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Product details

名称

AM-2099

分子类型

小分子

英文名称

AM-2099

货号

A651904-5mg

包装规格

5mg

浓度

≥98%

储存温度

-20°C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. Form:Solid 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

分子式

C19H13F3N4O3S2

分子量

466.46 g/mol

PubChem编号

86687532

Isomeric SMILES

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

IIUPAC Name

4-[2-methoxy-4-(trifluoromethyl)phenyl]-N-(1,3-thiazol-2-yl)quinazoline-7-sulfonamide

INCHI

1S/C19H13F3N4O3S2/c1-29-16-8-11(19(20,21)22)2-4-14(16)17-13-5-3-12(9-15(13)24-10-25-17)31(27,28)26-18-23-6-7-30-18/h2-10H,1H3,(H,23,26)

InChi Key

VSUDRCZPHWUXEW-UHFFFAOYSA-N

Smiles

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

PubChem CID

86687532

溶解性

DMSO : ≥ 150 mg/mL (321.57 mM)

氢键供体数Hydrogen Bond Donor Count

氢键受体数Hydrogen Bond Acceptor Count

可旋转键计数Rotatable Bond Count

精确质量Exact Mass

466.038 Da

单同位素质量Monoisotopic Mass

466.038 Da

拓扑极表面积Topological Polar Surface Area

131.000 Å²

重原子数Heavy Atom Count

形式电荷Formal Charge

复杂度Complexity

721

同位素原子数Isotope Atom Count

共价键合单元计数Covalently-Bonded Unit Count

XLogP3

3.9

Safety

「No Dangerous Attributes」

「No upstream and downstream information yet」

Technical Documents

「No technical documents」

Articles

「No related articles yet」

user reviews

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