L-765314

L-765314化学性质

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(Max Conc. mg/mL);143.51(Max Conc. mM)
Ethanol:100.0(Max Conc. mg/mL);191.35(Max Conc. mM)
酸度系数(pKa) :14.99±0.20(Predicted)
形态 :Solid
颜色 :White to off-white

L-765314性质、用途与生产工艺

生物活性 L-765314 是 α1b 肾上腺素能受体 (α1b adrenergic receptor) 的一个有效的、选择性拮抗剂，其在大鼠和人体中的 Ki 值分别为 5.4 nM 和 2.0 nM。
靶点

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).
体外研究

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.
体内研究

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上下游产品信息

上游原料

下游产品

L-765314 试剂级价格

L-765314生产厂家