计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
为什么选择此级别
，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
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)
规格
规格或纯度
10mM in DMSO
英文名称
AM-2099
生化机理
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。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
COC1=C(C=CC(=C1)C(F)(F)F)C2=NC=NC3=C2C=CC(=C3)S(=O)(=O)NC4=NC=CS4
PubChem CID
分子量
466.46
技术文档
高级数据
关联靶点（人）
SCN2A
Tclin
钠通道蛋白 2 型亚基 α(Sodium channel protein type 2 subunit alpha)
(1 活性数据)
SCN9A
Tclin
钠通道蛋白 9 型亚基 α(Sodium channel protein type 9 subunit alpha)
(7 活性数据)
SCN1A
Tclin
钠通道蛋白 1 型亚基 α(Sodium channel protein type 1 subunit alpha)
(1 活性数据)
SCN8A
Tclin
钠通道蛋白 8 型亚基 α(Sodium channel protein type 8 subunit alpha)
(1 活性数据)
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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溶液计算器
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