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Chemical Structure : AK106-001616
Catalog No.: PC-36162Not For Human Use, Lab Use Only.
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).
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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).
AK106-001616 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).
AK106-001616 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).
AK106-001616 demonstrates in vivo efficacy for inflammation, neuropathic pain, and pulmonary fibrosis.
| M.Wt | 427.504 | |
| Formula | C26H25N3O3 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Shimizu H, et al. J Pharmacol Exp Ther. 2019 Apr 10. pii: jpet.118.255034.
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