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AM-2099

Catalog No. T14201 CAS 1443373-17-8

AM-2099 is a voltage-gated sodium channel Nav1.7 inhibitor (IC50: 0.16 μM).

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AM-2099, CAS 1443373-17-8

Pack Size	Availability	Price/USD	Quantity
2 mg	5 days	$ 56.00
5 mg	5 days	$ 89.00

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Biological Description

Chemical Properties

Storage & Solubility Information

Description	AM-2099 is a voltage-gated sodium channel Nav1.7 inhibitor (IC50: 0.16 μM).
Targets&IC50	Nav1.7 (human):0.16 μM, Nav1.7 (mouse):0.18 μM, Nav1.7 (rat):3.5 μM
In vitro	AM-2099 exhibits over 100-fold selectivity for the Nav1.7 channel compared to Nav1.3, Nav1.4, Nav1.5, and Nav1.8, with diminished selectivity observed for Nav1.1, Nav1.2, and Nav1.6. Its affinity for the hERG channel is low (>30 μM), and it lacks significant inhibition (>50%) against both a 100-kinase panel (1 μM) and a broad CEREP panel (10 μM)[1]. In heterologous cells, AM-2099 consistently inhibits NaV1.7 in human, mouse, dog, and cynomolgus monkey, showing decreased efficacy against rat NaV1.7.
In vivo	AM-2099 exhibits a dose-dependent escalation in plasma exposure accompanied by a simultaneous dose-dependent decrease in scratching bouts in comparison to vehicle-treated animals, notably achieving statistical significance at the 60 mg/kg dosage[1]. It also presents a favorable pharmacokinetic profile in both rats and dogs. In rats, AM-2099 is characterized by low total clearance, moderate volume of distribution at steady state (Vdss), and half-life. Conversely, in dogs, it features very low clearance, a low Vdss, and an extended half-life (18 h).

Molecular Weight	466.46
Formula	C19H13F3N4O3S2
CAS No.	1443373-17-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 150 mg/mL (321.57 mM)

References and Literature

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.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

AM-2099 1443373-17-8 Others AM2099 AM 2099 inhibitor inhibit

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