AMG9810

Name: AMG9810
Brand: MedChemExpress
SKU: HY-101736
Rating: 5.0 (11 reviews)

製品番号: HY-101736 純度: 99.48%: Data Sheet SDS COA 取扱説明書
FAQs
Technical Support

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.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

CAS 番号 : 545395-94-6

容量	価格（税別）	在庫状況	数量

>無料サンプル (0.1 - 0.2 mg)		今すぐ申し込む
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 60	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 60	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$55	在庫あり	Estimated Time of Arrival: December 31
10 mg	$72	在庫あり	Estimated Time of Arrival: December 31
25 mg	$150	在庫あり	Estimated Time of Arrival: December 31
50 mg	$240	在庫あり	Estimated Time of Arrival: December 31
100 mg	$385	在庫あり	Estimated Time of Arrival: December 31
200 mg		お問い合わせ
500 mg		お問い合わせ

or バルクお問い合わせ

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

カスタマーレビュー

Based on 11 publication(s) in Google Scholar

Other Forms of AMG9810:

AMG9810 (Standard) お問い合わせ

顧客検証

RT-PCR

Cell Imaging/Staining

In Vivo Efficacy Study

: 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.

: 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.

: 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.

: 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).

: 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.

TRP Channel アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示

TRPA1 TRPC3 TRPC4 TRPC5 TRPC6 TRPC7 TRPM8 TRPM2 TRPM3 TRPM4 TRPM7 TRPML1 TRPML2 TRPML3 TRPV1 TRPV2 TRPV3 TRPV4 TRPV6

生物活性
プロトコル
純度とドキュメンテーション
参考文献
カスタマーレビュー

製品説明

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]

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	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	0.023 × 10^-6M Compound: 1	Inhibition of rat human chimera TRPV1 channel expressed in CHO cells Inhibition of rat human chimera TRPV1 channel expressed in CHO cells	[PMID: 17948977]
CHO	IC₅₀	0.023 x 10^-6M Compound: 1	Inhibition of rat human chimera TRPV1 channel expressed in CHO cells Inhibition of rat human chimera TRPV1 channel expressed in CHO cells	[PMID: 17948977]
CHO	IC₅₀	0.136 × 10^-6M Compound: 91	Inhibition of rat human chimera TRPV1 channel expressed in CHO cells Inhibition of rat human chimera TRPV1 channel expressed in CHO cells	[PMID: 17948977]
CHO	IC₅₀	0.136 x 10^-6M Compound: 91	Inhibition of rat human chimera TRPV1 channel expressed in CHO cells Inhibition of rat human chimera TRPV1 channel expressed in CHO cells	[PMID: 17948977]
CHO	IC₅₀	1200 nM Compound: 34	Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells	[PMID: 15634002]
CHO	IC₅₀	150 nM Compound: 1	Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells	[PMID: 15634002]
CHO	IC₅₀	17 nM Compound: 1	Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells Inhibition of capsaicin-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells	[PMID: 15634002]
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	3200 nM Compound: 34	Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells Inhibition of pH-induced calcium uptake by transient receptor potential vanilloid type 1 expressed in CHO cells	[PMID: 15634002]
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]
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]

体外実験

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.

体内実験

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.

分子量

337.41

分子式

C₂₁H₂₃NO₃

CAS 番号

545395-94-6

Appearance

Solid

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

輸送条件

Room temperature in continental US; may vary elsewhere.

保管条件

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶剤 & 溶解度

体外:

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the 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.

Molarity Calculator
Dilution Calculator

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

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）

体積 _（開始）

濃度 _（終了）

体積 _（終了）

体内:

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.

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
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.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

純度とドキュメンテーション

純度: 99.48%

Select Batch:

データシート (278 KB) SDS (392 KB)

COA (245 KB) HNMR (269 KB) LCMS (95 KB)

取扱説明書 (2659 KB)

参考文献

[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]

キナーゼ実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
細胞実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
動物実験 ^[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) はこれらの方法の精度を確認していません。こちらは参照専用です。
参考文献	[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

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

AMG9810 Related Classifications

Neurological Disease

Molarity Calculator
Dilution Calculator

The molarity calculator equation

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

質量		濃度		体積		分子量 *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

一般には略語で表示されます：C₁V₁ = C₂V₂

濃度 _（開始）	×	体積 _（開始）	=	濃度 _（終了）	×	体積 _（終了）
	×		=		×
C1		V1		C2		V2

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

AMG9810545395-94-6AMG 9810AMG-9810TRP ChannelTransient receptor potential channelsInhibitorinhibitorinhibit

最近チェックした製品:

製品名

カスタマ需要量 *

お名前 *

タイトル

メールアドレス *

電話番号 *

デパートメント

組纖名 *

市区町村

都道府県

国或いは地域 *

必ず会社名を記載ください。個人への返信は行いません。

備考

製品名

Lot #

お名前 *

メールアドレス *

電話番号 *

部門 *

組纖名 *

国或いは地域 *

備考

AMG9810

カスタマーレビュー

Other Forms of AMG9810:

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

TRP Channel アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AMG9810 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

お名前
メール *

	Sorry, but the email address you supplied was invalid.

AMG9810

カスタマーレビュー

Other Forms of AMG9810:

AMG9810 関連抗体

顧客検証

おすすめ

•関連スクリーニングライブラリ:

•関連小分子:

•関連タンパク質:

TRP Channel アイソフォーム固有の製品をすべて表示:

生物活性

プロトコル

純度とドキュメンテーション

参考文献

カスタマーレビュー

AMG9810 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AMG9810 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

Keywords:

最近チェックした製品:

カスタマーレビュー

Request for HNMR Report

Request for HNMR Report