store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
L-771688(SNAP 6383) 是一种新型有效和选择性的 α1A-肾上腺素受体拮抗剂, Ki 值为 0.43±0.02 nM。L-771688 KE 用于治疗良性前列腺增生。
产品描述 | L-771688 (SNAP 6383) is a novel potent and selective α1A-adrenoceptor antagonist with a Ki value of 0.43±0.02 nM.L-771688 KE is used for the treatment of benign prostatic hyperplasia. |
靶点活性 | Terazosin:1.8±0.65 nM (Ki), L-771688:0.052 ± 0.008 n M (Ki), GG818:0.026 ± 0.002 nM (Ki) |
体外活性 |
Highly potent inhibition of specific [3H]L-771688 binding to cloned human α1A-Adrenoceptors is observed with subtype-selective compounds GG818 (Ki=0.026±0.002 nM) and L-771688 (Ki=0.052±0.008 nM), as well as subtype non-selective α1-adrenoceptor antagonists prazosin (Ki=0.088±0.032 nM) and terazosin (Ki=1.8±0.65 nM). The relative amount of [3H]L-771688 (0.5 nM) binding in various rat tissue membranes is highest in the submaxillary gland (9.5 pmol/g tissue), followed by the brain (5.8 pmol/g tissue), vas deferens (4.3 pmol/g tissue), kidney (3.4 pmol/g tissue), heart (1.5 pmol/g tissue), urethra (1.1 pmol/g tissue), and prostate (0.88 pmol/g tissue). In contrast, low specific [3H]L-771688 binding is observed in rat urinary bladder (0.55 pmol/g tissue), liver (0.44 pmol/g tissue), aorta (0.11 pmol/g tissue), and spleen (0.11 pmol/g tissue)[1]. |
别名 | SNAP 6383 |
分子量 | 557.59 |
分子式 | C28H33F2N5O5 |
CAS No. | 200050-59-5 |
store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
L-771688 200050-59-5 GPCR/G Protein Neuroscience Adrenergic Receptor SNAP 6383 L 771688 L771688 Inhibitor inhibitor inhibit