Cas No.: | 590416-75-4 |
Chemical Name: | 3-(3-amino-4-((2,3-dihydro-1H-inden-2-yl)oxy)-5-(1-methyl-1H-indazol-5-yl)phenyl)propanoic acid |
Formula: | C26H25N3O3 |
M.Wt: | 427.504 |
Purity: | >98% |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | AK106-001616 (AK 106-001616) is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2) with IC50 of 3.8 nM (human cPLA2 enzyme); also inhibited rat cPLA2 with IC50 of 4.3 nM, shows no significant activity against human iPLA2, bovine sPLA2 IB and PAF-AH (>10,000 fold selectivity); suppressed the release of AA from Ca2+ ionophore A23187-stimulated rat RBL-2H3 cells (IC50=5.5 nM), also suppressed the production of PGE2 by LPS-stimulated human PBMCs (IC50=5.1 nM) and the production of LTB4 by Ca2+ ionophore A23187-stimulated RBL-2H3 cells (IC50=2.6 nM); demonstrates in vivo efficacy for inflammation, neuropathic pain, and pulmonary fibrosis.Rheumatoid ArthritisPhase 2 Clinical |