PF-8380是一種有效的自分泌運動因子(ATX)抑制劑(IC 50 2.8 nM/101 nM純化酶/全血)。ATX的過度活性與許多炎性病癥、癌癥和其它疾病相關。ATX產生的溶血磷脂酸(LPA)通過G蛋白偶聯受體LPA 1 -4刺激細胞增殖。PF-8380具有口服生物利用度,可在體內有效抑制ATX,降低大鼠關節(jié)炎模型中血清和炎癥部位的LPA水平。參考文獻由Bioz提供動力參見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的更多細節(jié)。
產品描述
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.