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Sildenafil Citrate

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Chemical Structure| 171599-83-0 同义名 : 枸橼酸西地那非 ;UK-92480 citrate;Apodefil;UK 92480;Tonafil
CAS号 : 171599-83-0
货号 : A523537
分子式 : C28H38N6O11S
纯度 : 98%
分子量 : 666.7
MDL号 : MFCD02102122
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
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 <<
实验方案
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
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.