ONO-0300302 is an orally active and potent LPA1 (lysophosphatidic acid receptor 1) antagonist, with an IC 50 of 0.086 μM. ONO-0300302 is a slow tight binding inhibitor, and its binding affinity increases with time, with K d of 0.34 nM (37 °C, 2 h). ONO-0300302 can be used for benign prostatic hyperplasia (BPH) research.
性状
Solid
IC50 & Target[1][2]
LPA1 Receptor 0.086 μM (IC50)
体外研究(In Vitro)
ONO-0300302 shows moderate stability against rat microsomes. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
-20°C, protect from light In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
参考文献
[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.
溶解度数据
In Vitro: DMSO : 220 mg/mL (460.65 mM; Need ultrasonic)配制储备液