the transient receptor potential protein group and plays an important role in detecting and regulating body temperature or sensing pain. TRPV1 can be activated by diverse stimuli, including several ingredients of the inflammatory soup which leads to a painful, burning sensation. It is reported that TRPV1 channel may play a pivotal role in many diseases like SIRS [1] [2]. AMG-517 is a TRPV1 antagonist. When tested with stable CHO cell lines expressing TRPV1, treated with AMG-517 inhibited the activation of TRPV1 [1]. In C57BL/6 mice with SIRS induced by LPS, pretreatment with AMG-517 (210 μg/kg) markedly decreased the survival rate and increased the risk of mortality [2]. When tested with Trpv1-/- mice, intraperitoneally treated with AMG-517 (256 nmol/kg) inhibited TRPV1 with inducing hyperthermia in a dose-dependent manner [3]. In capsaicin-induced flinch male Sprague-Dawley rats, oral administration of AMG-517 markedly decreased the number of flinches in a dose-dependent manner [1].References: [1].Gavva, N.R., et al., Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J Pharmacol Exp Ther, 2007. 323(1): p. 128-37.[2].Wanner, S.P., et al., Aging reverses the role of the transient receptor potential vanilloid-1 channel in systemic inflammation from anti-inflammatory to proinflammatory. Cell Cycle, 2012. 11(2): p. 343-9.[3].Garami, A., et al., Contributions of different modes of TRPV1 activation to TRPV1 antagonist-induced hyperthermia. J Neurosci, 2010. 30(4): p. 1435-40.

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