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Technical Data
| Formula | C22H30N6O4S.C6H8O7 |
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| Molecular Weight | 666.7 | CAS No. | 171599-83-0 | |
| Solubility (25°C)* | In vitro | DMSO | 23 mg/mL (34.49 mM) | |
| Water | Insoluble | |||
| Ethanol | Insoluble | |||
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* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Biological Activity
| Description | 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. | ||||
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| 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] |
Protocol (from reference)
References
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Customer Product Validation
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Data from [Mol Pharmacol, 2014, 5(3), 408-19]
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Data from [Data independently produced by J Cell Physiol, 2014, 10.1002/jcp.24843]
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Data from [Data independently produced by , , J Cell Physiol, 2016, 231(10):2286-302. ]
Selleck's Sildenafil Citrate has been cited by 22 publications
| 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 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.