Sildenafil Citrate

Katalog-Nr.S1431 Charge:S143103

Drucken

Technische Daten

Formel

C22H30N6O4S.C6H8O7
Molekulargewicht 666.7 CAS-Nr. 171599-83-0
Löslichkeit (25°C)* In vitro DMSO 100 mg/mL (149.99 mM)
Water Insoluble
Ethanol Insoluble
In vivo (Lösungsmittel einzeln und der Reihe nach zum Produkt hinzufügen.)
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 bedeutet schwer löslich oder unlöslich.
* Bitte beachten Sie, dass Selleck die Löslichkeit aller Verbindungen intern testet und die tatsächliche Löslichkeit geringfügig von veröffentlichten Werten abweichen kann. Dies ist normal und ist auf geringfügige Batch-zu-Batch-Variationen zurückzuführen.
* Versand bei Raumtemperatur (Stabilitätstests zeigen, dass dieses Produkt ohne Kühlmaßnahmen versendet werden kann.)

Vorbereitung von Stammlösungen

Biologische Aktivität

Beschreibung Sildenafil Citrate, ein selektiver inhibitor der zyklischen Guanosinmonophosphat (cGMP)-spezifischen Phosphodiesterase Typ 5 (PDE5), ist eine gut verträgliche und hochwirksame Behandlung für erektile Dysfunktion.
Ziele
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.

Protokoll (aus Referenz)

Referenzen

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

Kundenproduktvalidierung

<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>

Daten von [ 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.

Daten von [ 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.

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

Selleck's Sildenafil Citrate Wurde zitiert von 29 Publikationen

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

RÜCKGABERICHTLINIE
Die bedingungslose Rückgaberichtlinie von Selleck Chemical gewährleistet unseren Kunden ein reibungsloses Online-Einkaufserlebnis. Wenn Sie in irgendeiner Weise mit Ihrem Kauf unzufrieden sind, können Sie jeden Artikel innerhalb von 7 Tagen nach Erhalt zurückgeben. Im Falle von Produktqualitätsproblemen, sei es protokollbezogene oder produktbezogene Probleme, können Sie jeden Artikel innerhalb von 365 Tagen ab dem ursprünglichen Kaufdatum zurückgeben. Bitte befolgen Sie die nachstehenden Anweisungen, wenn Sie Produkte zurücksenden.

VERSAND UND LAGERUNG
Selleck-Produkte werden bei Raumtemperatur transportiert. Wenn Sie das Produkt bei Raumtemperatur erhalten, seien Sie versichert, dass die Qualitätskontrollabteilung von Selleck Experimente durchgeführt hat, um zu überprüfen, dass die normale Temperaturplatzierung von einem Monat die biologische Aktivität von Pulverprodukten nicht beeinträchtigt. Nach dem Sammeln lagern Sie das Produkt bitte gemäß den in der Datenblatt beschriebenen Anforderungen. Die meisten Selleck-Produkte sind unter den empfohlenen Bedingungen stabil.

NICHT FÜR DIE ANWENDUNG AM MENSCHEN, FÜR VETERINÄRMEDIZINISCHE DIAGNOSTIK ODER THERAPEUTISCHE ZWECKE.