189362-06-9
中文名称 | 189362-06-9 |
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中文同义词 | 化合物 T15640 |
英文名称 | K134 |
英文同义词 | K134;1-Cyclopropyl-1-((1R,2R)-2-hydroxycyclohexyl)-3-(3-((2-oxo-1,2-dihydroquinolin-6-yl)oxy)propyl)urea;OPC33509;Urea, N-cyclopropyl-N'-[3-[(1,2-dihydro-2-oxo-6-quinolinyl)oxy]propyl]-N-[(1R,2R)-2-hydroxycyclohexyl]-;K-134,K134 |
CAS号 | 189362-06-9 |
分子式 | C22H29N3O4 |
分子量 | 399.48 |
EINECS号 | |
相关类别 | |
Mol文件 | 189362-06-9.mol |
结构式 |
189362-06-9 性质
沸点 | 731.4±60.0 °C(Predicted) |
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密度 | 1.29±0.1 g/cm3(Predicted) |
储存条件 | 4°C, away from moisture and light |
溶解度 | 溶于二甲基亚砜 |
酸度系数(pKa) | 11.13±0.70(Predicted) |
IC50: 0.1 µM (PDE3A), 0.28 µM (PDE3B), 12.1 μM (PDE5)
K134 (K-134) inhibits rat platelet aggregation induced by collagen and ADP in a dose-dependent manner in vitro. The half-maximal (50%) inhibitory concentration (IC 50 ) values of K134 are 2.5 µM and 3.2 µM, respectively. In vitro experiments, K134 also inhibits mouse platelet aggregation induced by collagen and ADP in a dose-dependent manner, and the IC 50 s are 5.5 µM and 6.7 µM, respectively.
K134 (K-134) significantly prolongs middle cerebral artery (MCA) occlusion time at doses >10 mg/kg, and reduces cerebral infarct size at 30 mg/kg in the stroke model (n = 12, 87.5±5.6 vs. 126.8±7.5 mm 3 , P<0.01), indicating its potent antithrombotic effect. The overall bleeding risk of K134 is assessed in general in mice. Single oral administration of K134 does not prolong bleeding time at a dose of 30 mg/kg compared to control (106±5 vs. 110±5 s, not significant). Moreover, a sufficiently high enough plasma concentration of K134 (13.6±2.3 µM) is detected to inhibit platelet aggregation at 10 min after single administration in mice at a dose of 30 mg/kg, which is the same time point as the above test of bleeding time. Next, the effects of PDE3 inhibitors on thrombus formation are also investigated in an arteriovenous shunt model in rats. K134 significantly reduces the incidence of occlusive shunt thrombi at doses above 10 mg/kg (half-maximal effective dose: ED 50 =11 mg/kg). The plasma concentration of K134 is 0.43±0.08 µM (C max ) at a dose of 10 mg/kg.
安全信息
更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
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2024/01/25 | HY-U00186 | K134 | 1 mg | 2045元 | |
2024/01/25 | HY-U00186 | 189362-06-9 K134 | 189362-06-9 | 5mg | 4500元 |