PF-8380是一种有效的自分泌运动因子（ATX）抑制剂（IC 50 2.8 nM/101 nM纯化酶/全血）。ATX的过度活性与许多炎性病症、癌症和其它疾病相关。ATX产生的溶血磷脂酸（LPA）通过G蛋白偶联受体LPA 1 -4刺激细胞增殖。PF-8380具有口服生物利用度，可在体内有效抑制ATX，降低大鼠关节炎模型中血清和炎症部位的LPA水平。参考文献由Bioz提供动力参见BiozGierse J.等人（2010）“A Novel Autotaxin Inhibitor Reduces Lysophosphatidic Acid Levels in Plasma and the Site of Inflammation”Journal of Pharmacology and Experimental Therapeutics 334（1）：310的更多细节。
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PF-8380 is a potent autotaxin (ATX) inhibitor (IC50 2.8 nM/101 nM purified enzyme/whole blood). Excessive activity of ATX is associated with numerous inflammatory conditions cancers and other disease. Lysophosphatidic acid (LPA) produced by ATX stimulates cell proliferation through G-protein coupled receptorsLPA1-4. PF-8380 is orally bioavailable and effectively inhibits ATX in vivo reducing LPA levels in serum and at the site of inflammation in a rat arthritis model. Can delivered orally with the "Oral Formulation Vehicle".References Powered by Bioz See more details on BiozGierse J. et al (2010) "A Novel Autotaxin Inhibitor Reduces Lysophosphatidic Acid Levels in Plasma and the Site of Inflammation"> Journal of Pharmacology and Experimental Therapeutics 334(1):310.
