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AM095 free acid {[allProObj[0].p_purity_real_show]}

货号:A697231 同义名: AM095 Ambeed 开学季,买赠积分,赢豪礼

AM095 free acid is a potent LPA1 receptor antagonist with IC50 values of 0.98 and 0.73 μM for recombinant human or mouse LPA1 respectively.

AM095 free acid 化学结构 CAS号:1228690-36-5
AM095 free acid 化学结构
CAS号:1228690-36-5
AM095 free acid 3D分子结构
CAS号:1228690-36-5
AM095 free acid 化学结构 CAS号:1228690-36-5
AM095 free acid 3D分子结构 CAS号:1228690-36-5
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AM095 free acid 纯度/质量文件 产品仅供科研

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AM095 free acid 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].
体内研究

AM095 exhibits notable oral bioavailability and a moderate half-life, showing tolerability in rats and dogs following oral and intravenous administration. AM095 progressively inhibits the LPA-induced release of histamine. It also reduces the bleomycin-triggered rise in collagen, protein, and the infiltration of inflammatory cells in bronchoalveolar lavage fluid. Additionally, AM095 lessens kidney fibrosis in a model of unilateral ureteral obstruction in mice[3].

体外研究

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].

AM095 free acid 动物研究

Dose Rat: 2 mg/kg[1] (i.v.); 10 mg/kg[1] (p.o.) Mice: 10 mg/kg, 30 mg/kg[2] (p.o.)
Administration i.v., p.o.

AM095 free acid 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.

AM095 free acid 实验方案

计算器
存储液制备 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

AM095 free acid 技术信息

CAS号1228690-36-5
分子式C27H24N2O5
分子量 456.49
别名 AM095
运输蓝冰
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
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