ONO-0300302 |
カタログ番号GC65579 |
ONO-0300302 は、0.086 μM の IC50 を持つ、経口活性のある強力な LPA1 (リゾホスファチジン酸受容体 1) アンタゴニストです。
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Cas No.: 856689-51-5
Sample solution is provided at 25 µL, 10mM.
ONO-0300302 is an orally active and potent LPA1 (lysophosphatidic acid receptor 1) antagonist, with an IC50 of 0.086 μM. ONO-0300302 is a slow tight binding inhibitor, and its binding affinity increases with time, with Kd of 0.34 nM (37 °C, 2 h). ONO-0300302 can be used for benign prostatic hyperplasia (BPH) research[1].
ONO-0300302 shows moderate stability against rat microsomes[1].
ONO-0300302 inhibits significantly an LPA (lysophosphatidic acid receptor)-induced increase of intraurethral pressure (IUP) in rat (3 mg/kg, p.o.) and dog (1 mg/kg, p.o.) over 12 h[1].
[1]. Terakado M, et al. Discovery of a Slow Tight Binding LPA1 Antagonist (ONO-0300302) for the Treatment of Benign Prostatic Hyperplasia. ACS Med Chem Lett. 2017 Nov 20;8(12):1281-1286.
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