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1g |
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2g |
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5g |
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10g |
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Purity: ≥98%
Sildenafil (formerly UK92480; UK-92480; Trade name: Revatio), the free base form of Sildenafil, is a potent and selective inhibitor of phosphodiesterase type 5 (PDE5) with IC50 of 5.22 nM. Sildenafil has been approved for treating erectile dysfunction by increasing blood flow to the penis and is considered to be the best anti-erectile dysfunction (ED) drug.
ln Vitro |
When 1 μM sildenafil was pretreated instead of serotonin stimulation alone, it improved phosphorylation of ERK1/ERK2, increased the percentage of cells in S phase, and promoted cell proliferation (P<0.05). The OD value increased dramatically to 0.33 after pretreatment with 1 μM sildenafil citrate and serotonin stimulation, which was significantly different from serotonin stimulation alone (P<0.05). The phosphorylation of ERK1/ERK2 elicited by serotonin was considerably increased by 1 μM sildenafil [2].
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ln Vivo |
Sildenafil considerably raised ICP and ICP/BP in a canine erection model, but it had no discernible effect on blood pressure when compared to the vehicle [1]. At a dose of 10 mg/kg, sildenafil therapy dramatically decreased the number of TL+- cells. Eight days after pMCAo, sildenafil therapy (0.5 and/or 10 mg/kg dosages) dramatically decreased the amount of microglia/macrophages stained by Iba-1 [3]. According to preclinical animal models, sildenafil can lessen flap necrosis by secreting more growth factors (FGF and VEGF). It has also been demonstrated histologically to be beneficial against cavernous neural structures in rats [4].
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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.
[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. [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. [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 |
Molecular Formula |
C22H30N6O4S
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Molecular Weight |
474.58
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CAS # |
139755-83-2
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Related CAS # |
Sildenafil citrate;171599-83-0;Sildenafil-d3;1126745-90-1;Sildenafil-d8;951385-68-5;Sildenafil Mesylate;1308285-21-3;Sildenafil-d3N-1;1126745-87-6
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SMILES |
CN1CCN(S(=O)(C2=CC=C(OCC)C(C(NC3=C4N(C)N=C3CCC)=NC4=O)=C2)=O)CC1
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InChi Key |
BNRNXUUZRGQAQC-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C22H30N6O4S/c1-5-7-17-19-20(27(4)25-17)22(29)24-21(23-19)16-14-15(8-9-18(16)32-6-2)33(30,31)28-12-10-26(3)11-13-28/h8-9,14H,5-7,10-13H2,1-4H3,(H,23,24,29)
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Chemical Name |
Piperazine, 1-((3-(4,7-dihydro-1-methyl-7-oxo-3-propyl-1H-pyrazolo(4,3-d)pyrimidin-5-yl)-4-ethoxyphenyl)sulfonyl)-4-methyl-
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Synonyms |
UK-92480; UK 92480-10; UK 92480; UK92480 citrate; UK-92,480-10. Trade names: Revatio.
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.27 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.27 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: 30% PEG400+0.5% Tween80+5% propylene glycol:30 mg/mL Solubility in Formulation 4: ≥ 10 mg/mL (21.07 mM) (saturation unknown) in 50% PEG300 50% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
Sildenafil enhances the lethality of [pemetrexed + sorafenib].Oncotarget. 2017 Feb 21; 8(8): 13464–13475. td> |
[Pemetrexed + sorafenib + sildenafil] treatment inactivates cyto-protective STAT3, STAT5 and AKT whilst reducing the expression of cyto-protective proteins MCL-1, BCL-XL and Thioredoxin.Oncotarget. 2017 Feb 21; 8(8): 13464–13475. td> |
Sildenafil-induced PKG signaling plays a greater role in enhancing [pemetrexed + sorafenib] toxicity than nitric oxide synthase signaling.Oncotarget. 2017 Feb 21; 8(8): 13464–13475. td> |