PAT-048 是一种有效、选择性、可口服的自分泌运动因子 autotaxin 抑制剂，抑制 IL-6 mRNA 的表达，但在肺部纤维化模型中，对 autotaxin 蛋白水平和溶血磷脂酸 (LPA) 的产生无明显作用。在小鼠血浆中对 autotaxin 的 IC50 和 IC90 值分别为 20 nM 和 200 nM。在体内实验中，PAT-048 可降低皮肤纤维化。
CAS：1359983-15-5
分子式：C22H18ClF2N3O2S
分子量：461.91
纯度：98%
存储：Store at -20°C

Background:

PAT-048 is a potent, selective and orally active autotaxin inhibitor, inhibits IL-6 mRNA expression, but shows no effect on autotaxin protein and pulmonary lysophosphatidic acid (LPA) production in lung fibrosis model. PAT-048 shows an IC50 and IC90 of 20 nM and 200 nM for autotaxin in mouse plasma. PAT-048 reduces dermal fibrosis in vivo[1][2]. IC50: 20 nM (Autotaxin, in mouse plasma)[1] IC90: 200 nM (Autotaxin, in mouse plasma)[1]

[1]. Castelino FV, et al. An Autotaxin/Lysophosphatidic Acid/Interleukin-6 Amplification Loop Drives Scleroderma Fibrosis. Arthritis Rheumatol. 2016 Dec;68(12):2964-2974. [2]. Black KE, et al. Autotaxin activity increases locally following lung injury, but is not required for pulmonary lysophosphatidic acid production or fibrosis. FASEB J. 2016 Jun;30(6):2435-50.