AMG 9810

Cat. No. 2316

AMG 9810 C21H23NO3 [545395-94-6]

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Chemical Name: (2E)-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propenamide

Biological Activity

Potent and selective, competitive vanilloid TRPV1 receptor antagonist (IC50 = 17 nM). Inhibits capsaicin-, proton-, heat- and endogenous ligand-induced activation of human and rat recombinant TRPV1 receptors. Displays antihyperalgesic properties in a rat model of inflammatory pain.

Technical Data

M.Wt:
337.42
Formula:
C21H23NO3
Solubility:
Soluble to 50 mM in DMSO and to 100 mM in ethanol
Purity:
>98 %
Storage:
Desiccate at +4°C
CAS No:
545395-94-6

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.

Certificate of Analysis / Safety Data Sheet

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Doherty et al (2005) Discovery of potent, orally available vanilloid receptor-1 antagonists. Structure-activity relationship of N-aryl cinnamides. J.Med.Chem. 48 71. PMID: 15634002.

Gavva et al (2005) AMG 9810 [(E)-3-(4-t-Butylphenyl)-N-(2,3-dihydrobenzo[b][1,4]dioxin-6-yl)acrylamide], a novel vanilloid receptor 1 (TRPV1) antagonist with antihyperalgesic properties. J.Pharmacol.Exp.Ther. 313 474. PMID: 15615864.

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Citations are publications that use Tocris products. Selected citations for AMG 9810 include:

Gregus et al (2012) Spinal 12-lipoxygenase-derived hepoxilin A3 contributes to inflammatory hyperalgesia via activation of TRPV1 and TRPA1 receptors. Proc Natl Acad Sci U S A 109 6721. PMID: 22493235.

Sisignano et al (2012) 5,6-EET is released upon neuronal activity and induces mechanical pain hypersensitivity via TRPA1 on central afferent terminals. J Neurosci 32 6364. PMID: 22553041.

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Keywords: AMG 9810, supplier, Potent, selective, competitive, antagonists, TRPV1, Vanillioid, Receptors, VR1, Channels, Transient, Receptor, Potential, AMG9810, Tocris Bioscience, TRPV Antagonist products

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