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Purity: ≥98%
Sildenafil Citrate (formerly also known as UK-92480 citrate; Trade names Revatio;among others), the citrate form of Sildenafil, is a potent and selective inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5) with IC50 of 5.22 nM. Sildenafil Citrate is a well-tolerated and highly effective treatment for erectile dysfunction and pulmonary arterial hypertension.
| ln Vitro |
When compared to serotonin stimulation alone, pretreatment with 1 μM sildenafil citrate enhances phosphorylation of ERK1/ERK2, increases the proportion of cells in S phase, and promotes cell proliferation (P<0.05). An abrupt rise in the optical density (OD value) to 0.33 occurs after pretreatment with 1 μM sildenafil citrate and serotonin stimulation. This is significantly different from serotonin stimulation alone (P<0.05). It is evident that 1 μM sildenafil increases the upregulation of serotonin-induced ERK1/ERK2 phosphorylation[2].
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| ln Vivo |
Sildenafil citrate dramatically raises ICP and ICP/BP in the canine erection model, but has no discernible effect on blood pressure when compared to the vehicle[1]. Treatment with sildenafil dramatically reduces TL+-cell counts at 10 mg/kg, but not at 0.5 mg/kg. At this stage, animals treated with PBS have cells positive for the M1-like marker COX-2+ in the ischemic core, while animals treated with 10 mg/kg of sildenafil (but not 0.5 mg/kg) have most of these cells in the penumbra. In contrast, sildenafil therapy (0.5 or 10 mg/kg dosage) significantly reduces the amount of microglia/macrophages stained by Iba-1 eight days after pMCAo[3]. By boosting the release of growth factors (FGF and VEGF), sildenafil citrate has been proven to reduce flap necrosis in preclinical animal models. It has also been demonstrated histologically to be efficacious in rat cavernous nerve architecture[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.C6H8O7
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|---|---|
| Molecular Weight |
666.7
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| CAS # |
171599-83-0
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| Related CAS # |
Sildenafil;139755-83-2;Sildenafil citrate-d8;1215071-03-6
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| SMILES |
CCCC1=NN(C2=C1NC(=NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)C)OCC)C.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
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| InChi Key |
DEIYFTQMQPDXOT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H30N6O4S.C6H8O7/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;7-3(8)1-6(13,5(11)12)2-4(9)10/h8-9,14H,5-7,10-13H2,1-4H3,(H,23,24,29);13H,1-2H2,(H,7,8)(H,9,10)(H,11,12)
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| Chemical Name |
5-(2-ethoxy-5-((4-methylpiperazin-1-yl)sulfonyl)phenyl)-1-methyl-3-propyl-1,4-dihydro-7H-pyrazolo[4,3-d]pyrimidin-7-one 2-hydroxypropane-1,2,3-tricarboxylate
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| Synonyms |
UK-92480 citrate; UK 92480 citrate; Sildenafil Citrate; UK92480 citrate; UK 92480-10; 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) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.4999 mL | 7.4996 mL | 14.9993 mL | |
| 5 mM | 0.3000 mL | 1.4999 mL | 2.9999 mL | |
| 10 mM | 0.1500 mL | 0.7500 mL | 1.4999 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.
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