AMG9810
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.
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- Pureza: 99.48%
- No. CAS: 545395-94-6
- Fòrmula: C21H23NO3
- Peso molecular:337.41
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Protocolo
- Pureza y Documentación
- Referencias
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Publications Citing Use of MedChemExpress (MCE) AMG9810
More- Bioact Mater. 2025 Apr 4:50:134-151. [Abstract]
- Neuron. 2024 Jun 5;112(11):1815-1831.e4. [Abstract]
- Inflammopharmacology. 2024 Dec;32(6):3745-3759. [Abstract]
- Commun Biol. 2025 May 10;8(1):724. [Abstract]
- Int Immunopharmacol. 2025 Aug 13:164:115330. [Abstract]
- FASEB J. 2025 May 31;39(10):e70657. [Abstract]
- Stem Cell Rev Rep. 2021 Jun;17(3):999-1013. [Abstract]
- J Biol Chem. 2021 Jul;297(1):100806. [Abstract]
- Tissue Cell. 2025 Nov 21:99:103243. [Abstract]
- Cytotechnology. 2025 Aug;77(4):141. [Abstract]
- SSRN. 2025 Jul 2.
Customer Validation & Images
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In Vivo Efficacy Study
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RT-PCR
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Cell Imaging/Staining
Actividad biológica
IC50: 24.5 nM (human TRPV1), 85.6 nM (rat TRPV1)[1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| Caco-2 | CC50 |
14.22 μM
Compound: AMG-9810
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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
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10.21203/rs.3.rs-23951/v1 |
| Caco-2 | IC50 |
14.97 μM
Compound: AMG-9810
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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
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10.21203/rs.3.rs-23951/v1 |
| CHO | IC50 |
25 nM
Compound: 6
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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
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[PMID: 17489570] |
| CHO | IC50 |
294 nM
Compound: 6
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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
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[PMID: 17489570] |
| CHO | IC50 |
86 nM
Compound: 6
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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
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[PMID: 17489570] |
| CHO | IC50 |
93 nM
Compound: 6
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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
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[PMID: 17489570] |
| CHO | EC50 |
>4 μM
Compound: 9
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Agonist activity at TRPV1 expressed in CHO cells
Agonist activity at TRPV1 expressed in CHO cells
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[PMID: 17585749] |
| CHO | IC50 |
350 nM
Compound: 9
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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
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[PMID: 17585749] |
| CHO | IC50 |
79 nM
Compound: 9
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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
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[PMID: 17585749] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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No. CAS 545395-94-6
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Appearance Solid
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Peso molecular 337.41
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Fòrmula C21H23NO3
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Color White to light yellow
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SMILES
O=C(NC1=CC=C(OCCO2)C2=C1)/C=C/C3=CC=C(C(C)(C)C)C=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (11)
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Journal Impact Factor
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Most Recent
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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 Trpv1T634A/T634A mice.
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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
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.
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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.
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Stem Cell Rev Rep
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).
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J Biol Chem
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.
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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 -
Solvente y solubilidad
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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocolo
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.
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.
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.
Pureza y Documentación
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Ficha de datos (278 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
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