Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Sildenafil citrate (UK-92480 citrate) 是一种磷酸二酯酶 5 抑制剂,IC50为 5.22 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
5 mg | ¥ 153 | 现货 | ||
10 mg | ¥ 198 | 现货 | ||
25 mg | ¥ 318 | 现货 | ||
50 mg | ¥ 453 | 现货 | ||
100 mg | ¥ 646 | 现货 | ||
200 mg | ¥ 958 | 现货 | ||
500 mg | ¥ 1,580 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 226 | 现货 |
产品描述 | Sildenafil citrate (UK-92480 citrate) , a cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) Inhibitor, is used extensively for erectile dysfunction and less commonly for pulmonary hypertension. |
靶点活性 | PDE6:33 nM, PDE5:3.5 nM |
体外活性 | 在麻醉的狗体内,Sildenafil citrate增强盆骨神经刺激下阴茎的勃起功能.在Sprague-Dawley大鼠体内, 每天Sildenafil(20 mg/kg)以时间剂量依赖的方式改善勃起功能,同时Sildenafil明显减少细胞凋亡指数,并且增加akt 和eNOS的磷酸化作用. |
体内活性 | 在内皮细胞中,Sildenafil通过降低由高血糖引起的氧化应激和增加细胞内Ca2 +水平,改善胰岛素信号传导NO产生。Sildenafil citrate是一种强效的PDEⅤ型的可逆选择性抑制剂,其能够有效阻断cGMP的水解作用(Ki ~3 nM)。 |
激酶实验 | COX enzyme assay in vitro: Expression of COX protein in insect cells is determined by assessing PG-synthetic capability in homogenates from cells incubated for 3 days with COX-1 or COX-2 baculovirus. Cells expressing COX-1 or COX-2 are homogenized and incubated with arachidonic acid (10 μM). COX activity is determined by monitoring PG production. No COX activity is detected in mock-infected Sf9 cells. Celecoxib are preincubated with crude 1% CHAPS homogenates (2-10 μg of protein) for 10 minutes before addition of arachidonic acid. PGE2 formed is detected by ELISA after 10 minute incubation. |
细胞实验 | Sildenafil is prepared in DMSO and stored, and then diluted with appropriate medium before use[2]. Cells at approximately 90% confluence are harvested with 0.1% trypsin/0.01% ethylene diamine tetraacetic acid (EDTA) solution and seeded into a 96-well plate at a density of 2×104 cells/well and grown in RPMI-1640 containing 10% FBS for three days, followed by serum starvation for three days. Cells are then incubated for different time with various concentration of serotonin or 1 μM Sildenafil followed by serotonin with or without U0126, as indicated. Control cells are treated in the same way except sterile PBS replaced the drug. After treatment, medium is changed to fresh medium, and cells are incubated with 5 g/L of MTT for four hours. MTT is then dissolved with 150 μL of 10% DMSO for 20 minutes. The optical densities (OD) in the 96-well plates are determined using a microplate reader at 570 nm[2]. |
别名 | UK-92480 citrate, 西地那非柠檬酸盐, 枸橼酸西地那非 |
分子量 | 666.7 |
分子式 | C28H38N6O11S |
CAS No. | 171599-83-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 45 mg/mL (67.5 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 1.4999 mL | 7.4996 mL | 14.9993 mL | 37.4981 mL |
5 mM | 0.3 mL | 1.4999 mL | 2.9999 mL | 7.4996 mL | |
10 mM | 0.15 mL | 0.75 mL | 1.4999 mL | 3.7498 mL | |
20 mM | 0.075 mL | 0.375 mL | 0.75 mL | 1.8749 mL | |
50 mM | 0.03 mL | 0.15 mL | 0.3 mL | 0.75 mL |
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。
Sildenafil citrate 171599-83-0 Apoptosis Autophagy Metabolism PDE inhibit UK92480 UK-92480 citrate UK-92480 Citrate UK-92480 UK 92480 Citrate 西地那非柠檬酸盐 Inhibitor UK 92480 Phosphodiesterase (PDE) 枸橼酸西地那非 Sildenafil Sildenafil Citrate UK92480 Citrate inhibitor