For research use only. Not for therapeutic Use.
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].
| Catalog Number | I033886 |
| CAS Number | 856689-51-5 |
| Synonyms | 3-[1-[(2S,3S)-2-(2,3-dihydro-1H-inden-2-ylmethyl)-3-(3,5-dimethoxy-4-methylphenyl)-3-hydroxypropyl]pyrrol-3-yl]propanoic acid |
| Molecular Formula | C29H35NO5 |
| Purity | ≥95% |
| InChI | InChI=1S/C29H35NO5/c1-19-26(34-2)15-24(16-27(19)35-3)29(33)25(14-21-12-22-6-4-5-7-23(22)13-21)18-30-11-10-20(17-30)8-9-28(31)32/h4-7,10-11,15-17,21,25,29,33H,8-9,12-14,18H2,1-3H3,(H,31,32)/t25-,29+/m0/s1 |
| InChIKey | USAXUWZJQPBEDO-ABYGYWHVSA-N |
| SMILES | CC1=C(C=C(C=C1OC)C(C(CC2CC3=CC=CC=C3C2)CN4C=CC(=C4)CCC(=O)O)O)OC |
| 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. |
