AM-2099
Based on 1 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: 98.37%
- CAS No.: 1443373-17-8
- Formula: C19H13F3N4O3S2
- Molecular Weight:466.46
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) AM-2099
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Biological Activity
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Nav1.7 |
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Cell Line
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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
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[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
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[PMID: 27994738] |
| CHO | IC50 |
21 μM
Compound: 16
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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
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[PMID: 27994738] |
| HEK293 | IC50 |
>30 μM
Compound: 1
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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
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[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
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[PMID: 27994738] |
| HEK293 | IC50 |
>30 μM
Compound: 16
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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
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[PMID: 27994738] |
| HEK293 | IC50 |
0.009 μM
Compound: 16
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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
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[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
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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
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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
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[PMID: 27994738] |
| HEK293 | IC50 |
0.18 μM
Compound: 16
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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
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[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
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[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
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[PMID: 27994738] |
| HEK293 | IC50 |
3.7 μM
Compound: 16
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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
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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
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[PMID: 27994738] |
| HEK-293T | IC50 |
0.16 μM
Compound: 16
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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 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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1443373-17-8
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Appearance Solid
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Molecular Weight 466.46
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Formula C19H13F3N4O3S2
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Color White to light yellow
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SMILES
COC1=CC(C(F)(F)F)=CC=C1C2=NC=NC3=CC(S(=O)(NC4=NC=CS4)=O)=CC=C32
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
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
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Most Recent
Solvent & Solubility
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.
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 (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.
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.
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.
Protocol
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.
Purity & Documentation
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Data Sheet (278 KB)
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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)
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Handling Instructions (2659 KB)
References
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 | 2.1438 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 |
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