Cat. No. 5995
Chemical Name: N-[4-[[6-[4-(Trifluoromethyl)phenyl
Biological ActivityPotent TRPV1 antagonist (IC50 = 0.9 nM). Inhibits capsaican-induced flinching and reverses analgesia in an inflammatory pain model in rats. Orally bioavailable.
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All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Product Datasheet / Safety Datasheet
Doherty et al (2007) Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate. J.Med.Chem. 50 3515. PMID: 17585750.
Gavva et al (2007) Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade. J.Pharmacol.Exp.Ther. 323 128. PMID: 17652633.
Wang et al (2007) Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties. J.Med.Chem. 50 3528. PMID: 17585751.
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Keywords: AMG 517, supplier, AMG517, potent, TRPV1, transient, potential, channels, antagonists, pain, antihyperalgesia, Tocris Bioscience, TRPV Antagonist products