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ONO-7300243

CAS No. : 638132-34-0

MCE 站：ONO-7300243

产品活性：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。

研究领域：GPCR/G Protein

作用靶点：LPL Receptor

In Vitro: ONO-7300243 shows modest in vitro activity (IC₅₀=0.16 μM). ONO-7300243 exhibits almost identical levels of antagonist activity in vitro.

In Vivo: 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 (ID₅₀=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).

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