ONO-0300302 是一种口服有效的 LPA1 (溶血磷脂酸受体 1) 拮抗剂，其 IC50 为0.086 μM。ONO-0300302 是一种缓慢的紧密结合抑制剂，其结合亲和力随时间增加，其 Kd 为0.34 nM (37°C, 2 h)。ONO-0300302 可用于良性前列腺增生 (BPH) 的研究。
货号:ajcx39856
CAS:856689-51-5
分子式:C29H35NO5
分子量：477.59
溶解度:DMSO : 220 mg/mL (460.65 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.