Art. -Nr.: HY-15025A

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Sildenafil citrate

(Synonyms: UK-92480 citrate)

16 Cited Publications

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Based on 16 publication(s) in Google Scholar

Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC₅₀ of 5.22 nM.

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Reinheit: 99.86%
CAS. Nr.: 171599-83-0
Formel: C₂₈H₃₈N₆O₁₁S
Molecular Weight:666.70

Speicherung:

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Sildenafil citrate Chemical Structure

CAS. Nr.: 171599-83-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (16)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC₅₀ of 5.22 nM.

IC₅₀ & Target

PDE5

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen :

In Vitro

Pretreatment with 1 μM Sildenafil citrate 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].

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

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. At this time point, cells positive for the M1-like marker COX-2⁺ are found in the ischemic core in PBS-treated animals, whereas they are mostly observed in the penumbra in 10 mg/kg (but not 0.5 mg/kg) Sildenafil-treated animals. In contrast, 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].

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

Chemical Information

CAS. Nr. 171599-83-0
Appearance Solid
Molecular Weight 666.70
Formel C₂₈H₃₈N₆O₁₁S
Color White to off-white
SMILES

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

UK-92480 citrate
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)

Publications (16)

All Bio/Physico-chemical AssayRT-PCRIn Vivo Efficacy StudyWBHistological Imaging/StainingIHCCell Proliferation/Viability AssayCell Migration/Invasion AssayApoptosis AnalysisIF

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Journal Impact Factor

Nature

Rescuing dendritic cell interstitial motility sustains antitumour immunity. [Abstract]

2025 Sep;645(8079):244-253. PMID: 40562926

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Nature. 2025 Sep;645(8079):244-253. [Abstract]

The mean velocities of immature BMDCs in 3D collagen gel treated with vehicle, 30 μM Sildenafil or sildenafil plus 10 μM ODQ. From left to right, n = 98, 79, 126 cells.

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Nature. 2025 Sep;645(8079):244-253. [Abstract]

Tumour growth and survival curves of MC38-Pde5−/− tumour-bearing mice treated with vehicle or Sildenafil (20 μg/g).
Phytomedicine

Crocin inhibits neutrophil migration and activation to treat hypoxic pulmonary hypertension through targeting HCK. [Abstract]

2025 Sep 25:148:157334. PMID: 41043333
ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Phytother Res

Celastrol Ameliorates Hypoxia-Induced Pulmonary Hypertension by Regulation of the PDE5-cGMP-PKG Signaling Pathway. [Abstract]

2025 Mar;39(3):1549-1564. PMID: 39887769

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Phytother Res. 2025 Mar;39(3):1549-1564. [Abstract]

Sildenafil citrate (SN, 25 mg/kg; oral gavage; once a day for 21 days). Summarized values of right ventricular systolic pressure (RVSP).

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Phytother Res. 2025 Mar;39(3):1549-1564. [Abstract]

Sildenafil citrate (SN, 25 mg/kg; oral gavage; once a day for 21 days). Histological images with H&E staining of RV cross- sectional cells and representative views of Masson's trichrome staining to detect RV fibrosis, Scale bar, 20 μm.

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Phytother Res. 2025 Mar;39(3):1549-1564. [Abstract]

Sildenafil citrate (SN, 25 mg/kg; oral gavage; once a day for 21 days). Immunohistochemistry staining of lung samples for α-SMA, and the expression of Ki-67 and PCNA in pulmonary arteries was verified by immunohistochemistry staining.Scale bar, 20 μm.

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Phytother Res. 2025 Mar;39(3):1549-1564. [Abstract]

Sildenafil citrate (SN, 25 mg/kg; oral gavage; once a day for 21 days). Western blot on PDE5 and PKG in mice lung tissue, n = 3.

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Phytother Res. 2025 Mar;39(3):1549-1564. [Abstract]

Sildenafil citrate (SN, 1 μM; 24 h). Quantitative measurement of EdU incorporation into HPASMCs.

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Phytother Res. 2025 Mar;39(3):1549-1564. [Abstract]

Sildenafil citrate (SN, 1 μM; 24 h). Summarized data showing the number of migrating cells.

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Phytother Res. 2025 Mar;39(3):1549-1564. [Abstract]

Sildenafil citrate (SN, 1 μM; 24 h). Summary data showing the number of apoptotic HPASMCs.
Br J Pharmacol

An adenosinergic positive feedback loop extends pharmacological cardioprotection duration. [Abstract]

2024 Dec;181(23):4920-4936. PMID: 39256947
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Bioeng Transl Med

Ultrasound-targeted microbubble destruction mediates PDE5i/NO integration for cavernosum remodeling and penile rehabilitation. [Abstract]

2023 Jul 2;8(5):e10568. PMID: 37693040
Int J Mol Sci

A Dual-Acting Nitric Oxide Donor and Phosphodiesterase 5 Inhibitor Activates Autophagy in Primary Skin Fibroblasts. [Abstract]

2022 Jun 20;23(12):6860. PMID: 35743299

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Jun 20;23(12):6860. [Abstract]

P62 mRNA levels in NHF upon Sildenafil treatment (100 μM, 6 h) in presence or absence of ConA (2.5 nM, 2 h).

Sildenafil citrate purchased from MedChemExpress. Usage Cited in: Int J Mol Sci. 2022 Jun 20;23(12):6860. [Abstract]

Analysis of the autophagic flux in NHF upon treatment with Sildenafil (100 μM, 24 h) in presence or absence of ConA (2.5 nM; 2 h).
ACS Omega

Computational Approaches to Identify Molecules Binding to Mycobacterium tuberculosis KasA. [Abstract]

2020 Nov 15;5(46):29935-29942. PMID: 33251429
Biochim Biophys Acta Mol Basis Dis

OTUD1 promotes isoprenaline- and myocardial infarction-induced heart failure by targeting PDE5A in cardiomyocytes. [Abstract]

2024 Mar;1870(3):167018. PMID: 38185350
Sci Rep

Characterization of five novel vasopressin V2 receptor mutants causing nephrogenic diabetes insipidus reveals a role of tolvaptan for M272R-V2R mutation. [Abstract]

2020 Oct 2;10(1):16383. PMID: 33009446
Saudi Pharm J

Fisetin alleviates pulmonary arterial hypertension by inhibiting the TGF-β1/Smad 2/3 signaling pathway. [Abstract]

2026 Jun 25;34(3):39. PMID: 42347890
J Nat Med

Nobiletin alleviates hypoxia-induced pulmonary hypertension by inhibiting calcium-sensing receptor. [Abstract]

2025 Sep;79(5):1154-1166. PMID: 40581895
Biochem Biophys Res Commun

Lactic acid inhibits iNKT cell functions via a phosphodiesterase-5 dependent pathway. [Abstract]

2021 Apr 2:547:9-14. PMID: 33588236
Physiol Rep

β3 adrenergic agonism: A novel pathway which improves right ventricular-pulmonary arterial hemodynamics in pulmonary arterial hypertension. [Abstract]

2023 Jan;11(1):e15549. PMID: 36597221

Sildenafil citrate purchased from MedChemExpress. 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 (50 mg/kg), or riociguat compared with hypoxic mice treated with vehicle.
Biomed Chromatogr

A novel standard-free detection of adulteration method for sildenafil derivatives in dietary supplements. [Abstract]

2024 Aug;38(8):e5925. PMID: 38837800

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (75.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : 2 mg/mL (3.00 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.4999 mL

7.4996 mL

14.9992 mL

5 mM

0.3000 mL

1.4999 mL

2.9998 mL

10 mM

0.1500 mL

0.7500 mL

1.4999 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture). When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

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

Solubility: ≥ 5 mg/mL (7.50 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 5 mg/mL (7.50 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 5 mg/mL (7.50 mM); Clear solution

This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protokoll

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].

MedChemExpress (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.

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (287 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Wang Z, et al. The Selectivity and Potency of the New PDE5 Inhibitor TPN729MA. J Sex Med. 2013 Nov;10(11):2790-7. [Content Brief]

[2]. Li BB, et al. Sildenafil potentiates the proliferative effect of porcine pulmonary artery smooth muscle cells induced by serotonin in vitro. Chin Med J (Engl). 2011 Sep;124(17):2733-40. [Content Brief]

[3]. Moretti R, et al. Sildenafil, a cyclic GMP phosphodiesterase inhibitor, induces microglial modulation after focal ischemia in the neonatal mouse brain. J Neuroinflammation. 2016 Apr 28;13(1):95. [Content Brief]

[4]. Korkmaz MF, et al. The Effect of Sildenafil on Recuperation from Sciatic Nerve Injury in Rats. Balkan Med J. 2016 Mar;33(2):204-11. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
H₂O / DMSO	1 mM	1.4999 mL	7.4996 mL	14.9992 mL	37.4981 mL
DMSO	5 mM	0.3000 mL	1.4999 mL	2.9998 mL	7.4996 mL
	10 mM	0.1500 mL	0.7500 mL	1.4999 mL	3.7498 mL
	15 mM	0.1000 mL	0.5000 mL	0.9999 mL	2.4999 mL
	20 mM	0.0750 mL	0.3750 mL	0.7500 mL	1.8749 mL
	25 mM	0.0600 mL	0.3000 mL	0.6000 mL	1.4999 mL
	30 mM	0.0500 mL	0.2500 mL	0.5000 mL	1.2499 mL
	40 mM	0.0375 mL	0.1875 mL	0.3750 mL	0.9375 mL
	50 mM	0.0300 mL	0.1500 mL	0.3000 mL	0.7500 mL
	60 mM	0.0250 mL	0.1250 mL	0.2500 mL	0.6250 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

Keywords

Sildenafil citrate

16 Cited Publications

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Sildenafil citrate

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Publications Citing Use of MedChemExpress (MCE) Sildenafil citrate

Alle Phosphodiesterase (PDE) Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (16)

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Sildenafil citrate Related Classifications

HY-15025A Related Classifications