638132-34-0
| 中文名称 | 638132-34-0 |
|---|---|
| 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;化合物ONO-7300243 |
| 英文名称 | ONO-7300243 |
| 英文同义词 | ONO-7300243;Benzeneacetic acid, 4-[[(3,5-dimethoxy-4-methylbenzoyl)(3-phenylpropyl)amino]methyl]-;2-[4-[[(3,5-Dimethoxy-4-methylbenzoyl)-(3-phenylpropyl)amino]methyl]phenyl]acetic acid;ONO7300243,inhibit,Inhibitor,ONO 7300243,ONO-7300243,LPL Receptor,Lysophospholipid Receptor;2-(4-((3,5-Dimethoxy-4-methyl-N-(3-phenylpropyl)benzamido)methyl)phenyl)acetic acid |
| CAS号 | 638132-34-0 |
| 分子式 | C28H31NO5 |
| 分子量 | 461.55 |
| EINECS号 | |
| 相关类别 | API |
| Mol文件 | 638132-34-0.mol |
| 结构式 |  |
638132-34-0 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 | DMSO 中≥46.1 mg/mL；不溶于水； ≥11.55 mg/mL，乙醇溶液，超声波 |
| 形态 | 固体 |
| 酸度系数(pKa) | 4.30±0.10(Predicted) |
IC50: 0.19-0.13 μM (LPA1)
ONO-7300243 shows modest in vitro activity (IC 50 =0.16 μM). ONO-7300243 exhibits almost identical levels of antagonist activity in vitro.
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).
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/01/25 | HY-100882 | ONO-7300243 | 1 mg | 409元 | |
| 2024/01/25 | HY-100882 | 638132-34-0 ONO-7300243 | 638132-34-0 | 5mg | 900元 |