Sildenafil Citrate

CatalogusnummerS1431 Batch:S143103

Afdrukken

Technische gegevens

Formule

C22H30N6O4S.C6H8O7
Moleculair gewicht 666.7 CAS-nr. 171599-83-0
Oplosbaarheid (25°C)* In vitro DMSO 100 mg/mL (149.99 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Voeg oplosmiddelen afzonderlijk en in volgorde toe aan het product.)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
* <1 mg/ml betekent licht oplosbaar of onoplosbaar.
* Houd er rekening mee dat Selleck de oplosbaarheid van alle verbindingen intern test en de werkelijke oplosbaarheid enigszins kan afwijken van gepubliceerde waarden. Dit is normaal en is te wijten aan lichte batch-tot-batch variaties.
* Verzending op kamertemperatuur (Stabiliteitstests tonen aan dat dit product zonder koelmaatregelen kan worden verzonden.)

Voorbereiden van stamoplossingen

Biologische activiteit

Beschrijving Sildenafil Citrate, een selectieve remmer van cyclisch guanosinemonofosfaat (cGMP)-specifieke fosfodiësterase type 5 (PDE5), is een goed verdragen en zeer effectieve behandeling voor erectiestoornissen.
Doelen
PDE5
(Cell-free assay)		 PDE6
(Cell-free assay)
3.5 nM 33 nM
In vitro Sildenafil citrate is a potent PDE type 5 reversible and selective inhibitor that blocks cGMP hydrolysis effectively (Ki ∼3 nM). Sildenafil exhibited high affinity for PDE type 5 and type 6 with inhibition constants (Ki) of ∼3.5 and 33 nM, respectively. Sildenafil enhances sodium nitroprusside- or transmural electrical stimulation-induced relaxation of precontracted corpus cavernosum muscle strips in organ baths, suggesting that sildenafil augments the activity of NO-mediated relaxation. Sildenafil citrate 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.
In vivo Sildenafil citrate enhances erectile function following pelvic nerve stimulation in anesthetized dogs as measured by increased intracavernosal pressure. Sildenafil citrate significantly reverses impaired carbachol-stimulated relaxation and inhibits superoxide formation by cavernosal tissue from hypercholesterolaemic rabbits. 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. Sildenafil use results in smooth muscle-collagen ratio protection and CD31 and eNOS expression preservation in Sprague-Dawley rats. Sildenafil reduces apoptotic indices significantly compared with control, and increases phosphorylation of akt and eNOS in Sprague-Dawley rats.

Protocol (uit referentie)

Referenties

  • https://pubmed.ncbi.nlm.nih.gov/11289569/
  • https://pubmed.ncbi.nlm.nih.gov/15963496/
  • https://pubmed.ncbi.nlm.nih.gov/18331274/

Klantproductvalidatie

<p>T24 cells were treated with vehicle, SIL (2 uM), DOX (200 nM) as indicated. Cells were isolated 6 and 12 hours after exposure, and the phosphorylation of γH2AX was determined, with the fold increase in phosphorylation shown.</p>

Gegevens van [ Mol Pharmacol , 2014 , 5(3), 408-19 ]

BT549 and HOSS1 cells in 96 well plates were treated with celecoxib (CEL 5.0 uM) and/or sildenafil (SIL, 2.0 uM). Six h after treatment cells were fixed to the plate and immunohistochemistry performed to determine the plasma membrane levels of CD95. The upper images obtained using the Hermes Wiscan imaging system is representative of the data. The intensity of CD95 immunostaining was determined using the Wisoft data analysis package (n = 3 +/- SEM). * p < 0.05 value greater than celecoxib treatment alone.

Gegevens van [ J Cell Physiol , 2014 , 10.1002/jcp.24843 ]

ADOR lung cancer cells (a July 2015 PDX model) were transfected with an empty vector plasmid or plasmids to express GRP78 and HSP27 together. Twenty-four hours after transfection cells were treated with vehicle control or with OSU-03012 (2.0mM) sildenafil (2mM) for 6 h after which cells were fixed in place and permeabilized using 0.5% Triton X100. Immuno-fluorescence was performed to detect the expression levels of Calnexin; glucosidase I; and glucosidase IIa at 10 magnification using a Hermes WiScan system.

Gegevens van [ , , J Cell Physiol, 2016, 231(10):2286-302. ]

Selleck's Sildenafil Citrate Is geciteerd door 29 Publicaties

Aging-related Repositioned Drugs, Donepezil and Sildenafil Citrate, Increase Apoptosis of Anti-mitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms [ Anticancer Research, September 2018, 5149-5157] PubMed: 30194162
Phosphodiesterase 5 (PDE5) Is Highly Expressed in Cancer-Associated Fibroblasts and Enhances Breast Tumor Progression [ Cancers, November 06, 2019, 1740] PubMed: 31698786
Repurposing statins and phenothiazines to treat chemoresistant neuroblastoma [ EMBO Molecular Medicine, December 23, 2025, Online ahead of print] PubMed: 41437160
Sildenafil protects against pulmonary hypertension induced by hypoxia in neonatal rats via activation of PPARγ-mediated downregulation of TRPC [ International Journal of Molecular Medicine, December 20, 2021, 19] PubMed: 34935055
Astragaloside IV alleviates hypoxic pulmonary hypertension by inhibiting RELM-β to reduce PINK1/Parkin-mediated mitophagy in pulmonary artery smooth muscle cells (PASMCs) [ Br J Pharmacol, 2025, 10.1111/bph.70166] PubMed: 40801101
Ginsenoside Rg1 Ameliorates Pulmonary Hypertension by Inhibiting cGAS/STING Mediated Cell Senescence [ Drug Des Devel Ther, 2025, 19:6487-6504] PubMed: 40756267
Nobiletin attenuates monocrotaline-induced pulmonary arterial hypertension through PI3K/Akt/STAT3 pathway [ J Pharm Pharmacol, 2023, rgad045] PubMed: 37158759
Astragaloside IV ameliorates pulmonary vascular remodeling in hypoxia-induced pulmonary hypertension by restraining the T follicular helper cell response and expanding T follicular regulatory cell response [ Phytomedicine, 2022, 102:154171] PubMed: 35636165
Sildenafil protects against pulmonary hypertension induced by hypoxia in neonatal rats via activation of PPARγ‑mediated downregulation of TRPC [ Int J Mol Med, 2022, 49(2)19] PubMed: 34935055
RGS2-mediated translational control mediates cancer cell dormancy and tumor relapse [ J Clin Invest, 2021, 131(1)136779] PubMed: 33393490

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NIET VOOR HUMANE, VETERINAIRE DIAGNOSTISCHE OF THERAPEUTISCHE DOELEINDEN.