Sildenafil Citrate

製品コードS1431 バッチS143104

印刷

化学情報

Chemical Structure Synonyms UK-92480 Citrate Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C22H30N6O4S.C6H8O7
分子量 666.7 CAS No. 171599-83-0
Solubility (25°C)* 体外 DMSO 20 mg/mL warmed with 50ºC water bath (29.99 mM)
Water Insoluble
Ethanol Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Sildenafil Citrate, a selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), is a well-tolerated and highly effective treatment for erectile dysfunction.
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. [1]
in vivo Sildenafil citrate enhances erectile function following pelvic nerve stimulation in anesthetized dogs as measured by increased intracavernosal pressure. [1] Sildenafil citrate significantly reverses impaired carbachol-stimulated relaxation and inhibits superoxide formation by cavernosal tissue from hypercholesterolaemic rabbits. [2] 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. [3]

プロトコル(参考用のみ)

カスタマーフィードバック

Data from [Mol Pharmacol, 2014, 5(3), 408-19]

Data from [Data independently produced by J Cell Physiol, 2014, 10.1002/jcp.24843]

Data from [Data independently produced by , , J Cell Physiol, 2016, 231(10):2286-302. ]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

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
Additive protective effects of sacubitril/valsartan and bosentan on vascular remodelling in experimental pulmonary hypertension [ Cardiovasc Res, 2021, 117(5):1391-1401] PubMed: 32653925
Kyoto probe-1 reveals phenotypic differences between mouse ES cells and iTS-P cells [ Sci Rep, 2020, 10(1):18084] PubMed: 33093580
Phosphodiesterase 5 (PDE5) Is Highly Expressed in Cancer-Associated Fibroblasts and Enhances Breast Tumor Progression. [ Cancers (Basel), 2019, 11(11)] PubMed: 31698786
Evaluation of Sildenafil and Tadalafil for Reversing Constriction of Fetal Arteries in a Human Placenta Perfusion Model. [ Hypertension, 2018, 72(1):167-176] PubMed: 29735634
The cyclic GMP/protein kinase G pathway as a therapeutic target in head and neck squamous cell carcinoma [Tuttle TR, et al. Cancer Lett, 2016, 370(2):279-85] PubMed: 26551887
AR-12 Inhibits Multiple Chaperones Concomitant With Stimulating Autophagosome Formation Collectively Preventing Virus Replication [Booth L, et al. J Cell Physiol, 2016, 231(10):2286-302] PubMed: 27187154

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。