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AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.

| Pack Size | Price | USA Warehouse | Global Warehouse | Quantity |
|---|---|---|---|---|
| 5 mg | $299 | 5 days | 5 days |
| Description | AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research. |
| Targets&IC50 | Nav1.7 (rat):3.5 μM, Nav1.7 (human):0.16 μM, Nav1.7 (mouse):0.18 μM |
| In vitro | 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). In heterologous cells, comparable inhibition is observed across human, mouse, dog, and cynomolgus monkey NaV1.7 with reduced activity against rat NaV1.7.[1] |
| In vivo | 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. 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. However, when dosed in dogs AM-2099 shows very low clearance, a low Vdss and long halflife (18 h).[1] |
| Synonyms | AM2099 |
| Molecular Weight | 466.46 |
| Formula | C19H13F3N4O3S2 |
| Cas No. | 1443373-17-8 |
| Smiles | O=S(=O)(NC1=NC=CS1)C=2C=CC=3C(=NC=NC3C=4C=CC(=CC4OC)C(F)(F)F)C2 |
| Relative Density. | 1.531 g/cm3 (Predicted) |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 120 mg/mL (257.26 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
| In Vivo Formulation | 10% DMSO+40% PEG300+5% Tween-80+45% Saline: 3.3 mg/mL (7.07 mM), Sonication is recommended. Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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Dissolve 2 mg of the compound in 100 μL DMSO
to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
1) Add 100 μL of the DMSO
stock solution to 400 μL PEG300
and mix thoroughly until the solution becomes clear.
2) Add 50 μL Tween 80 and mix well until fully clarified.
3) Add 450 μL Saline,PBS or ddH2O
and mix thoroughly until a homogeneous solution is obtained.
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