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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References |
1. Deliyanti D, Zhang Y, Khong F, Berka DR, Stapleton DI, Kelly DJ, Wilkinson-Berka JL. (2015)
FT011, a Novel Cardiorenal Protective Drug, Reduces Inflammation, Gliosis and Vascular Injury in Rats with Diabetic Retinopathy. PLoS One, 10 (7): e0134392. [PMID:26222724] |
2. Gilbert RE, Zhang Y, Williams SJ, Zammit SC, Stapleton DI, Cox AJ, Krum H, Langham R, Kelly DJ. (2012)
A purpose-synthesised anti-fibrotic agent attenuates experimental kidney diseases in the rat. PLoS One, 7 (10): e47160. [PMID:23071743] |
3. Lau X, Zhang Y, Kelly DJ, Stapleton DI. (2013)
Attenuation of Armanni-Ebstein lesions in a rat model of diabetes by a new anti-fibrotic, anti-inflammatory agent, FT011. Diabetologia, 56 (3): 675-9. [PMID:23242170] |
4. Miller T, Papaioannou N. (2019)
Anti-fibrotic compounds. Patent number: WO2018144620A9. Assignee: Shire Human Genetic Therapies, Inc.. Priority date: 31/01/2018. Publication date: 24/01/2019. |
5. Zammit SC, Cox AJ, Gow RM, Zhang Y, Gilbert RE, Krum H, Kelly DJ, Williams SJ. (2009)
Evaluation and optimization of antifibrotic activity of cinnamoyl anthranilates. Bioorg Med Chem Lett, 19 (24): 7003-6. [PMID:19879136] |
6. Zhang Y, Edgley AJ, Cox AJ, Powell AK, Wang B, Kompa AR, Stapleton DI, Zammit SC, Williams SJ, Krum H et al.. (2012)
FT011, a new anti-fibrotic drug, attenuates fibrosis and chronic heart failure in experimental diabetic cardiomyopathy. Eur J Heart Fail, 14 (5): 549-62. [PMID:22417655] |