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西地那非 /Sildenafil {[allProObj[0].p_purity_real_show]}

货号:A504277 同义名: UK-92480;Revatio

Sildenafil, one of the selective phosphodiesterase-5 (PDE5) inhibitors (IC50= 5.22 nM), is considered the best treatment for erectile dysfunction.

Sildenafil 化学结构 CAS号:139755-83-2
Sildenafil 化学结构
CAS号:139755-83-2
Sildenafil 3D分子结构
CAS号:139755-83-2
Sildenafil 化学结构 CAS号:139755-83-2
Sildenafil 3D分子结构 CAS号:139755-83-2
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Sildenafil 纯度/质量文件 产品仅供科研

货号:A504277 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 PDE PDE1 PDE10A PDE2 PDE3 PDE4 PDE5 PDE6 其他靶点 纯度
Doxofylline 99+%
Deltarasin +++

PDEδ , Kd: 38 nM

99+%
7-(2,3-Dihydroxypropyl)theophylline 98%
Aminophylline +

PDE, IC50: 0.12 mM

98+%
Anagrelide HCl 99%+
Irsogladine mAChR,AChR 98%
PF-8380 +++

Autotaxin, IC50: 2.8 nM

99%+
Dipyridamole 98%
Balipodect ++++

PDE10A, IC50: 0.3 nM

99%+
PF-2545920 ++++

PDE10A, IC50: 0.37 nM

97%
Luteolin +

PDE1, Ki: 15.0 μM

++

PDE2, Ki: 6.4 μM

+

PDE3, Ki: 13.9 μM

+

PDE4, Ki: 11.1 μM

+

PDE5, Ki: 9.5 μM

98%
Milrinone ++

PDE2, IC50: 5.2 μM

++

PDE3, IC50: 2.1 μM

ATPase 98%
Pimobendan ++

PDE3, IC50: 0.32 μM

98%
Cilostazol ++

PDE3, IC50: 0.2 μM

98%
Fenspiride HCl +

PDE3, pIC50: 3.44

+

PDE4, pIC50: 4.16

98%
(S)-(+)-Rolipram ++

PDE4, IC50: 0.75 μM

98%
Apremilast +++

PDE4, IC50: 74 nM

98%
GSK256066 ++++

PDE4B, IC50: 3.2 pM

98+%
Roflumilast ++++

PDE4A1, IC50: 0.7 nM

PDE4A4, IC50: 4.3 nM

99%
Rolipram +++

PDE4B, IC50: 130 nM

99%+
Cilomilast +++

LPDE4, IC50: 100 nM

HPDE4, IC50: 120 nM

98+%
Avanafil ++++

PDE5, IC50: 1 nM

98%
Vardenafil HCl Trihydrate ++++

PDE5, IC50: 0.7 nM

98%
Tadalafil ++++

PDE5, IC50: 1.8 nM

98%
Icariin ++

PDE5, IC50: 0.432 μM

98%
Sildenafil +++

PDE6, IC50: 33 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Sildenafil 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].
体内研究

In the dog model of erection, Sildenafil citrate significantly increases ICP and ICP/BP but has no significant effect on BP compared to vehicle[1].

Sildenafil treatment significantly reduces the number of TL+-cells at 10 mg/kg but not at 0.5 mg/kg. Additionally, 8 days after pMCAo, Sildenafil treatment (0.5 and/or 10 mg/kg dose) significantly reduces the number of microglia/macrophages stained by Iba-1[3].

Sildenafil citrate has been reported to decrease flap necrosis in preclinical animal models by increasing the secretion of growth factors (FGF and VEGF). Histologically, it is shown to be effective in rat cavernous nerve architecture[4].

体外研究

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].

Sildenafil 细胞研究

细胞系 浓度 检测类型 检测时间 活动说明 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
HEK293T cells Function assay 45 mins Inhibition of mouse Ido2 transfected in HEK293T cells using L-tryptophan as substrate assessed as kynurenine formation after 45 mins by spectrophotometric analysis, IC50=4.5 μM 23122865

Sildenafil 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 <<

Sildenafil 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.

Sildenafil 实验方案

计算器
存储液制备 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

Sildenafil 技术信息

CAS号139755-83-2
分子式C22H30N6O4S
分子量 474.57
别名 UK-92480;Revatio;Viagra
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

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

动物实验配方
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