中文同义词:
2-(4-((3,5-二甲氧基-4-甲基-N-(3-苯基丙基)苯甲酰胺)甲基)苯基)乙酸
英文同义词:
ONO-7300243;Benzeneacetic acid, 4-[[(3,5-dimethoxy-4-methylbenzoyl)(3-phenylpropyl)amino]methyl]-
沸点
688.1±55.0 °C(Predicted)
密度
1.180±0.06 g/cm3(Predicted)
储存条件
Sealed in dry,Store in freezer, under -20°C
酸度系数(pKa)
4.30±0.10(Predicted)
生物活性
ONO-7300243 是一种新型有效的溶血磷脂酸受体 1 (LPA1) 拮抗剂，IC50 为 0.16 μM。
靶点
IC50: 0.19-0.13 μM (LPA1)
体外研究
ONO-7300243 shows modest in vitro activity (IC 50 =0.16 μM). ONO-7300243 exhibits almost identical levels of antagonist activity in vitro.
体内研究
ONO-7300243 shows good efficacy in vivo. The oral dosing of 17a at 30 mg/kg leads to reduced intraurethral pressure in rats. ONO-7300243 shows stronge effects in vivo (88% inhibition at 10 mg/kg i.d., 62% inhibition at 3 mg/kg i.d.) compared with compound 12g. The results reveal that ONO-7300243 shows good membrane permeability and good metabolic stability against rat liver microsomes (MS). ONO-7300243 exhibits good selectivity towards LPAl over LPA2, most likely because low molecular weight and low lipophilicity lead to reduced compound promiscuity and increased selectivity. ONO-7300243 inhibits the LPA-induced IUP increase in a dose dependent manner (ID 50 =11.6 mg/kg p.o.) up to 1 h after dosing. Significant effects are observed at 10 and 30 mg/kg (p<0.05 vs.vehicle). ONO-7300243 (30 mg/kg, p.o.) leads to a significant decrease in the IUP in conscious rats without LPA stimulation compared with the vehicle without affecting the mean blood pressure (MBP). The results of a rat pharmacokinetic study of ONO-7300243 show that this material had a rapid clearance (CLtot=15.9 mL/min/kg at 3 mg/kg i.v.) and a short half-life (0.3 h).
