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L-765314  ≥98%

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包装规格：1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性：溶于DMSO（50mg/mL 超声）
产品描述：基本信息 产品编号： L10412 产品名称： L-765314 CAS: 189349-50-6   储存条件 粉末 -20℃ 四年     分子式： C27H34N6O5 溶于液体 -80℃ 6个月 分子量： 522.60 -20℃ 1个月 化学名：  1-Piperazinecarboxylic acid,4-(4-amino-6,7-dimethoxy-2-quinazolinyl)-2-[[(1,1-dimethylethyl)amino]carbonyl]-,phenylmethyl ester,(2S)- Solubility (25°C)：   体外:   DMSO 100mg/mL Ethanol 100mg/mL Water Insoluble 体内(现配现用):   ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.9135mL 9.5675mL 19.1351mL 5mM 0.3827mL 1.9135mL 3.8270mL 10mM 0.1914mL 0.9568mL 1.9135mL   生物活性 产品描述 一种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 5.4nM 和 2.0nM。 靶点 Ki:5.4±0.6nM (rat α1b receptor ),2.0±0.66nM (human α1b receptor),50±8nM (rat α1d receptor),34±6nM (human α1d receptor),500±20nM (rat α1b receptor ),420±62nM (human α1b receptor).   体外研究 L-765314 exhibits two displacement sites.The high-affinity site accounts for approximately 25% of binding (IC50) 1.90nM and represents binding to the R1b sites.The low-affinity site accounts for the residual 75% of binding (IC50) 790nM 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 Cmax of L-765314 (A322312) is 1.05μM and the t1/2 is 0.5h.L-765314 shows weak potency for inhibiting the pressor response to either phenylephrine or A-61603 (AD25>3mg/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 0.3mg/kg.The results of hypotensive potency in rats show that both L-765314 and terazosin tend to decrease heart rate (about 25 bpm at 1mg/kg iv).   推荐实验方法(仅供参考) 动物实验:   Rats The potency of terazosin and L-765314 for inhibiting the pressor responses to phenylephrine and A-61603 is evaluated in anesthetized male Sprague-Dawley rats (n=4).The rats are dosed i.v with either vehicle or ascending doses of test compounds,and the peak changes in mean arterial pressure are measured.The dose of antagonist eliciting a 25 mmHg decrease in mean arterial pressure (AD25) is calculated as an index of hypotensive potency.The rats are dosed i.v with L765314 at 3mg/kg ,and the plasma is assayed by LCMS for parent compound.
保存条件：-20℃

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