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ASB 14780

Names

[ CAS No. ]:
1069046-00-9

[ Name ]:
ASB 14780

[Synonym ]:
ASB14780
3-[1-(4-Phenoxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoic acid, 2-amino-2-(hydroxymethyl)-1,3-propanediol
3-(3-Phenethyl-1-(4-phenoxyphenyl)-1H-indol-5-yl)propanoic acid, 2-amino-2-(hydroxymethyl)-1,3-propanediol
3-[1-(4-Phenoxyphenyl)-3-(2-phenylethyl)-1H-indol-5-yl]propanoic acid - 2-amino-2-(hydroxymethyl)-1,3-propanediol (1:1)
1H-Indole-5-propanoic acid, 1-(4-phenoxyphenyl)-3-(2-phenylethyl)-, compd. with 2-amino-2-(hydroxymethyl)-1,3-propanediol (1:1)

Biological Activity

[Description]:

ASB 14780 (ASB14780, ASB-14780) is a potent, selective and orally active cytosolic phospholipase A2α (cPLA2α) inhibitor with IC50 of 20 nM; displays excellen selectivity over other known secreted phospholipase A2s (sPLA2s), such as sPLA2-IA, sPLA2-IIA, sPLA2-III, and sPLA2-IB; 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.

[References]

References 1. Tomoo T, et al. J Med Chem. 2014 Sep 11;57(17):7244-62. 2. Kanai S, et al. J Pharmacol Exp Ther. 2016 Mar;356(3):604-14. View Related Products by Target Phospholipase

Chemical & Physical Properties

[ Molecular Formula ]:
C31H27NO3·C4H11NO3

[ Molecular Weight ]:
582.686

[ Exact Mass ]:
582.273010

Related Compounds