AMG 9810

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Cat.No. 2316 - AMG 9810 | C21H23NO3 | CAS No. 545395-94-6
Description: Potent and selective, competitive antagonist of TRPV1
Chemical Name: (2E)-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propenamide
Purity: ≥98% (HPLC)
Datasheet
Citations (14)
Reviews
Literature

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.

Compound Libraries

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Technical Data

M. Wt 337.42
Formula C21H23NO3
Storage Desiccate at +4°C
Purity ≥98% (HPLC)
CAS Number 545395-94-6
PubChem ID 680502
InChI Key GZTFUVZVLYUPRG-IZZDOVSWSA-N
Smiles CC(C)(C)C1=CC=C(C=C1)\C=C\C(=O)NC1=CC=C2OCCOC2=C1

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 16.87 50
ethanol 33.74 100

Preparing Stock Solutions

The following data is based on the product molecular weight 337.42. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.96 mL 14.82 mL 29.64 mL
5 mM 0.59 mL 2.96 mL 5.93 mL
10 mM 0.3 mL 1.48 mL 2.96 mL
50 mM 0.06 mL 0.3 mL 0.59 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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References

References are publications that support the biological activity of the product.

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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Keywords: AMG 9810, AMG 9810 supplier, Potent, selective, competitive, antagonists, TRPV1, Vanillioid, Receptors, VR1, Channels, Transient, Receptor, Potential, AMG9810, TRPV, 2316, Tocris Bioscience

14 Citations for AMG 9810

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

Mouchbahani-Constance et al (2018) Lionfish venom elicits pain predominantly through the actiation of non-peptidergic nociceptors. Pain PMID: 29965829

David-Pereira (2017) The medullary dorsal reticular nucleus as a relay for descending pronociception induced by the mGluR5 in the rat infralimbic cortex. Neuroscience 349 341 PMID: 28300633

Park et al (2011) Resolvin D2 is a potent endogenous inhibitor for transient receptor potential subtype V1/A1, inflammatory pain, and spinal cord synaptic plasticity in mice: distinct roles of resolvin D1, D2, and E1. Front Cell Neurosci 31 18433 PMID: 22171045

Pitcher et al (2007) Spinal NKCC1 blockade inhibits TRPV1-dependent referred allodynia. J Transl Med 3 17 PMID: 17603899

Wang et al (2015) Mother root of Aconitum carmichaelii Debeaux exerts antinociceptive effect in Complet Freund's Adjuvant-induced mice: roles of dynorpin/κ-opioid system and transient receptor potential vanilloid type-1 ion channel. Proc Natl Acad Sci U S A 13 284 PMID: 26320055

Martin et al (2015) Endocannabinoids Mediate Muscarinic Acetylcholine Receptor-Dependent Long-Term Depression in the Adult Medial Prefrontal Cortex. Oncotarget 9 457 PMID: 26648844

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

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

Montrucchio et al (2013) Plant derived aporphinic alkaloid S-(+)-dicentrine induces antinociceptive effect in both acute and chronic inflammatory pain models: evidence for a role of TRPA1 channels. PLoS One 8 e67730 PMID: 23861794

Saloman et al (2013) P2X? and TRPV1 functionally interact and mediate sensitization of trigeminal sensory neurons. Neuroscience 232 226 PMID: 23201260

Li et al (2015) The Cancer Chemotherapeutic Paclitaxel Increases Human and Rodent Sensory Neuron Responses to TRPV1 by Activation of TLR4. J Neurosci 35 13487 PMID: 26424893

Hakimizadeh et al (2012) Endocannabinoid System and TRPV1 Receptors in the Dorsal Hippocampus of the Rats Modulate Anxiety-like Behaviors. Iran J Basic Med Sci 15 795 PMID: 23493622

Yan et al (2011) Dural afferents express acid-sensing ion channels: a role for decreased meningeal pH in migraine headache. Pain 152 106 PMID: 20971560

Patwardhan et al (2009) Activation of TRPV1 in the spinal cord by oxidized linoleic acid metabolites contributes to inflammatory hyperalgesia. J Neurosci 106 18820 PMID: 19843694


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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


Pain

Pain Research Product Guide

A collection of over 250 products for pain research, the guide includes research tools for the study of:

  • Nociception
  • Ion Channels
  • G-Protein-Coupled Receptors
  • Intracellular Signaling
Pain

Pain Poster

Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.