Cat. No.: HY-100727

AM-2099

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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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Pureté: 98.37%
CAS No.: 1443373-17-8
Formule: C₁₉H₁₃F₃N₄O₃S₂
Masse moléculaire:466.46

Stockage:

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

AM-2099 Chemical Structure

CAS No.: 1443373-17-8

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Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Solvant et solubilité
- In Vitro
- In Vivo
Protocole
Pureté et documentation
Références
Help & FAQs
Classifications
Bioz

Activité biologique

Description

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

Voir tous les produits spécifiques à Isoform Sodium Channel :

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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]
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]
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]

In Vitro

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.

In Vivo

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.

Chemical Information

CAS No. 1443373-17-8
Appearance Solid
Masse moléculaire 466.46
Formule C₁₉H₁₃F₃N₄O₃S₂
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
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

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

Publications (1)

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Journal Impact Factor

bioRxiv

2026 Mar 26.

Solvant et solubilité

In Vitro:

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.

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

2.1438 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

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.

Calculateur de molarité

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 (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.

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.

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

Protocole

Animal Administration^[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) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (278 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)
Instruction de manipulation (2659 KB)

Références

[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]

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	2.1438 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

Keywords

AM-2099

1 Cited Publications

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AM-2099

Membrane Transporter/Ion Channel Compound Library

Neuroprotective Compound Library

Mechanoreceptors Compound Library

Targeted Diversity Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AM-2099

Voir tous les produits spécifiques à Isoform Sodium Channel

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

AM-2099

Membrane Transporter/Ion Channel Compound Library

Neuroprotective Compound Library

Mechanoreceptors Compound Library

Targeted Diversity Library

Sodium Channel Blocker Library

Heterocyclic Compound Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Highly Selective Inhibitors Library

Ion Channel Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) AM-2099

Voir tous les produits spécifiques à Isoform Sodium Channel

Activité biologique

Chemical Information

Publications (1)

Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

AM-2099 Related Classifications

HY-100727 Related Classifications