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/ Sildenafil Citrate

西地那非柠檬酸盐 /Sildenafil Citrate {[allProObj[0].p_purity_real_show]}

货号：A523537 同义名： 枸橼酸西地那非 / UK-92480 citrate;Apodefil

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

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Sildenafil Citrate 化学结构 CAS号：171599-83-0
Sildenafil Citrate 化学结构
CAS号：171599-83-0
Sildenafil Citrate 3D分子结构
CAS号：171599-83-0
Sildenafil Citrate 化学结构 CAS号：171599-83-0
Sildenafil Citrate 3D分子结构 CAS号：171599-83-0
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Sildenafil Citrate 纯度/质量文件 产品仅供科研

货号：A523537 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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 ✔ AChR,mAChR 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 ++++

PDE4A4, IC50: 4.3 nM

PDE4A1, IC50: 0.7 nM

 		99%
Rolipram +++

PDE4B, IC50: 130 nM

 		99%+
Cilomilast +++

HPDE4, IC50: 120 nM

LPDE4, IC50: 100 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 Citrate 生物活性

描述 Phosphodiesterases (PDEs) are metallo hydrolases which can be found in all tissues. PDES have 11 families which are named from PDE1 to PDE11 respectively[3]. Sildenafil Citrate is a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific PDE5, which is a well-tolerated and highly effective treatment for erectile dysfunction. Sildenafil Citrate is orally active with IC50 of 4nM and increases intracellular cGMP concentrations in cultured smooth muscle cells treated with sodium nitroprusside and in rabbit corpus cavernosum in vitro. Sildenafil is metabolized in the liver by cytochrome P450 and is converted into an active metabolite with characteristics similar to the parent compound[2]. Furthermore, Sildenafil citrate significantly reverses impaired carbachol-stimulated relaxation and inhibits superoxide formation by cavernosal tissue from hypercholesterolaemic rabbits[7]. Sildenafil improves erectile function in a time- and dose-dependent fashion with maximization of erectile function recovery occurring with daily 20 mg/kg at the 28-day time point in Sprague-Dawley rats, resulting in smooth muscle-collagen ratio protection and CD31 and eNOS expression preservation and reduces apoptotic indices significantly compared with control, and increases phosphorylation of akt and eNOS[8]. In a recent clinical trial, 46 pregnant women with severe intrauterine growth restriction were randomly allocated into two groups each included 23 patients. Intervention group received sildenafil citrate 20mg orally three times a day, in addition to fish oil and zinc supplementation. Control group received tablets similar to sildenafil and the same treatment as intervention group. Results showed significant difference between groups after intake of sildenafil. Umbilical artery pulsatility index decreased significantly (p value = 0.001) while middle cerebral artery pulsatility index increased significantly in intervention group (p value=0.001). Moreover, abdominal circumference growth velocity improved after two weeks of sildenafil intake (p value=0.001)[6].
作用机制 PDES catalyze the breakdown of cAMP or cGMP into the inactive 5′-AMP or GMP, modulating the duration and intensity of their intracellular response. While sildenafil citrate reversible and selective blocks cGMP hydrolysis of PDE5 (Ki ∼3 nM) [2].

Sildenafil Citrate 动物研究

Dose Mice: 26 mg/kg - 40 mg/kg[3] (p.o.); 1 mg/kg - 40 mg/kg[4] (i.p.) Rat: 1.4 mg/kg[5] (i.p.); 20 mg/kg[6] (p.o.)
Administration p.o., i.p.

Sildenafil Citrate 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
NCT00866463 Erectile Dysfunction Phase 1 Completed - United States, Connecticut ... 展开 >> Pfizer Investigational Site New Haven, Connecticut, United States, 06511 收起 <<
NCT00511498 Prostate Cancer Not Applicable Completed - United States, Maryland ... 展开 >> Johns Hopkins Bayview Medical Center Baltimore, Maryland, United States, 21224 收起 <<
NCT01375699 Breast Cancer ... 展开 >> Gastrointestinal Cancer Genitourinary Cancer Sarcoma Gynecologic Cancer 收起 << Phase 1 Completed - United States, Virginia ... 展开 >> Virginia Commonwealth University/Massey Cancer Center Richmond, Virginia, United States, 23298-0037 收起 <<

Sildenafil Citrate 参考文献

[1]147:12-21. doi: 10.1016/j.pharmthera.2014.10.003. Epub 2014 Oct 31.

[2]Nehra A. Sildenafil citrate, a selective phosphodiesterase type 5 inhibitor: urologic and cardiovascular implications. World J Urol. 2001 Feb;19(1):40-5. doi: 10.1007/pl00007091.

[3]Das A. PDE5 inhibitors as therapeutics for heart disease, diabetes and cancer. Pharmacol Ther. 2015 Mar;147:12-21. doi: 10.1016/j.pharmthera.2014.10.003. Epub 2014 Oct 31.

[4]33(10):1631-1637. doi: 10.1080/14767058.2018.1523892. Epub 2018 Oct 21.

[5]Shukla N. Effect of sildenafil citrate and a nitric oxide donating sildenafil derivative, NCX 911, on cavernosal relaxation and superoxide formation in hypercholesterolaemic rabbits. Eur J Pharmacol. 2005 Jul 11;517(3):224-31. doi: 10.1016/j.ejphar.2005.05.012.

[6] Shehata NAA. Addition of sildenafil citrate for treatment of severe intrauterine growth restriction: a double blind randomized placebo controlled trial. J Matern Fetal Neonatal Med. 2020 May;33(10):1631-1637. doi: 10.1080/14767058.2018.1523892. Epub 2018 Oct 21.

Sildenafil Citrate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.50mL

0.30mL

0.15mL

7.50mL

1.50mL

0.75mL

15.00mL

3.00mL

1.50mL

Sildenafil Citrate 技术信息

CAS号171599-83-0
分子式C28H38N6O11S
分子量 666.7
别名 枸橼酸西地那非 ;UK-92480 citrate;Apodefil;UK 92480;Tonafil
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度

DMSO: 50 mg/mL(75 mM)，配合低频超声助溶，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

H2O: 2 mg/mL(3 mM)，配合低频超声助溶
动物实验配方

Tags: Sildenafil | 171599-83-0 | UK-92480 | UK92480 | UK 92480 | PDE5 Inhibitor | Metabolic Enzyme/Protease | Autophagy | Apoptosis | Anti-infection | Phosphodiesterase (PDE) | Autophagy | Apoptosis | Bacterial | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Sildenafil Citrate 纯度/质量文件 | Sildenafil Citrate 亚型比较 | Sildenafil Citrate 生物活性 | Sildenafil Citrate 动物研究 | Sildenafil Citrate 临床数据 | Sildenafil Citrate 参考文献 | Sildenafil Citrate 实验方案 | Sildenafil Citrate 技术信息

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