L-765314
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) |
| 酸度系数(pKa) | 14.99±0.20(Predicted) |
| 形态 | 固体 |
| 颜色 | 白色至米白色 |
L-765314 用途与合成方法
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).
L-765314 价格(试剂级)
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024-11-08 | S0862 | L-765314 | 189349-50-6 | 5mg | 1220.31 |
| 2024-11-08 | S0862 | L-765314 | 189349-50-6 | 25mg | 3660.93 |
