Homo Sildenafil

  • CAT Number: R008548
  • CAS Number: 642928-07-2
  • Molecular Formula: C23H32N6O4S
  • Molecular Weight: 488.607
  • Purity: ≥95%
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Homo Sildenafil(CAS: 642928-07-2) is a PHOSPHODIESTERASE TYPE-5 INHIBITOR; VASODILATOR AGENT and UROLOGICAL AGENT that is used in the treatment of ERECTILE DYSFUNCTION and PRIMARY PULMONARY HYPERTENSION.

Catalog Number R008548
CAS Number 642928-07-2
Synonyms

5-[2-Ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]phenyl]-1,6-dihydro-1-methyl-3-propyl-7H-pyrazolo[4,3-d]pyrimidin-7-one;

Molecular Formula

C23H32N6O4S

Purity 95%
Storage Store at -20°C
IUPAC Name 5-[2-ethoxy-5-(4-ethylpiperazin-1-yl)sulfonylphenyl]-1-methyl-3-propyl-4H-pyrazolo[4,3-d]pyrimidin-7-one
InChI InChI=1S/C23H32N6O4S/c1-5-8-18-20-21(27(4)26-18)23(30)25-22(24-20)17-15-16(9-10-19(17)33-7-3)34(31,32)29-13-11-28(6-2)12-14-29/h9-10,15H,5-8,11-14H2,1-4H3,(H,24,25,30)
InChIKey MJEXYQIZUOHDGY-UHFFFAOYSA-N
SMILES CCCC1=NN(C2=C1NC(=NC2=O)C3=C(C=CC(=C3)S(=O)(=O)N4CCN(CC4)CC)OCC)C
Reference

[1]. Int J Impot Res. 2019 Mar;31(2):65-70. doi: 10.1038/s41443-018-0099-2. Epub 2019 Mar 5.<br />
Sildenafil/Viagra in the treatment of premature ejaculation.<br />
Krishnappa P(1)(2), Fernandez-Pascual E(3), Carballido J(3), Martinez-Salamanca JI(3).<br />
Author information: (1)Department of Urology, NU Hospitals, Bangalore, India. [email protected]. (2)Department of Urology, Hospital Universitario Puerta de Hierro-Majadahonda, Madrid, Spain. [email protected]. (3)Department of Urology, Hospital Universitario Puerta de Hierro-Majadahonda, Madrid, Spain.<br />
The arrival of Pfizer&#39;s blue pill Sildenafil in 1998 brought a great relief both to patient and physician signalling the start of a great era of medical therapy in sexual medicine. Since then the sexual medicine experts have been prescribing sildenafil in erectile dysfunction with acceptable minor adverse events. But the use of sildenafil in premature ejaculation (PE) is still debated. 2018 being the 20th anniversary of sildenafil, we have compiled interesting facts about the role of sildenafil in PE from various original articles, systematic reviews, meta-analyses, economic brochures and sexual medicine committee guidelines. The major issues in most of these studies were the heterogeneity in the definition of PE and estimating the exact ejaculatory latency time. This perspective article highlights the positive role of sildenafil in the management of PE (even without ED) with acceptable adverse events. Now that we have a standardised definition of PE from International Society of Sexual Medicine (ISSM) and a psychogenic component in PE definition, more randomised placebo-controlled studies are required to further establish its role.<br />
DOI: 10.1038/s41443-018-0099-2 PMID: 30837718 [Indexed for MEDLINE]<br />
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[2]. Int Urol Nephrol. 2017 Oct;49(10):1731-1740. doi: 10.1007/s11255-017-1644-5. Epub 2017 Jul 24.<br />
Direct comparison of tadalafil with sildenafil for the treatment of erectile dysfunction: a systematic review and meta-analysis.<br />
Gong B(1), Ma M(2), Xie W(1), Yang X(1), Huang Y(1), Sun T(3), Luo Y(1), Huang J(1).<br />
Author information: (1)Department of Urology, The First Affiliated Hospital of Nanchang University, Nanchang, 330000, Jiangxi Province, China. (2)Department of Urology, The First Affiliated Hospital of Nanchang University, Nanchang, 330000, Jiangxi Province, China. [email protected]. (3)Department of Urology, The First Affiliated Hospital of Nanchang University, Nanchang, 330000, Jiangxi Province, China. [email protected].<br />
AIMS: Erectile dysfunction (ED) is a major care problem worldwide. Tadalafil and sildenafil are the two most common phosphodiesterase 5 inhibitors used to treat ED. This systematic review and meta-analysis were conducted to directly compare tadalafil with sildenafil for the treatment of ED. METHODS: We designed a strategy for searching the PubMed, Embase, EBSCO, Web of Science and Cochrane library databases; the reference lists of the retrieved studies were also investigated. A literature review was performed to identify all published randomized or non-randomized controlled trials that compared tadalafil with sildenafil for the treatment of ED and to assess the quality of the studies. Two investigators independently and blindly screened the studies for inclusion. The meta-analysis was performed using RevMan 5.0. RESULTS: A total of 16 trials that compared tadalafil with sildenafil for the treatment of ED were included in the meta-analysis. In the meta-analysis, tadalafil and sildenafil appeared to have similar efficacies and overall adverse event rates. However, compared with sildenafil, tadalafil significantly improved psychological outcomes. Furthermore, the patients and their partners preferred tadalafil over sildenafil, and no significant difference was found in the adherence and persistence rates between tadalafil and sildenafil. Additionally, the myalgia and back pain rates were higher and the flushing rate was lower with tadalafil than with sildenafil. CONCLUSION: Tadalafil shares a similar efficacy and safety with sildenafil and significantly improves patients&#39; sexual confidence. Furthermore, patients and their partners prefer tadalafil to sildenafil. Hence, tadalafil may be a better choice for ED treatment.<br />
DOI: 10.1007/s11255-017-1644-5 PMCID: PMC5603624 PMID: 28741090 [Indexed for MEDLINE]<br />
<br />
[3]. Am J Ther. 2019 Jul/Aug;26(4):e520-e526. doi: 10.1097/MJT.0000000000000766.<br />
Sildenafil for Pulmonary Arterial Hypertension.<br />
Bhogal S(1), Khraisha O(1), Al Madani M(1), Treece J(1), Baumrucker SJ(2), Paul TK(1).<br />
Author information: (1)Department of Medicine, Division of Cardiology, East Tennessee State University, Johnson City, TN. (2)Department of Hospice and Palliative Medicine Wellmont Health System, Kingsport, TN.<br />
Pulmonary hypertension is a life-threatening illness with debilitating physical and emotional consequences. The progression of this devastating disease is characterized by a continuous increase in pulmonary vascular resistance, which results in elevated pulmonary artery pressure and leads to right heart failure. Treatment is focused on targeting the underlying complex etiology via the endothelin, prostacyclin, and nitric oxide (NO) pathways. Emergence of new treatments over the past 2 decades has led to improvement in the functional status and time to clinical worsening. Even with recent advances, outcomes remain suboptimal. Phosphodiesterase-5 (PDE-5) inhibitors, such as sildenafil, were approved for treatment of pulmonary arterial hypertension (PAH) by the Food and Drug Administration (FDA) in 2005, which holds promise in improving quality of life and therefore making this class of medications effective palliative therapy agents. In this review, we summarize the emergence of sildenafil as a treatment for PAH and its role as palliative therapy.<br />
DOI: 10.1097/MJT.0000000000000766 PMID: 30946047 [Indexed for MEDLINE]<br />
<br />
[4]. J Pharm Biomed Anal. 2018 Feb 5;149:586-590. doi: 10.1016/j.jpba.2017.11.057. Epub 2017 Nov 27.<br />
New metabolites of hongdenafil, homosildenafil and hydroxyhomosildenafil.<br />
Yeo M(1), Park Y(2), Lee H(2), Choe S(3), Baek SH(4), Kim HK(1), Pyo JS(5).<br />
Author information: (1)College of Pharmacy and Brain Busan 21 program, Kyungsung University, Busan 48434, Republic of Korea. (2)Busan Institute, National Forensic Service, 50 Geumhoro, Mulgeumeup, Yangsan, 50612, Republic of Korea. (3)Department of Drug and toxicology, National Forensic Service, Wonju, 26460, Republic of Korea. (4)College of Pharmacy, Ajou University, Suwon, 16499, Republic of Korea. (5)College of Pharmacy and Brain Busan 21 program, Kyungsung University, Busan 48434, Republic of Korea. Electronic address: [email protected].<br />
Recently, illegal sildenafil analogues have emerged, causing serious social issues. In spite of the importance of sildenafil analogues, their metabolic profiles or clinical effects have not been reported yet. In this study, new metabolites of illegal sildenafil analogues such as hongdenafil, homosildenafil, and hydroxyhomosildenafil were determined using liquid chromatography quadrupole-time of flight mass spectrometry (LC-Q-TOF-MS) and tandem mass spectrometry (LC-Q-TOF-MS/MS). To prepare metabolic samples, in vitro and in vivo studies were performed. For in vivo metabolites analysis, urine and feces samples of rats treated with sildenafil analogues were analyzed. For in vitro metabolites analysis, human liver microsomes incubated with sildenafil analogues were extracted and analyzed. All metabolites were characterized by LC-Q-TOF-MS and LC-Q-TOF-MS/MS. As a result, five, six, and seven metabolites were determined in hongdenafil, homosildenafil, and hydroxyhomosildenafil treated samples, respectively. These results could be applied to forensic science and other analytical fields. Moreover, these newly identified metabolites could be used as fundamental data to determine the side effect and toxicity of illegal sildenafil analogues.<br />
DOI: 10.1016/j.jpba.2017.11.057 PMID: 29197805 [Indexed for MEDLINE]<br />
<br />
[5]. Vet Rec. 2017 Apr 22;180(16):404. doi: 10.1136/vr.103832. Epub 2017 Feb 10.<br />
Sildenafil improves clinical signs and radiographic features in dogs with congenital idiopathic megaoesophagus: a randomised controlled trial.<br />
Quintavalla F(1), Menozzi A(1), Pozzoli C(2), Poli E(2), Donati P(3), Wyler DK(4), Serventi P(1), Bertini S(1).<br />
Author information: (1)Department of Veterinary Science, University of Parma, Parma, Italy. (2)Department of Neuroscience, University of Parma, Parma, Italy. (3)Cerro Maggiore, Milano, Italy. (4)The Animal Medical Hospital and Whitestone Veterinary Care, New York, NY, USA.<br />
We evaluated the efficacy of oral sildenafil citrate in dogs with congenital idiopathic megaoesophagus (CIM). Twenty-one puppies were randomly assigned to two groups (treatment and control). The dogs were given sildenafil oral suspension 1 mg/kg every 12 hours for 14 days or placebo in a masked fashion. Clinical signs (frequency of regurgitation and weight gain) and oesophagrams (relative oesophageal diameter, ROD) were evaluated in order to assess the efficacy of drug treatment, by examiners who were unaware of the study protocol. In addition, a set of in vitro experiments on isolated samples of canine lower oesophageal sphincter (LOS) was performed, and the effects of increasing concentrations of sildenafil on basal tone and electrically-stimulated motility were assessed. Sildenafil administration significantly reduced the number of regurgitation episodes (0.88&plusmn;1.40 v 2.65&plusmn;1.56, P&lt;0.0001) and significantly increased weight gain in the treated dogs compared to controls (79.76&plusmn;28.30 per cent v 53.40&plusmn;19.30 per cent, P=0.034). ROD values, at the end of the treatment period, were significantly decreased in the sildenafil group, compared to pre-treatment values (0.97&plusmn;0.19 v 0.24&plusmn;0.14, P&lt;0.0001), in contrast to control subjects (0.98&plusmn;0.17 v 1.10&plusmn;0.25, P=0.480). In accordance with the in vivo findings, sildenafil dose-dependently reduced basal tone and increased electrically-induced relaxation of dog LOS samples. These results suggest that sildenafil citrate helps ameliorate clinical and radiographic signs in dogs with CIM by reducing LOS tone, and could represent a novel therapeutic tool for the treatment of this disease.<br />
British Veterinary Association.<br />
DOI: 10.1136/vr.103832 PMID: 28188161 [Indexed for MEDLINE]

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