Home Transmembrane Transporters TRP Channel antagonist - TLR inhibitor AMG-9810 For research use only.

AMG-9810

AMG-9810 is a potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.

AMG-9810 Chemical Structure

AMG-9810 Chemical Structure

CAS: 545395-94-6

Purity & Quality Control

Batch: Purity: 99.95%
99.95

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Biological Activity

Description AMG-9810 is a potent, competitive and selective vanilloid receptor 1 (TRPV1) antagonist and inhibits capsaicin activation with IC50 of 24.5 nM and 85.6 nM for human TRPV1 and rat TRPV1, repectively. AMG-9810 blocks all known modes of TRPV1 activation, including protons-, heat-, and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG-9810 significantly reduces the mRNA expression of TLR2 and TLR4. AMG-9810 also promotes mouse skin tumorigenesis mediated through EGFR/Akt/mTOR signaling.
Targets
TLR2 [2] TLR4 [2] hTRPV1 [1]
(Cell-free assay)		 rTRPV1 [1]
(Cell-free assay)
24.5 nM 85.6 nM

Chemical lnformation & Solubility

Molecular Weight 337.41 Formula

C21H23NO3
CAS No. 545395-94-6 SDF --
Smiles CC(C)(C)C1=CC=C(/C=C/C(=O)NC2=CC=C3OCCOC3=C2)C=C1
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 67 mg/mL ( (198.57 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 22 mg/mL

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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