AM-2099

Name: AM-2099
Brand: MedChemExpress
SKU: HY-100727
Rating: 4.5 (1 reviews)

製品番号: HY-100727 純度: 98.37%: Data Sheet SDS COA 取扱説明書
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Technical Support

AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC₅₀ of 0.16 μM for human Nav1.7.

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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。

AM-2099 構造式

CAS 番号 : 1443373-17-8

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 92	在庫あり	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 92	在庫あり	Estimated Time of Arrival: December 31
Solid
5 mg	$90	在庫あり	Estimated Time of Arrival: December 31
10 mg	$150	在庫あり	Estimated Time of Arrival: December 31
25 mg	$260	在庫あり	Estimated Time of Arrival: December 31
50 mg	$400	在庫あり	Estimated Time of Arrival: December 31
100 mg	$650	在庫あり	Estimated Time of Arrival: December 31
250 mg	$1140	在庫あり	Estimated Time of Arrival: December 31
500 mg	$1820	在庫あり	Estimated Time of Arrival: December 31
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カスタマーレビュー

Based on 1 publication(s) in Google Scholar

Other Forms of AM-2099:

AM-2099 (Standard) お問い合わせ

顧客検証

•bioRxiv. 2026 Mar 26.

Sodium 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

Na_v1.1 Na_v1.2 Na_v1.3 Na_v1.4 Na_v1.5 Na_v1.6 Na_v1.7 Na_v1.8 Na_v1.9

生物活性
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参考文献
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製品説明

AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC₅₀ of 0.16 μM for human Nav1.7.

IC₅₀ & Target

Nav1.7

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	2.1 μM Compound: 16	Inhibition of 20% inactivated human Nav1.2 expressed in CHO cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.2 expressed in CHO cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
CHO	IC₅₀	21 μM Compound: 16	Inhibition of 20% inactivated human Nav1.3 expressed in CHO cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.3 expressed in CHO cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
CHO	IC₅₀	> 30 μM Compound: 16	Inhibition of 20% inactivated human Nav1.8 expressed in CHO cells assessed as inhibition of TTX-resistant current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.8 expressed in CHO cells assessed as inhibition of TTX-resistant current by whole cell patch clamp method	[PMID: 27994738]
HEK-293T	IC₅₀	0.16 μM Compound: 16	Inhibition of 20% inactivated cynomolgus monkey Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of 20% inactivated cynomolgus monkey Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK-293T	IC₅₀	0.18 μM Compound: 16	Inhibition of 20% inactivated dog Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of 20% inactivated dog Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK-293T	IC₅₀	3.5 μM Compound: 16	Inhibition of 20% inactivated rat Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of 20% inactivated rat Nav1.7 expressed in HEK293T cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK293	IC₅₀	0.009 μM Compound: 16	Inhibition of human Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -60 mV measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of human Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -60 mV measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK293	IC₅₀	0.14 μM Compound: 16	Inhibition of 20% inactivated human Nav1.7 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.7 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK293	IC₅₀	0.16 μM Compound: 1	Inhibition of human Nav1.7 expressed in HEK293 cells incubated for 3 to 5 mins at -125 mV holding potential by electrophysiology assay Inhibition of human Nav1.7 expressed in HEK293 cells incubated for 3 to 5 mins at -125 mV holding potential by electrophysiology assay	[PMID: 28287723]
HEK293	IC₅₀	0.16 μM Compound: 16	Inhibition of human Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -125 mV measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of human Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -125 mV measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK293	IC₅₀	0.18 μM Compound: 16	Inhibition of 20% inactivated mouse Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of 20% inactivated mouse Nav1.7 expressed in HEK293 cells assessed as inhibition of sodium current measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK293	IC₅₀	16 μM Compound: 16	Inhibition of 20% inactivated human Nav1.5 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.5 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK293	IC₅₀	17 μM Compound: 16	Inhibition of 20% inactivated human Nav1.4 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.4 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK293	IC₅₀	3.7 μM Compound: 16	Inhibition of 20% inactivated human Nav1.6 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.6 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK293	IC₅₀	7.2 μM Compound: 16	Inhibition of human Nav1.7 in closed state expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -140 mV measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of human Nav1.7 in closed state expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -140 mV measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]
HEK293	IC₅₀	7.3 μM Compound: 16	Inhibition of 20% inactivated human Nav1.1 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method Inhibition of 20% inactivated human Nav1.1 expressed in HEK293 cells assessed as inhibition of peak inward current by whole cell patch clamp method	[PMID: 27994738]
HEK293	IC₅₀	> 30 μM Compound: 1	Inhibition of human Nav1.5 expressed in HEK293 cells assessed as reduction in peak inward current by ionworks quattro electrophysiology assay Inhibition of human Nav1.5 expressed in HEK293 cells assessed as reduction in peak inward current by ionworks quattro electrophysiology assay	[PMID: 28287723]
HEK293	IC₅₀	> 30 μM Compound: 16	Displacement of [3H]dofetilide from human ERG expressed in HEK293 cell membranes measured after 90 mins by TopCount scintillation counting method Displacement of [3H]dofetilide from human ERG expressed in HEK293 cell membranes measured after 90 mins by TopCount scintillation counting method	[PMID: 27994738]
HEK293	IC₅₀	> 30 μM Compound: 16	Inhibition of human Nav1.5 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -125 mV measured for 3 to 5 mins by whole cell voltage clamp method Inhibition of human Nav1.5 expressed in HEK293 cells assessed as inhibition of sodium current at holding potential of -125 mV measured for 3 to 5 mins by whole cell voltage clamp method	[PMID: 27994738]

体外実験

In heterologous cells, comparable inhibition is observed across human, mouse, dog, and cynomolgus monkey NaV1.7 with reduced activity against rat NaV1.7. AM-2099 is more than 100-fold selective over Nav1.3, Nav1.4, Nav1.5, and Nav1.8, while lower levels of selectivity are observed against Nav1.1, Nav1.2, and Nav1.6. AM-2099 demonstrates low affinity for hERG (>30 μM) and does not show greater than 50% inhibition against a panel of 100 kinases (1 μM) and a broad CEREP panel (10 μM). ^[1].

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

体内実験

AM-2099 demonstrates a favorable pharmacokinetic profile in rat and dog. In rats AM-2099 shows low total clearance and moderate Vdss and half-life. In contrast, when dosed in dogs AM-2099 shows very low clearance, a low Vdss and long halflife (18 h). AM-2099 demonstrates a dose-dependent increase in plasma exposure with a concomitant dose-dependent reduction in scratching bouts compared to vehicle-treated animals, with a statistically significant reduction observed at the 60 mg/kg dose^[1].

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

分子量

466.46

分子式

C₁₉H₁₃F₃N₄O₃S₂

CAS 番号

1443373-17-8

Appearance

Solid

Color

White to light yellow

SMILES

COC1=CC(C(F)(F)F)=CC=C1C2=NC=NC3=CC(S(=O)(NC4=NC=CS4)=O)=CC=C32

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 : ≥ 150 mg/mL (321.57 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	2.1438 mL	10.7190 mL	21.4381 mL
5 mM	0.4288 mL	2.1438 mL	4.2876 mL
10 mM	0.2144 mL	1.0719 mL	2.1438 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 (5.36 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 (5.36 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.

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: 98.37%

Select Batch:

データシート (278 KB) SDS (252 KB)

COA (255 KB) HNMR (156 KB) LCMS (339 KB)

取扱説明書 (2659 KB)

参考文献

[1]. Marx IE, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. [Content Brief]

動物実験 ^[1]	Mice: AM-2099 (5, 20, 60 mg/kg) is dosed orally to C57BL/6 male mice 120 minutes prior to intradermal administration of histamine. Instances of scratching behavior are then measured over a 30-minute time period^[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]. Marx IE, et al. Sulfonamides as Selective NaV1.7 Inhibitors: Optimizing Potency and Pharmacokinetics to Enable in Vivo Target Engagement. ACS Med Chem Lett. 2016 Sep 21;7(12):1062-1067. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1438 mL	10.7190 mL	21.4381 mL	53.5952 mL
	5 mM	0.4288 mL	2.1438 mL	4.2876 mL	10.7190 mL
	10 mM	0.2144 mL	1.0719 mL	2.1438 mL	5.3595 mL
	15 mM	0.1429 mL	0.7146 mL	1.4292 mL	3.5730 mL
	20 mM	0.1072 mL	0.5360 mL	1.0719 mL	2.6798 mL
	25 mM	0.0858 mL	0.4288 mL	0.8575 mL	2.1438 mL
	30 mM	0.0715 mL	0.3573 mL	0.7146 mL	1.7865 mL
	40 mM	0.0536 mL	0.2680 mL	0.5360 mL	1.3399 mL
	50 mM	0.0429 mL	0.2144 mL	0.4288 mL	1.0719 mL
	60 mM	0.0357 mL	0.1787 mL	0.3573 mL	0.8933 mL
	80 mM	0.0268 mL	0.1340 mL	0.2680 mL	0.6699 mL
	100 mM	0.0214 mL	0.1072 mL	0.2144 mL	0.5360 mL

AM-2099 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:

AM-20991443373-17-8AM2099AM 2099Sodium ChannelNa channelsNa+ channelsInhibitorinhibitorinhibit

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Molarity Calculator

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Complete Stock Solution Preparation Table

AM-2099 Related Classifications

Molarity Calculator

Dilution Calculator

The molarity calculator equation

The dilution calculator equation

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AM-2099

カスタマーレビュー

Other Forms of AM-2099:

AM-2099 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:

Sodium 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

AM-2099 関連抗体

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

AM-2099 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:

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