AK106-001616( AK 106-001616 )

Catalog No. M15184 CAS No. 590416-75-4

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HNMR

HPLC

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Product Name

AK106-001616
Note

Research use only, not for human use.
Brief 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).
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 Arthritis Phase 2 Clinical.
In Vitro

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In Vivo

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Synonyms

AK 106-001616
Pathway

Metabolic Enzyme/Protease
Target

Phospholipase
Recptor

Phospholipase
Research Area

Inflammation/Immunology
Indication

Rheumatoid Arthritis

CAS Number

590416-75-4
Formula Weight

427.504
Molecular Formula

C26H25N3O3
Purity

>98% (HPLC)
Solubility

——
SMILES

Cn1ncc2cc(ccc12)c3cc(CCC(=O)O)cc(N)c3OC4Cc5ccccc5C4
Chemical Name

3-(3-amino-4-((2,3-dihydro-1H-inden-2-yl)oxy)-5-(1-methyl-1H-indazol-5-yl)phenyl)propanoic acid

1. Shimizu H, et al. J Pharmacol Exp Ther. 2019 Apr 10. pii: jpet.118.255034.

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