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AM-2099

CAS No. : 1443373-17-8

MCE 站：AM-2099

产品活性：AM-2099是电压门控钠通道Nav1.7的有效，选择性的抑制剂，对人类Nav1.7的IC₅₀值为0.16 μM。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Sodium Channel

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 ?M) and does not show greater than 50% inhibition against a panel of 100 kinases (1 ?M) and a broad CEREP panel (10 ?M). .

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.

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