Sildenafil citrate
作者：齊岳
發(fā)布時間：2023-09-11
09:05:09
點(diǎn)擊數(shù)：
產(chǎn)品名稱：Sildenafil citrate
產(chǎn)品描述：
| 產(chǎn)品描述 | Sildenafil, a cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) Inhibitor, is used extensively for erectile dysfunction and less commonly for pulmonary hypertension. |
| 靶點(diǎn)活性 | PDE5:3.5 nM, PDE6:33 nM |
| 體外活性 | 在麻醉的狗體內(nèi),Sildenafil citrate增強(qiáng)盆骨神經(jīng)刺激下陰莖的勃起功能.在Sprague-Dawley大鼠體內(nèi), 每天Sildenafil（20 mg/kg）以時間劑量依賴的方式改善勃起功能,同時Sildenafil明顯減少細(xì)胞凋亡指數(shù),并且增加akt 和eNOS的磷酸化作用. |
| 體內(nèi)活性 | 在內(nèi)皮細(xì)胞中,Sildenafil通過降低由高血糖引起的氧化應(yīng)激和增加細(xì)胞內(nèi)Ca2 +水平,改善胰島素信號傳導(dǎo)NO產(chǎn)生。Sildenafil citrate是一種強(qiáng)效的PDEⅤ型的可逆選擇性抑制劑,其能夠有效阻斷cGMP的水解作用(Ki ～3 nM)。 |
| 激酶實驗 | 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. |
| 細(xì)胞實驗 | 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]. |
| 別名 | 西地那非檸檬酸鹽, UK-92480 citrate, 枸櫞酸西地那非 |
| 分子量 | 666.7 |
| 分子式 | C28H38N6O11S |
| CAS No. | 171599-83-0 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 66.7 mg/mL (100 mM)
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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西安齊岳生物科技有限公司是集化學(xué)科研和定制與一體的高科技化學(xué)公司。業(yè)務(wù)范圍包括化學(xué)試劑和產(chǎn)品的研發(fā)、生產(chǎn)、銷售等。涉及產(chǎn)品為通用試劑的分銷、非通用試劑的定制與研發(fā)，涵蓋生物科技、化學(xué)品、中間體和化工材料等領(lǐng)域。
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