Art. -Nr.: HY-101736

AMG9810

11 Cited Publications

Kundenbewertung

Based on 11 publication(s) in Google Scholar

AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC₅₀ values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.48%
CAS. Nr.: 545395-94-6
Formel: C₂₁H₂₃NO₃
Molecular Weight:337.41

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

AMG9810 Chemical Structure

CAS. Nr.: 545395-94-6

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (11)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

AMG9810 is a selective and competitive vanilloid receptor 1 (TRPV1) antagonist with IC₅₀ values of 24.5 and 85.6 nM for human and rat TRPV1, repectively.

IC₅₀ & Target

IC50: 24.5 nM (human TRPV1), 85.6 nM (rat TRPV1)^[1]

Alle TRP Channel Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	14.22 μM Compound: AMG-9810	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	14.97 μM Compound: AMG-9810	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
CHO	IC₅₀	25 nM Compound: 6	Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay	[PMID: 17489570]
CHO	IC₅₀	294 nM Compound: 6	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay	[PMID: 17489570]
CHO	IC₅₀	86 nM Compound: 6	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay Antagonist activity at rat TRPV1 expressed in CHO cells assessed as blockade of capsaicin-induced receptor activation by [45Ca2+] uptake assay	[PMID: 17489570]
CHO	IC₅₀	93 nM Compound: 6	Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay Antagonist activity at human TRPV1 expressed in CHO cells assessed as blockade of acid-induced receptor activation by [45Ca2+] uptake assay	[PMID: 17489570]
CHO	EC₅₀	>4 μM Compound: 9	Agonist activity at TRPV1 expressed in CHO cells Agonist activity at TRPV1 expressed in CHO cells	[PMID: 17585749]
CHO	IC₅₀	350 nM Compound: 9	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of acid-induced calcium influx	[PMID: 17585749]
CHO	IC₅₀	79 nM Compound: 9	Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx Antagonist activity at rat TRPV1 expressed in CHO cells assessed as inhibition of capsaicin-induced calcium influx	[PMID: 17585749]

In Vitro

AMG9810 is a competitive antagonist of capsaicin activation (IC₅₀ value for human TRPV1, 24.5±15.7 nM; rat TRPV1, 85.6±39.4 nM) and blocks all known modes of TRPV1 activation, including protons (IC₅₀ value for rat TRPV1, 294±192 nM; human TRPV1, 92.7±72.8 nM), heat (IC₅₀ value for rat TRPV1, 21±17 nM; human TRPV1, 15.8±10.8 nM), and endogenous ligands, such as anandamide, N-arachidonyl dopamine, and oleoyldopamine. AMG9810 blocks capsaicin-evoked depolarization and calcitonin gene-related peptide release in cultures of rat dorsal root ganglion primary neurons. AMG9810 inhibits capsaicin-, proton-, heat-, and endogenous ligand-induced uptake of ⁴⁵Ca²⁺ into TRPV1-expressing cells^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

AMG9810 is effective at preventing capsaicin-induced eye wiping in a dose-dependent manner, and it reverses thermal and mechanical hyperalgesia in a model of inflammatory pain induced by intraplantar injection of complete Freund's adjuvant. At effective doses, AMG9810 does not show any significant effects on motor function. AMG9810 is the first cinnamide TRPV1 antagonist reported to block capsaicin-induced eye wiping behavior and reverse hyperalgesia in an animal model of inflammatory pain^[1]. AMG9810, promotes mouse skin tumor development. The topical application of AMG9810 results in a significant increase in the expression level of the epidermal growth factor receptor (EGFR) and its downstream Akt/mammalian target of rapamycin (mTOR)-signaling pathway^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Chemical Information

CAS. Nr. 545395-94-6
Appearance Solid
Molecular Weight 337.41
Formel C₂₁H₂₃NO₃
Color White to light yellow
SMILES

O=C(NC1=CC=C(OCCO2)C2=C1)/C=C/C3=CC=C(C(C)(C)C)C=C3
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (11)

All RT-PCRCell Imaging/StainingIn Vivo Efficacy Study

Sort by:

Journal Impact Factor

Bioact Mater

Janus piezoelectric adhesives regulate macrophage TRPV1/Ca2+/cAMP axis to stimulate tendon-to-bone healing by multi-omics analysis. [Abstract]

2025 Apr 4:50:134-151. PMID: 40242507
Neuron

TRPV1 analgesics disturb core body temperature via a biased allosteric mechanism involving conformations distinct from that for nociception. [Abstract]

2024 Jun 5;112(11):1815-1831.e4. PMID: 38492574

AMG9810 purchased from MedChemExpress. Usage Cited in: Neuron. 2024 Jun 5;112(11):1815-1831.e4. [Abstract]

AMG9810 (4 mg/kg; ip) markedly increased CBT in Trpv1^+/+ mice, and the effect was absent in Trpv1^-/- mice.

AMG9810 purchased from MedChemExpress. Usage Cited in: Neuron. 2024 Jun 5;112(11):1815-1831.e4. [Abstract]

AMG9810 (4 mg/kg; ip) markedly increased CBT in Trpv1^T634A/T634A mice.
Inflammopharmacology

A medicine and food homology formula prevents cognitive deficits by inhibiting neuroinflammation and oxidative stress via activating AEA-Trpv1-Nrf2 pathway. [Abstract]

2024 Dec;32(6):3745-3759. PMID: 39305407
Commun Biol

IL-33/ST2 drives inflammatory pain via CCL2 signaling and activation of TRPV1 and TRPM8. [Abstract]

2025 May 10;8(1):724. PMID: 40348921

AMG9810 purchased from MedChemExpress. Usage Cited in: Commun Biol. 2025 May 10;8(1):724. [Abstract]

AMG9810 (30 mg/kg; 200 μL; intraplantarly injected) attenuated IL-33-induced mechanical (E) and thermal hypersensitivity in ST2^−/− mice.
Int Immunopharmacol

Galanin regulates M1/M2 polarization of microglia after spinal cord injury through TRPV1/Ca2+/CaMKII/NRF2 signaling pathway. [Abstract]

2025 Aug 13:164:115330. PMID: 40811950
FASEB J

Capsazepine Inhibits Astrocyte Activation and Attenuates Neuroinflammation by Targeting Syntaxin 7. [Abstract]

2025 May 31;39(10):e70657. PMID: 40386937

AMG9810 purchased from MedChemExpress. Usage Cited in: FASEB J. 2025 May 31;39(10):e70657. [Abstract]

qPCR analysis of pro-inflammatory cytokines treated with TRPV1 in-hibitor. Levels of IL- 6 and C3 were measured in the primary astrocytes treated with Ctrl, 0.1 μg/mL LPS, 0.1 μg/mL LPS + 10 μM CZP, 0.1 μg/mL LPS + 30 μM CZP, 0.1 μg/mL LPS + 5 μM SB366791, 0.1 μg/mL LPS + 10 μM SB366791, 0.1 μg/mL LPS + 10 μM AMG9810 or 0.1 μg/mL LPS + 50 μM AMG9810.
Stem Cell Rev Rep

Satellite Glial Cells Give Rise to Nociceptive Sensory Neurons. [Abstract]

2021 Jun;17(3):999-1013. PMID: 33389681

AMG9810 purchased from MedChemExpress. Usage Cited in: Stem Cell Rev Rep. 2021 Jun;17(3):999-1013. [Abstract]

AMG9810 (5 µM; 10 min) significantly decreased calcium flux response induced by capsaicin; withdrawal of Trpv1 antagonist AMG9810 led to rapid calcium transients in response to capsaicin in Dorsal root ganglia (DRG) derived satellite glial cells (SGCs).
J Biol Chem

Molecular mechanism underlying modulation of TRPV1 heat activation by polyols. [Abstract]

2021 Jul;297(1):100806. PMID: 34022223

AMG9810 purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2021 Jul;297(1):100806. [Abstract]

AMG9810 (10, 30 mg/kg; ip) significantly increased the thermal paw withdrawal latency compared with the control group in rats.
Tissue Cell

Sensory neuron TRPV1-mediated macrophage polarization and immune response regulate dental implant osseointegration. [Abstract]

2025 Nov 21:99:103243. PMID: 41297248
Cytotechnology

S1P receptor 1 antagonist ponesimod alleviates postherpetic neuralgia in rats by normalizing spinal TRPV1 expression and inhibiting MAPK-mediated glial activation. [Abstract]

2025 Aug;77(4):141. PMID: 40642600
SSRN

2025 Jul 2.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : ≥ 33 mg/mL (97.80 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.9638 mL

14.8188 mL

29.6375 mL

5 mM

0.5928 mL

2.9638 mL

5.9275 mL

10 mM

0.2964 mL

1.4819 mL

2.9638 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (7.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

Kinase Assay^[1]

Cultured adult rat dorsal root ganglia neurons in 96-well plates are washed twice with release buffer to initiate the assay. CGRP release is induced by incubation of neurons with capsaicin for 10 min at room temperature. The cultures are preincubated with increasing concentrations of capsazepine or AMG9810 for 15 min, followed by 300 nM capsaicin activation for 10 min at room temperature. The extracellular medium is collected and the CGRP content is determined using a commercially kit^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[2]

To assess cyotoxicity of AMG9810, N/TERT1 cells are treated with different concentrations of AMG9810 (0.25, 0.5, 1, 5 μM) and cultured for various periods of time (24, 48, 72 h). The CellTiter 96 AQueous One Solution is added to each well and then cells are kept in a 37°C, 5% CO₂ incubator for 1 h. Absorbance is then measured at 492 and 690 nm with a plate reader^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

Rats: AMG9810 is dissolved in DMSO. Rats are acclimated for 30 to 45 min in a 30×30×30-cm Plexiglas chambers before the intraperitoneal injection of either vehicle (DMSO) or AMG 9810. Injections are made over a 5-s period in the lower right ventral quadrant of the abdomen either 15, 30, or 60 min before intraocular application of capsaicin. Intraocular application of capsaicin (3 μg/20 μL in 10% ethanol/PBS) or vehicle (20 μL in 10% ethanol/PBS) is done with a pipette, and the number of front paw eye wipes is counted over a 5-min period in 1-min intervals ^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Gavva NR, et al. AMG9810 [(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. 2005 Apr;313(1):474-84. [Content Brief]

[2]. Li S, et al. TRPV1-antagonist AMG9810 promotes mouse skin tumorigenesis through EGFR/Akt signaling. Carcinogenesis. 2011 May;32(5):779-85. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.9638 mL	14.8188 mL	29.6375 mL	74.0938 mL
	5 mM	0.5928 mL	2.9638 mL	5.9275 mL	14.8188 mL
	10 mM	0.2964 mL	1.4819 mL	2.9638 mL	7.4094 mL
	15 mM	0.1976 mL	0.9879 mL	1.9758 mL	4.9396 mL
	20 mM	0.1482 mL	0.7409 mL	1.4819 mL	3.7047 mL
	25 mM	0.1186 mL	0.5928 mL	1.1855 mL	2.9638 mL
	30 mM	0.0988 mL	0.4940 mL	0.9879 mL	2.4698 mL
	40 mM	0.0741 mL	0.3705 mL	0.7409 mL	1.8523 mL
	50 mM	0.0593 mL	0.2964 mL	0.5928 mL	1.4819 mL
	60 mM	0.0494 mL	0.2470 mL	0.4940 mL	1.2349 mL
	80 mM	0.0370 mL	0.1852 mL	0.3705 mL	0.9262 mL

Keywords

AMG9810

11 Cited Publications

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

AMG9810

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AMG9810

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG9810

Membrane Transporter/Ion Channel Compound Library

Neuronal Signaling Compound Library

Anti-Cancer Compound Library

Covalent Screening Library

Mechanoreceptors Compound Library

Pain-Related Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Cysteine Targeted Covalent Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AMG9810

Alle TRP Channel Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (11)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

AMG9810 Related Classifications

HY-101736 Related Classifications