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AM095 free acid

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Chemical Structure| 1228690-36-5 同义名 : AM095
CAS号 : 1228690-36-5
货号 : A697231
分子式 : C27H24N2O5
纯度 : 98%
分子量 : 456.49
MDL号 : MFCD22665734
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 65 mg/mL(142.39 mM),配合低频超声,并水浴加热至45℃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 AM095 suppresses the LPA-triggered calcium movement in CHO cells that are genetically modified to express either human or mouse LPA1. The IC50 values for the suppression of LPA-evoked calcium movement by AM095 in CHO cells expressing human or mouse LPA1 are 0.025 μM and 0.023 μM, respectively[1]. AM095 diminishes the LPA-induced vasorelaxation by approximately 90% at a concentration of 10 μM compared to the control treated with a vehicle[2]. AM095 hinders the LPA-driven chemotaxis of CHO cells that overexpress mouse LPA1 (IC50=778 nM) and human A2058 melanoma cells (IC50=233 nM)[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.19mL

0.44mL

0.22mL

10.95mL

2.19mL

1.10mL

21.91mL

4.38mL

2.19mL

参考文献

[1]Castelino FV, et al. Amelioration of dermal fibrosis by genetic deletion or pharmacologic antagonism of lysophosphatidic acid receptor 1 in a mouse model of scleroderma. Arthritis Rheum. 2011 May;63(5):1405-15

[2]Ruisanchez E, et al. Lysophosphatidic acid induces vasodilation mediated by LPA1 receptors, phospholipase C, and endothelial nitric oxide synthase. FASEB J. 2014 Feb;28(2):880-90

[3]Swaney, J. S., et al. Pharmacokinetic and pharmacodynamic characterization of an oral lysophosphatidic acid type 1 receptor-selective antagonist. Journal of Pharmacology and Experimental Therapeutics (2011), 336(3), 693-700.