Sildenafil

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Chemical Structure| 139755-83-2 同义名 : UK-92480; Revatio; Viagra
CAS号 : 139755-83-2
货号 : A504277
分子式 : C22H30N6O4S
纯度 : 98%
分子量 : 474.57
MDL号 : MFCD00867528
存储条件：

Pure form Sealed in dry,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 30 mg/mL(63.21 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
生物活性
靶点

  • PDE6

    PDE6, IC50:33 nM

  • PDE5

    PDE5, IC50:3.5 nM

  • PDE5

    PDE5, IC50:5.22 nM

  • PDE5
描述 Pre-treatment with 1 μM Sildenafil enhances the phosphorylation of ERK1/ERK2, increases the percentage of cells in S phase, and promotes cell proliferation compared to serotonin stimulation alone (P<0.05). Additionally, pretreatment with 1 μM Sildenafil citrate followed by serotonin stimulation significantly increases the OD value to 0.33, which is significantly different from serotonin stimulation alone (P<0.05). Moreover, 1 μM Sildenafil markedly enhances the upregulation of ERK1/ERK2 phosphorylation induced by serotonin[2].
细胞研究
细胞系 浓度 检测类型 检测时间 活性说明 数据源
CHO cells Function assay Inhibition of human ERG expressed in CHO cells by whole cell patch clamp technique, IC50=3.31131 μM 18448342
COS7 cells Function assay Inhibition of human recombinant PDE5A1 expressed in COS7 cells, IC50=0.075 μM 18778098
HEK293T cells Function assay 2 h Displacement of [3H]ZM241385 from human AA2AR expressed in HEK293T cells after 2 hrs by liquid scintillation counter, Ki=0.19953 μM 22563707
临床研究
NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02372487 Pregnancy Complication Not Applicable Unknown June 2016 Egypt ... 展开 >> Menoufia University Recruiting Shebin Elkom, Egypt Contact: tarek elsayed    00201222739097       Contact: mohamed maher          Principal Investigator: tarek sayed          Saudi Arabia Alhayah national hospital Recruiting Abha, Saudi Arabia Contact: mohamed maher    +966558198655       Contact: tarek sayyed          Principal Investigator: mohamed maher          Alhayah national hospital Recruiting Abha, Saudi Arabia Contact: mohamed maher    +966558198655       Principal Investigator: mohamed maher 收起 <<
NCT02524184 Obesity Phase 4 Unknown September 2016 China, Hubei ... 展开 >> Wuhan General Hospital Recruiting Wuhan, Hubei, China, 430070 Contact: Guangda Xiang, MD    13517275283    Guangda64@hotmail.com    Contact: Lin Xiang, MD    18627838901    xianglin832010@hotmail.com 收起 <<
NCT01800292 Hypertension, Pulmonary Artery... 展开 >> Ventricular Dysfunction, Left 收起 << Phase 4 Completed - United States, Arizona ... 展开 >> University of Arizona Medical Center Tucson, Arizona, United States, 85724 收起 <<
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.54mL

2.11mL

1.05mL

21.07mL

4.21mL

2.11mL
参考文献

[1]Wayman C, et al. Cligosiban, A Novel Brain-Penetrant, Selective Oxytocin Receptor Antagonist, Inhibits Ejaculatory Physiology in Rodents. J Sex Med. 2018 Dec;15(12):1698-1706.

[2]Karpenko IA, et al. Selective nonpeptidic fluorescent ligands for oxytocin receptor: design, synthesis, and application to time-resolved FRET binding assay. J Med Chem. 2015 Mar 12;58(5):2547-52.

[3]Moretti R, et al. Sildenafil, a cyclic GMP phosphodiesterase inhibitor, induces microglial modulation after focal ischemia in the neonatal mouse brain. J Neuroinflammation. 2016 Apr 28;13(1):95.