ASB14780 (ASB-14780) is a potent, selective and orally active cytosolic phospholipase A2α (cPLA2α) inhibitor with IC50 of 20 nM.
ASB 14780 displays excellen selectivity over other known secreted phospholipase A2s (sPLA2s), such as sPLA2-IA, sPLA2-IIA, sPLA2-III, and sPLA2-IB.
ASB 14780 markedly ameliorates liver injury and hepatic fibrosis, attenuates the CCl4-induced expression of α-SMA protein and the mRNA expression of collagen 1a2, α-SMA, and TGF-β1 in the liver, and inhibits the expression of monocyte/macrophage markers, CD11b and MCP-1 in vivo, while preventing the recruitment of monocytes/macrophages to the liver.
Physicochemical Properties
M.Wt
582.69
Formula
C31H27NO3 · C4H11NO3
Appearance
Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility
10 mM in DMSO
Chemical Name/SMILES
3-[1-(4-phenoxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoic acid 2-amino-2-(hydroxymethyl)propane-1,3-diol salt
References
1. Tomoo T, et al. J Med Chem. 2014 Sep 11;57(17):7244-62.
