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AM-2099
😃Good
Catalog No. T14201Cas No. 1443373-17-8
Alias AM2099
AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.
AM-2099
😃Good
Catalog No. T14201Alias AM2099Cas No. 1443373-17-8
AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 2 mg | $278 | 5 days | |
| 5 mg | $409 | In Stock |
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Product Introduction
Bioactivity
Chemical Properties
| Description | AM-2099 is a selective voltage-gated sodium channel Nav1.7 inhibitor used in pain research. |
| Targets&IC50 | Nav1.7 (mouse):0.18 μM, Nav1.7 (rat):3.5 μM, Nav1.7 (human):0.16 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] |
| Alias | 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 & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 120 mg/mL (257.26 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
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