For research use only. Not for therapeutic Use.
ONO-7300243（Cat No.:I004409） is a novel and potent lysophosphatidic acid receptor 1 (LPA1) antagonist with IC50 of 0.16 μM. ONO-7300243 exhibits almost identical levels of antagonist activity in vitro.
| Catalog Number | I004409 |
| CAS Number | 638132-34-0 |
| Synonyms | 2-(4-((3,5-dimethoxy-4-methyl-N-(3-phenylpropyl)benzamido)methyl)phenyl)acetic acid |
| Molecular Formula | C28H31NO5 |
| Purity | ≥95% |
| Target | LPL Receptor |
| Solubility | 10 mM in DMSO |
| Storage | Store at -20°C |
| IUPAC Name | 2-[4-[[(3,5-dimethoxy-4-methylbenzoyl)-(3-phenylpropyl)amino]methyl]phenyl]acetic acid |
| InChI | InChI=1S/C28H31NO5/c1-20-25(33-2)17-24(18-26(20)34-3)28(32)29(15-7-10-21-8-5-4-6-9-21)19-23-13-11-22(12-14-23)16-27(30)31/h4-6,8-9,11-14,17-18H,7,10,15-16,19H2,1-3H3,(H,30,31) |
| InChIKey | WGABOZPQOOZAOI-UHFFFAOYSA-N |
| SMILES | CC1=C(C=C(C=C1OC)C(=O)N(CCCC2=CC=CC=C2)CC3=CC=C(C=C3)CC(=O)O)OC |
| Reference | 1:ACS Med Chem Lett. 2016 Aug 19;7(10):913-918. eCollection 2016 Oct 13. Discovery of ONO-7300243 from a Novel Class of Lysophosphatidic Acid Receptor 1 Antagonists: From Hit to Lead.Terakado M,Suzuki H,Hashimura K,Tanaka M,Ueda H,Kohno H,Fujimoto T,Saga H,Nakade S,Habashita H,Takaoka Y,Seko T, PMID: 27774128 PMCID: PMC5066152 [Available on 2017-10-13] DOI: 10.1021/acsmedchemlett.6b00225 </br><span>Abstract:</span> Lysophosphatidic acid (LPA) evokes various physiological responses through a series of G protein-coupled receptors known as LPA1-6. A high throughput screen against LPA1 gave compound 7a as a hit. The subsequent optimization of 7a led to ONO-7300243 (17a) as a novel, potent LPA1 antagonist, which showed good efficacy in vivo. The oral dosing of 17a at 30 mg/kg led to reduced intraurethral pressure in rats. Notably, this compound was equal in potency to the α1 adrenoceptor antagonist tamsulosin, which is used in clinical practice to treat dysuria with benign prostatic hyperplasia (BPH). In contrast to tamsulosin, compound 17a had no impact on the mean blood pressure at this dose. These results suggest that LPA1 antagonists could be used to treat BPH without affecting the blood pressure. Herein, we report the hit-to-lead optimization of a unique series of LPA1 antagonists and their in vivo efficacy. |
