| Bioactivity | 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]. |
| Invitro | ONO-0300302 shows moderate stability against rat microsomes[1]. |
| 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[1]. |
| Name | ONO-0300302 |
| CAS | 856689-51-5 |
| Formula | C29H35NO5 |
| Molar Mass | 477.59 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | -20°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| Reference | [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. |