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CAS No.: 1228690-19-4

AM966 Catalog No. CSN13766

Synonyms: AM966

AM966 is a high affinity, selective, oral LPA1 (lysophosphatidic acid receptor, IC50=17 nM) antagonist, with selectivity for this receptor over the other LPA receptors.

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400-920-2911

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 LPA Receptor

IC50:17nM
描述LPA (lysophosphatidic acid), which has been shown to be involved in certain diseases such as atherosclerosis and cancer, can act through its receptor like LPA receptor 1, LPA receptor 2, or LPA receptor 3 and elicit different biological actions, like Ca²⁺ mobilization, changing in cAMP accumulation, changing cell shape and motility, and cell proliferation. AM966 is a potent antagonist of LPA1 receptors, with selectivity for this receptor over the other LPA receptors (LPA2-5 receptors). AM966 is usually used in the study of lung. AM966 can inhibit LPA-stimulated intracellular calcium release from Chinese hamster ovary cells stably expressing human LPA1 receptors with IC50 value of 17nM, as well as inhibited LPA-induced chemotaxis of human IMR-90 lung fibroblasts expressing LPA1 receptors, human A2058 melanoma cells and CHO mLPA1 cells with IC50 values of 181nM, 138nM and 469nM, respectively. Oral administration of 30mg/kg AM966, BID, for 3 days could reduce vascular leakage, inflammation and lung injury and inflammation in a 3-day-bleomycin-induced model. Also it inhibited lung fibrosis and maintains body weight in a model of bleomycin-induced lung injury for 14 days, and increase the survival in a most of bleomycin-induced lung fibrosis for 21–28 days. AM966 at concentration of 1μM could induce lung endothelial barrier dysfunction in HLMVECs, due to its induction of phosphorylation of MLC through activation of RhoA/Rho kinase pathway and phosphorylation of VE-cadherin, activation of which are mediated by LPA1.
作用机制AM966 can antagonize LPA1 receptors and inhibit LPA-stimulated intracellular calcium release.^[1]
动物研究
剂量
Mice: 30 mg/kg^[3] (i.p.); 10 mg/kg, 30 mg/kg^[1] (p.o.)

给药途径
i.p., p.o.
参考文献

动物研究
剂量	Mice: 30 mg/kg^[3] (i.p.); 10 mg/kg, 30 mg/kg^[1] (p.o.)
给药途径	i.p., p.o.

[1] Swaney JS, Chapman C, et al. A novel, orally active LPA(1) receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. Br J Pharmacol. 2010 Aug;160(7):1699-713.
[2] Cai J, Wei J, et al. AM966, an Antagonist of Lysophosphatidic Acid Receptor 1, Increases Lung Microvascular Endothelial Permeability through Activation of Rho Signaling Pathway and Phosphorylation of VE-Cadherin. Mediators Inflamm. 2017;2017:6893560.
[3] Radiation Inducing Pulmonary Cellular Senescence through the LPA-LPA1-Akt Pathway

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.0369 mL
- 10.1846 mL
- 20.3693 mL
- 5 mM
- 0.4074 mL
- 2.0369 mL
- 4.0739 mL
- 10 mM
- 0.2037 mL
- 1.0185 mL
- 2.0369 mL

技术信息

CAS号

1228690-19-4

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C27H23ClN2O5

运输

蓝冰

分子量

490.93

别名

AM966

溶解度

DMSO	95.0 mg/mL (193.5 mM) warming

动物实验配方

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