产品说明书

AM966

Print
Chemical Structure| 1228690-19-4 同义名 : -
CAS号 : 1228690-19-4
货号 : A234317
分子式 : C27H23ClN2O5
纯度 : 99%+
分子量 : 490.935
MDL号 : MFCD20486575
存储条件：

粉末 Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 105 mg/mL(213.88 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 AM966 is a potent, selective, orally bioavailable antagonist of the LPA1 receptor. It effectively inhibits LPA1-mediated chemotaxis in various cell types, including human A2058 melanoma cells (IC50=138±43 nM), IMR-90 human lung fibroblasts (IC50=182±86 nM), and CHO mLPA1 cells (IC50=469±54 nM) [1]. LPA-induced activation of ERK1/2 is entirely suppressed by AM966 (100 nM), which exhibits selective antagonism against LPA1 receptor over LPA2-5, with an IC50 value of 3.8±0.4 nM. Pretreatment with AM966 (100 nM) completely abolishes ERK1/2 phosphorylation induced by Mianserin [2].
作用机制 AM966 can antagonize LPA1 receptors and inhibit LPA-stimulated intracellular calcium release.[1]
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.04mL

0.41mL

0.20mL

10.18mL

2.04mL

1.02mL

20.37mL

4.07mL

2.04mL
参考文献

[1]Swaney, JS, et al. A novel, orally active LPA1 receptor antagonist inhibits lung fibrosis in the mouse bleomycin model. Br J Pharmacol. 2010 Aug;160(7):1699-713.

[2]Olianas MC, et al. Antidepressants activate the lysophosphatidic acid receptor LPA(1) to induce insulin-like growth factor-I receptor transactivation, stimulation of ERK1/2 signaling and cell proliferation in CHO-K1 fibroblasts. Biochem Pharmacol. 2015 Jun 15;95(4):311-23.