货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S83344-5mg	≥98%	￥880.00 S83344-5mg ￥880.00 3-5天	0 货期：3-5天	-	-	-	-
S83344-10mg	≥98%	￥1480.00 S83344-10mg ￥1480.00 3-5天	0 货期：3-5天	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S83344-5mg

≥98%

￥880.00

货期：3-5天

S83344-10mg

≥98%

￥1480.00

货期：3-5天

产品描述：

AM-2099 is a potent and selective inhibitor of voltage-gated sodium channel Nav1.7 with an IC50 of 0.16 μM for human Nav1.7.

靶点：

IC50: 0.16 μM (human Nav1.7), 0.18 μM (mouse Nav1.7), 3.5 μM (rat Nav1.7);Others

体外研究：

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).

体内研究：

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

参考文献：

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.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.144 ml	10.719 ml	21.438 ml
5 mM	0.429 ml	2.144 ml	4.288 ml
10 mM	0.214 ml	1.072 ml	2.144 ml
50 mM	0.043 ml	0.214 ml	0.429 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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