AM-2099

小分子

AM-2099

A656863-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC 50 of 0.16 μM for human Nav1.7. 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 µM) and does not show greater than 50% inhibition against a panel of 100 kinases (1 µM) and a broad CEREP panel (10 µM).. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. IC50& Target:IC50: 0.16 μM (human Nav1.7), 0.18 μM (mouse Nav1.7), 3.5 μM (rat Nav1.7)

AM-2099 是一种强效的电压门控钠通道 Nav1.7 选择性抑制剂，对人类 Nav1.7 的 IC 50 为 0.16 μM。

1443373-17-8(DMSO)

C19H13F3N4O3S2

466.46 g/mol

COC1=C(C=CC(=C1)C(F)(F)F)C2=NC=NC3=C2C=CC(=C3)S(=O)(=O)NC4=NC=CS4