Sildenafil citrate
Based on 16 publication(s) in Google Scholar
Sildenafil citrate is a potent phosphodiesterase type 5 (PDE5) inhibitor with IC50 of 5.22 nM.
For research use only. We do not sell to patients.
- Purity: 99.86%
- CAS No.: 171599-83-0
- Formula: C28H38N6O11S
- Molecular Weight:666.70
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Sildenafil citrate
More- Nature. 2025 Sep;645(8079):244-253. [Abstract]
- Phytomedicine. 2025 Sep 25:148:157334. [Abstract]
- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Phytother Res. 2025 Mar;39(3):1549-1564. [Abstract]
- Br J Pharmacol. 2024 Dec;181(23):4920-4936. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Bioeng Transl Med. 2023 Jul 2;8(5):e10568. [Abstract]
- Int J Mol Sci. 2022 Jun 20;23(12):6860. [Abstract]
- ACS Omega. 2020 Nov 15;5(46):29935-29942. [Abstract]
- Biochim Biophys Acta Mol Basis Dis. 2024 Mar;1870(3):167018. [Abstract]
- Sci Rep. 2020 Oct 2;10(1):16383. [Abstract]
- Saudi Pharm J. 2026 Jun 25;34(3):39. [Abstract]
- J Nat Med. 2025 Sep;79(5):1154-1166. [Abstract]
- Biochem Biophys Res Commun. 2021 Apr 2:547:9-14. [Abstract]
- Physiol Rep. 2023 Jan;11(1):e15549. [Abstract]
- Biomed Chromatogr. 2024 Aug;38(8):e5925. [Abstract]
Customer Validation & Images
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Bio/Physico-chemical Assay
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In Vivo Efficacy Study
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In Vivo Efficacy Study
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Histological Imaging/Staining
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IHC
Biological Activity
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PDE5 |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 171599-83-0
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Appearance Solid
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Molecular Weight 666.70
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Formula C28H38N6O11S
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Color White to off-white
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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
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Synonyms
UK-92480 citrate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
Publications (16)
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Journal Impact Factor
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Most Recent
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Nature
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).
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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.
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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).
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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
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.
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Biomed Chromatogr
A novel standard-free detection of adulteration method for sildenafil derivatives in dietary supplements. [Abstract]2024 Aug;38(8):e5925. PMID: 38837800
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 2 years; -20°C, 1 year (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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.
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.
Purity & Documentation
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Data Sheet (287 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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.
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