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ASB14780
- Parent CAS: 1069044-40-1
- Soluble in DMSO
- MF: C31H27NO3.C4H11NO3
- MW: 582.69
Description
ASB14780 is a highly potent, orally active inhibitor of cytosolic phospholipase A2α (cPLA2α) . It displays an IC50 value of 20 nM in vitro and ranges from 0.54 to 0.64 µM in guinea pig and human whole blood assays.
ASB14780 fights inflammation in ear edema and asthma models. It also shows strong potential against nonalcoholic fatty liver diseases by blocking fatty liver progression and hepatic fibrosis. It works by markedly reducing liver (alpha )-SMA protein expression alongside collagen 1a2, α-SMA, and TGFβ1 mRNA levels, while simultaneously suppressing monocyte and macrophage inflammatory markers.
cPLA2α pharmacology is highly relevant to asthma and progressive fibrosis research; ASB14780 serves as a valuable tool that supports mechanistic studies of cPLA2α pathways in biochemical, cellular, and hepatic fibrosis disease-model assays.
Key Features
- Orally active cPLA2α inhibitor with high potency (IC50 20 nM)
- Specifically targets cPLA2α and shows no inhibition toward sPLA2
- Modulates cPLA2α-dependent signaling or biological activity
- Suppresses human and guinea pig blood inflammation
Applications
- cPLA2α pharmacology and target-validation studies
- cPLA2α pathway and signaling assays
- Disease-model research related to asthma, fibrosis
- Metabolic pathway and biomarker-response studies
Note: ASB14780 was sold as the tromethamine (THAM) salt, as it was used in the original publication.
More Information
| Parent CAS No. | 1069044-40-1 |
|---|---|
| Chemical Name | 3-(3-Phenethyl-1-(4-phenoxyphenyl)-1H-indol-5-yl)propanoic acid tris salt |
| SMILES | N1(C2=CC=C(OC3=CC=CC=C3)C=C2)C2=C(C=C(CCC(O)=O)C=C2)C(CCC2=CC=CC=C2)=C1.C(O)C(N)(CO)CO |
| MFCD | N.A. |
| InChi | InChI=1S/C31H27NO3.C4H11NO3/c33-31(34)20-13-24-12-19-30-29(21-24)25(14-11-23-7-3-1-4-8-23)22-32(30)26-15-17-28(18-16-26)35-27-9-5-2-6-10-27;5-4(1-6,2-7)3-8/h1-10,12,15-19,21-22H,11,13-14,20H2,(H,33,34);6-8H,1-3,5H2 |
| InChiKey | MBPXGBINIINSEU-UHFFFAOYSA-N |
| CID | 68519061 |
| Short Description | cPLA2α inhibitor |
References
- T Tomoo et al. Design, synthesis, and biological evaluation of 3-(1-Aryl-1H-indol-5-yl)propanoic acids as new indole-based cytosolic phospholipase A2α inhibitors. J Med Chem. 2014 Sep 11;57(17):7244-62.
- S Kanai et al. ASB14780, an Orally Active Inhibitor of Group IVA Phospholipase A2, Is a Pharmacotherapeutic Candidate for Nonalcoholic Fatty Liver Disease. J Pharmacol Exp Ther. 2016 Mar;356(3):604-14.
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