638132-34-0

638132-34-0化学性质

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
溶解度 :≥46.1 mg/mL in DMSO; insoluble in H2O; ≥11.55 mg/mL in EtOH with ultrasonic
形态 :solid
酸度系数(pKa) :4.30±0.10(Predicted)
颜色 :White to off-white

638132-34-0性质、用途与生产工艺

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).