Synonyms: example 27 [WO2018144620] | FT-011 | FT011 | SHP-627
Compound class:
Synthetic organic
Comment: Asengeprast is the INN for a G protein-coupled receptor 68 (GPR68) antagonist with anti-inflammatory potential. We obtained the chemical structure and proposed mechanism of action from INN proposed list 130 (released Feb. 2024). This structure matched to clinical lead FT001 via PubChem, which has proposed anti-inflammatory and anti-fibrotic actions that may be of benefit across a range of human diseases [1-3,6]. Asengeprast's structure was claimed in patent WO2018144620 in 2019 [4].
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Bioactivity Comments |
Anti-fibrotic activity (determined as inhibition of TGF-β-stimulated production of collagen) has been demonstrated in in vitro cell-based studies [5]. An IC50 of 21.4 μM for inhibition of [14C]proline incorporation into collagen was reported in [4]. Evidence to support antagonist action at GPR68 is not publicly available (March 2024). |