Sildenafil

Catalog No.S4684 Batch:S468402

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Technical Data

Formula

C22H30N6O4S
Molecular Weight 474.58 CAS No. 139755-83-2
Solubility (25°C)* In vitro DMSO 95 mg/mL (200.17 mM)
Water 3.5 mg/mL (7.37 mM)
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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description Sildenafil (Revatio, UK-92480, Viagra) is a Phosphodiesterase 5 Inhibitor with IC50 of 5.22 nM.
Targets
PDE5 [1]
5.22 nM
In vitro Sildenafil improves insulin signalling and NO production in endothelial cells, probably by reducing oxidative stress induced by hyperglycemia and by increasing intracellular Ca2+ levels[2].
In vivo Acute administration of the PDE-5 inhibitor sildenafil in a single clinically relevant dose does not modulate the in vivo function of the hypertrophic failing right heart of the rat measured by echocardiography and invasive hemodynamics[1].

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    HUVEC and HAEC

  • Concentrations

    1 μM

  • Incubation Time

    5 or 72 h

  • Method

    HUVEC and HAEC from passages 3 to 6 are cultured for 72 hours in presence of 5.5 mmol/L glucose, 30 mmol/L glucose (high glucose; HG), 10 mmol/L Gluc-N with or without 1 µM of sildenafil (5 or 72 h) and/or 10−7 M insulin.
Animal Study:

[1]
  • Animal Models

    Wistar rats

  • Dosages

    1 mg/kg

  • Administration

    i.v.

Customer Product Validation

Data from [Data independently produced by , , EXPERIMENTAL AND THERAPEUTIC MEDICINE, 2017, 13:2645-2650]

Selleck's Sildenafil has been cited by 20 publications

Monitoring recovery after CNS demyelination, a novel tool to de-risk pro-remyelinating strategies [ Brain, 2023, 146(6):2453-2463] PubMed: 36995973
Additive protective effects of sacubitril/valsartan and bosentan on vascular remodelling in experimental pulmonary hypertension [ Cardiovasc Res, 2021, 117(5):1391-1401] PubMed: 32653925
(Curcumin+sildenafil) enhances the efficacy of 5FU and anti-PD1 therapies in vivo. [ J Cell Physiol, 2020, 10.1002/jcp.29580] PubMed: 31985048
Kyoto probe-1 reveals phenotypic differences between mouse ES cells and iTS-P cells [ Sci Rep, 2020, 10(1):18084] PubMed: 33093580
Skeletal restoration by phosphodiesterase 5 inhibitors in osteopenic mice: Evidence of osteoanabolic and osteoangiogenic effects of the drugs. [ Bone, 2020, 10.1016/j.bone.2020.115305] PubMed: 32126313
The role of PDE5a in oocyte maturation of zebrafish. [ Gen Comp Endocrinol, 2020, 286:113303] PubMed: 31654676
Neratinib augments the lethality of [regorafenib + sildenafil] [Booth L J Cell Physiol, 2019, 234(4):4874-4887] PubMed: 30203445
Palbociclib augments Neratinib killing of tumor cells that is further enhanced by HDAC inhibition [Booth L Cancer Biol Ther, 2018, 10.1080/15384047.2018.1507665] PubMed: 30183517
Aging-related Repositioned Drugs, Donepezil and Sildenafil Citrate, Increase Apoptosis of Anti-mitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms [Kim JY Anticancer Res, 2018, 38(9):5149-5157] PubMed: 30194162
NEDD4 over-expression regulates the afatinib resistant phenotype of NSCLC cells [ Oncol Signal, 2018, 1(1):19-30] PubMed: 30740589

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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.