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ATX inhibitor 1

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Chemical Structure| 2225892-70-4 同义名 : -
CAS号 : 2225892-70-4
货号 : A1175078
分子式 : C21H23Cl2N2O6P
纯度 : 99%+
分子量 : 501.297
MDL号 : MFCD31813633
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(498.71 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 Autotaxin (ATX) is a key enzyme that converts lysophosphatidylcholine to lysophosphatidic acid (LPA).Inhibition of ATX decreased estrogen and LPA‑induced cell proliferation. High LPA levels markedly elevated the phosphorylation levels of extracellular signal‑regulated kinase (ERK). ATX downregulation moderately decreased estrogen‑ and LPA‑induced phosphorylation of ERK[2]. In pulmonary fibrosis, ATX levels rise in the broncheoalveolar fluid (BALF) and stimulate LPA production. LPA engagement of its receptors activate multiple G-protein mediated signal transduction pathways leading to different responses from pulmonary cells including the production of pro-inflammatory signals from stressed epithelial cells, the modulation of endothelial physiology, the activation of TGF signaling and the stimulation of fibroblast accumulation[3]. Autotaxin (ATX) is a potential target for the treatment of various cancers. ATX inhibitor 1 is a potent ATX inhibitor (IC50: 1.23 nM, FS-3 and 2.18 nM, bis-pNPP)[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.99mL

0.40mL

0.20mL

9.97mL

1.99mL

1.00mL

19.95mL

3.99mL

1.99mL
参考文献

[1]Balupuri A, et al. Discovery and optimization of ATX inhibitors via modeling, synthesis and biological evaluation. Eur J Med Chem. 2018. 148, 397-409.

[2]Guo Zhang,et al. ATX‑LPA axis facilitates estrogen‑induced endometrial cancer cell proliferation via MAPK/ERK signaling pathway. Mol Med Rep. 2018. 17(3), 4245-4252.

[3]Ioanna Ninou,et al. Autotaxin in Pathophysiology and Pulmonary Fibrosis. Front Med (Lausanne). 2018. 5, 180.