Recommanded Product: 144291-47-4On October 13, 2016 ,《Discovery of ONO-7300243 from a Novel Class of Lysophosphatidic Acid Receptor 1 Antagonists: From Hit to Lead》 was published in ACS Medicinal Chemistry Letters. The article was written by Terakado, Masahiko; Suzuki, Hidehiro; Hashimura, Kazuya; Tanaka, Motoyuki; Ueda, Hideyuki; Kohno, Hiroshi; Fujimoto, Taku; Saga, Hiroshi; Nakade, Shinji; Habashita, Hiromu; Takaoka, Yoshikazu; Seko, Takuya. The article contains the following contents:
Lysophosphatidic acid (LPA) evokes various physiol. responses through a series of G protein-coupled receptors known as LPA1-6. A high throughput screen against LPA1 gave compound 4′-{[(4-methoxybenzoyl)(3-phenylpropyl)amino]methyl}-2-biphenylcarboxylic acid (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 clin. 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, the authors report the hit-to-lead optimization of a unique series of LPA1 antagonists and their in vivo efficacy. In the part of experimental materials, we found many familiar compounds, such as Methyl 4′-formyl-[1,1′-biphenyl]-2-carboxylate(cas: 144291-47-4Recommanded Product: 144291-47-4)
Methyl 4′-formyl-[1,1′-biphenyl]-2-carboxylate(cas: 144291-47-4) belongs to esters. They are important in biology, being one of the main classes of lipids and comprising the bulk of animal fats and vegetable oils.Recommanded Product: 144291-47-4 Polyesters are important plastics, with monomers linked by ester moieties.
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics