L-765314
| 中文名称 | L-765314 |
|---|---|
| 中文同义词 | (2S)-4-(4-氨基-6,7-二甲氧基-2-喹唑啉基)-2-[[(1,1-二甲基乙基)氨基]羰基]-1-哌嗪甲酸苯甲酯;(S)-4-(4-氨基-6,7-二甲氧基喹唑啉-2-基)-2-(叔丁基氨基甲酰基)哌嗪-1-甲酸苄酯;化合物L-765314;化合物L-765314,10 MM DMSO 溶液;L-765314 ,S0862 |
| 英文名称 | L-765,314 |
| 英文同义词 | 1-Piperazinecarboxylic acid, 4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-, phenylmethyl ester, (S)-;1-Piperazinecarboxylic acid, 4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-, phenylmethyl ester, (2S)-;Benzyl (S)-4-(4-amino-6,7-dimethoxyquinazolin-2-yl)-2-(tert-butylcarbamoyl)piperazine-1-carboxylate;Adrenergic Receptor,L-765314,Inhibitor,Beta Receptor,L765314,inhibit,L 765314;L-765314, 10 mM in DMSO;L-765314 ，S0862 |
| CAS号 | 189349-50-6 |
| 分子式 | C27H34N6O5 |
| 分子量 | 522.6 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 189349-50-6.mol |
| 结构式 |  |
L-765314 性质
| 密度 | 1.269±0.06 g/cm3(Predicted) |
|---|---|
| 储存条件 | 2-8°C(protect from light) |
| 溶解度 | DMSO:75.0(最大浓度 mg/mL);143.51(最大浓度 mM) 乙醇:100.0(最大浓度 mg/mL);191.35(最大浓度 mM) |
| 形态 | 固体 |
| 酸度系数(pKa) | 14.99±0.20(Predicted) |
| 颜色 | 白色至米白色 |
Ki: 5.4±0.6 nM (rat α1b receptor ), 2.0±0.66 nM (human α1b receptor), 50±8 nM (rat α1d receptor), 34±6 nM (human α1d receptor), 500±20 nM (rat α1b receptor ), 420±62 nM (human α1b receptor).
L-765314 exhibits two displacement sites. The high-affinity site accounts for approximately 25% of binding (IC 50 ) 1.90 nM and represents binding to the R1b sites. The low-affinity site accounts for the residual 75% of binding (IC 50 ) 790 nM and represents binding to the R1a sites.
The results of plasma assayed by liquid chromatograph/mass spectrometer (LCMS) show that the mean C max of L-765314 (A322312) is 1.05 μM and the t 1/2 is 0.5 h. L-765314 shows weak potency for inhibiting the pressor response to either phenylephrine or A-61603 (AD 25 >3 mg/kg for each). On the basis of the inhibition of pressor responses to the R1a subtype selective agonist A-61603, L-765314 appears to be selective versus the R1a receptor up to a dose of 0.3 mg/kg. The results of hypotensive potency in rats show that both L-765314 and terazosin tend to decrease heart rate (about 25 bpm at 1 mg/kg iv).
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2026/03/03 | S0862 | L-765314 L-765314 | 189349-50-6 | 5mg | 1220.31元 |
| 2026/03/03 | S0862 | L-765314 L-765314 | 189349-50-6 | 25mg | 3660.93元 |