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AB145874

AMG 9810, TRPV1 receptor antagonist

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(1 Publication)

MW 337.4 Da, Purity >99%. Potent, 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. Active in vitro and in vivo.

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1 Images
Chemical Structure - AMG 9810, TRPV1 receptor antagonist (AB145874)
  • Chemical Structure

Lab

Chemical Structure - AMG 9810, TRPV1 receptor antagonist (AB145874)

2D chemical structure image of ab145874, AMG 9810, TRPV1 receptor antagonist

Key facts

CAS number

545395-94-6

Purity

>99%

Form

Solid

form

Formulation

Constituents: 100% 2E-N-(2,3-Dihydro-1,4-benzodioxin-6-yl)-3-[4-(1,1-dimethylethyl)phenyl]-2-propenamide

Molecular weight

337.4 Da

Molecular formula

C<sub>2</sub><sub>1</sub>H<sub>2</sub><sub>3</sub>NO<sub>3</sub>

PubChem

680502

Nature

Synthetic

Solubility

Soluble in ethanol to 100 mM

Soluble in DMSO to 100 mM

Biochemical name

Amg-9810

Biological description

Potent, 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. Active in vitro and in vivo.

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Canonical smiles

CC(C)(C)C1=CC=C(C=C1)C=CC(=O)NC2=CC3=C(C=C2)OCCO3

Isomeric smiles

CC(C)(C)C1=CC=C(C=C1)/C=C/C(=O)NC2=CC3=C(C=C2)OCCO3

InChi

InChI=1S/C21H23NO3/c1-21(2,3)16-7-4-15(5-8-16)6-11-20(23)22-17-9-10-18-19(14-17)25-13-12-24-18/h4-11,14H,12-13H2,1-3H3,(H,22,23)/b11-6+

InChiKey

GZTFUVZVLYUPRG-IZZDOVSWSA-N

IUPAC Name

(E)-3-(4-tert-butylphenyl)-N-(2,3-dihydro-1,4-benzodioxin-6-yl)prop-2-enamide

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Complementary Products

Primary Antibodies

AB267556

PE Anti-IL2 Receptor beta/p75 antibody [EPR22892-2]

RabMAb|Recombinant

Flow Cytometry - PE Anti-IL2 Receptor beta/p75 antibody [EPR22892-2] (AB267556)

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Primary Antibodies

AB243179

Anti-Ferredoxin--nitrite reductase antibody

Western blot - Anti-Ferredoxin--nitrite reductase antibody (AB243179)

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  • 0
Primary Antibodies

AB89821

Anti-Perforin antibody [5B10]

Immunohistochemistry (Formalin/PFA-fixed paraffin-embedded sections) - Anti-Perforin antibody [5B10] (AB89821)

  • 0
  • 0
Primary Antibodies

AB171744

Anti-PKLR antibody [EPR11093]

BOND RX™ Validated|RabMAb|Recombinant

Immunohistochemistry (Formalin/PFA-fixed paraffin-embedded sections) - Anti-PKLR antibody [EPR11093] (AB171744)

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Properties and storage information

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
Store under desiccating conditions|The product can be stored for up to 12 months
Handling instructions

Need more advice on solubility, usage and handling? Please visit our our product support page for more details.

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Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.

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Refer to SDS for further information.

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Supplementary information

This supplementary information is collated from multiple sources and compiled automatically.

TRPV1 also known as the transient receptor potential vanilloid 1 or capsaicin receptor is a non-selective cation channel with a molecular mass of approximately 95 kDa. It acts mechanically by allowing the influx of calcium and sodium ions upon activation. This receptor is expressed predominantly in sensory neurons specifically in dorsal root ganglia and trigeminal ganglia which are key regions involved in pain perception. TRPV1 can also be found in various non-neuronal tissues influencing a range of physiological responses.
Biological function summary

The role of TRPV1 extends beyond sensory perception. It is involved in detecting and regulating body temperature and is activated by heat acidic conditions and certain lipid metabolites. The receptor operates as part of a homotetrameric complex contributing to neural signaling. It is activated by chemical ligands such as capsaicin the compound responsible for the spicy sensation in chili peppers influencing pain and inflammation pathways.

Pathways

TRPV1 plays essential roles in pain and nociception pathways. It intersects with the inflammatory pathway where its activity is modulated by protein kinase C (PKC) and phospholipase C (PLC). These pathways involve calcium signaling and relate to proteins such as PKA and calcineurin which modulate TRPV1 activity through phosphorylation and dephosphorylation affecting the body's response to noxious stimuli.

TRPV1 is a critical player in pain management and inflammatory disorders. It has been linked to chronic pain conditions like neuropathic pain and is also involved in migraine pathophysiology. In these contexts TRPV1 interacts with proteins like CGRP and TRPA1 which are also implicated in pain signaling and migraine mechanisms. Antagonists such as capsazepine AMG 9810 and AMG-517 have been researched for therapeutic targeting of TRPV1 in these disorders.
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Product protocols

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Publications (1)

Recent publications for all applications. Explore the full listand refine your search

ACS pharmacology & translational science 7:236-248 PubMed38230281

2024

Optogenetic Activation of Peripheral Somatosensory Neurons in Transgenic Mice as a Neuropathic Pain Model for Assessing the Therapeutic Efficacy of Analgesics.

Applications

Unspecified application

Species

Unspecified reactive species

Hao-Hao Chen,Muhammad Mohsin,Jia-Yi Ge,Yu-Ting Feng,Jing-Ge Wang,Yu-Sen Ou,Zuo-Jie Jiang,Bo-Ya Hu,Xing-Jun Liu
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Product promise

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