2. Metabolic Enzyme/Protease Autophagy Apoptosis Anti-infection
  3. Phosphodiesterase (PDE) Autophagy Apoptosis Bacterial
  4. Sildenafil

Sildenafil  (Synonyms: UK-92480)

Cat. No.: HY-15025 Purity: 99.90%
COA Handling Instructions

Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.

For research use only. We do not sell to patients.

Sildenafil Chemical Structure

Sildenafil Chemical Structure

CAS No. : 139755-83-2

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Solution
10 mM * 1 mL in DMSO USD 61 In-stock
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10 mM * 1 mL
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100 mg USD 77 In-stock
200 mg USD 132 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Sildenafil:

Sildenafil Related Antibodies

Top Publications Citing Use of Products

    Sildenafil purchased from MCE. Usage Cited in: Physiol Rep. 2023 Jan;11(1):e15549.  [Abstract]

    The index of cell proliferation in the lungs is significantly reduced in hypoxic mice that received CL316243, sildenafil, or riociguat compared with hypoxic mice treated with vehicle.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Sildenafil (UK-92480) is a potent phosphodiesterase type 5 (PDE5) inhibitor with an IC50 of 5.22 nM.

    IC50 & Target

    PDE5

     

    In Vitro

    Pretreatment with 1 μM Sildenafil potentiates the phosphorylation of ERK1/ERK2, an increase in the percentage of cells in S phase and cell proliferation, compared with serotonin stimulation alone (P<0.05). Pretreatment with 1 μM Sildenafil citrate followed by serotonin stimulation leads to dramatic increase in OD value to 0.33, significantly different compared with serotonin stimulation alone (P<0.05). 1 μM Sildenafil obviously enhances the upregulation of ERK1/ERK2 phosphorylation induced by serotonin[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Sildenafil Related Antibodies
    In Vivo

    In the dog model of erection, Sildenafil citrate significantly increases ICP and ICP/BP but shows no significant effect on BP compared with vehicle[1]. Sildenafil treatment significantly decreases the number of TL+-cells at 10 but not 0.5 mg/kg. 8 days after pMCAo the number of microglia/macrophages stained by Iba-1 are significantly reduced by Sildenafil treatment (0.5 and/or 10 mg/kg dose)[3]. Sildenafil citrate has been reported to decrease flap necrosis in preclinical animal models by increasing the secretion of growth factors (FGF and VEGF), and histologically is shown to be effective in rat cavernous nerve architecture[4].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    474.58

    Appearance

    Solid

    Formula

    C22H30N6O4S
    CAS No.
    SMILES

    O=C1C(N(C)N=C2CCC)=C2N=C(C3=CC(S(=O)(N4CCN(C)CC4)=O)=CC=C3OCC)N1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 1 year
    -20°C 6 months
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 29 mg/mL (61.11 mM)

    H2O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1071 mL 10.5356 mL 21.0713 mL
    5 mM 0.4214 mL 2.1071 mL 4.2143 mL
    10 mM 0.2107 mL 1.0536 mL 2.1071 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  50% PEG300    50% saline

      Solubility: ≥ 10 mg/mL (21.07 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.27 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.90%

    COA (251 KB) LCMS (108 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Cells at approximately 90% confluence are harvested with 0.1% trypsin/0.01% ethylene diamine tetraacetic acid (EDTA) solution and seeded into a 96-well plate at a density of 2×104 cells/well and grown in RPMI-1640 containing 10% FBS for three days, followed by serum starvation for three days. Cells are then incubated for different time with various concentration of serotonin or 1 μM Sildenafil followed by serotonin with or without U0126, as indicated. Control cells are treated in the same way except sterile PBS replaced the drug. After treatment, medium is changed to fresh medium, and cells are incubated with 5 g/L of MTT for four hours. MTT is then dissolved with 150 μL of 10% DMSO for 20 minutes. The optical densities (OD) in the 96-well plates are determined using a microplate reader at 570 nm[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [3][4]

    Mice[3]
    Ischemia is induced in C57Bl/6 mice on postnatal (P) day 9 by permanent middle cerebral artery occlusion (pMCAo), and followed by either PBS or Sildenafil intraperitoneal (i.p.) injections. In the first set of experiments, animals are randomly divided into five groups and treated with either PBS or a single dose of Sildenafil citrate (0.5, 2.5, 10, and 15 mg/kg), given intraperitoneally (i.p.) 5 min after pMCAo. In the second set of experiments, animals are randomly divided into three groups and treated with either PBS or a single dose of Sildenafil citrate (0.5 and 10 mg/kg, i.p.) 5 min after pMCAo.
    Rats[4]
    Thirty male Sprague-Dawley rats weighing between 210 and 240 g are used. Rats from all groups are anesthetized with xylazine + ketamine and then a crush injury is created by using a one-minute long vascular clamp to the right sciatic nerve. One day before the procedure, rats from Group 1 are started on a 28-day treatment consisting of a daily dose of 20 mg/kg body weight Sildenafil given orally via nasogastric tube, while the rats from Group 2 are started on an every-other-day dose of 10 mg/kg body weight Sildenafil citrate. Rats from Group 3 did not receive any drugs. Subjects in all 3 groups are fed ad libitum with normal rat chow and tap water. Forty-two days after the nerve damage is created, the rats underwent a static sciatic index (SSI) test, sedation and motor coordination tests, and accelerated rotarod tests. Rats are sacrificed under anesthesia and their sciatic nerves are removed surgically. Histopathologic analyses of the nerves and bone densitometry evaluation of the extremities are then performed.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Sildenafil Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Sildenafil139755-83-2UK-92480UK92480UK 92480Phosphodiesterase (PDE)AutophagyApoptosisBacterialInhibitorinhibitorinhibit

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