Share to

Details

Safety

Technical Documents

Articles

reviews

Consult

returns

Product details

名称

AM-2099

分子类型

小分子

英文名称

AM-2099

货号

A656863-1ml

包装规格

1ml

浓度

10mM in DMSO

储存温度

-80℃储存

运输条件

超低温冰袋运输

产品介绍

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)

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。

CAS号

1443373-17-8(DMSO)

分子式

C19H13F3N4O3S2

分子量

466.46 g/mol

Smiles

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

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

user reviews

Consultation

Warm reminder：

Because the manufacturer may temporarily adjust product specifications, prices, inventory, parameters and other information without notice, and there are differences in each user's consultation time and procurement needs, the platform reply content is only of reference value within a certain period. Sorry for the inconvenience caused to you, and thank you for your understanding and support! Please consult the online customer service for the latest details. Everything is subject to the real-time reply of the customer service.！

After Sales Services

Please check the quantity, appearance and product information in time when you receive the goods. In case of damage, wrong delivery, abnormal quality and other problems, please feel free to contact us.

Service Hotline:400-6226-992 ，We will handle it for you as soon as possible, thank you for your support and trust.！