AMG 517
Chemical Name: N-[4-[[6-[4-(Trifluoromethyl)phenyl]-4-pyrimidinyl]oxy]-2-benzothiazolyl]acetamide
Purity: ≥98%
Biological Activity
AMG 517 is a potent TRPV1 antagonist (IC50 = 0.9 nM). Inhibits capsaican-induced flinching and reverses analgesia in an inflammatory pain model in rats. Orally bioavailable.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Novel vanilloid receptor-1 antagonists: 2. Structure-activity relationships of 4-oxopyrimidines leading to the selection of a clinical candidate.
Doherty et al.
J.Med.Chem., 2007;50:3515 -
Repeated administration of vanilloid receptor TRPV1 antagonists attenuates hyperthermia elicited by TRPV1 blockade.
Gavva et al.
J.Pharmacol.Exp.Ther., 2007;323:128 -
Novel vanilloid receptor-1 antagonists: 3. The identification of a second-generation clinical candidate with improved physicochemical and pharmacokinetic properties.
Wang et al.
J.Med.Chem., 2007;50:3528
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