Tadalafil is a phosphodiesterase type 5 (PDE5) inhibitor. It is sold in liquid form in 30mg per ml vials for research and analytical purposes.
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WHAT IS TADALAFIL?
Tadalafil is a selective inhibitor of the enzyme phosphodiesterase type 5
(PDE5), identified in the smooth muscle cells of various tissues. It increases the perfusion of the lower urinary tract in animal test subjects.
Its empirical formula is C22H19N3 O4, with a molecular weight of 389.4g/mol. It is one of a family of 11 PDEs that degrade cyclic guanosine monophosphate or cyclic adenosine monophosphate.
STRUCTURE OF TADALAFIL
Molecular Formula: C22H19N3 O4
CAS number: 171596-29-5
IUPAC name: 2R,8R)-2-(1,3-benzodioxol-5-yl)-6-methyl-3,6,17-triazatetracyclo[8.7.0.03,8.011,16]heptadeca-1(10),11,13,15-tetraene-4,7-dione
MECHANISM OF ACTION
In animal studies, tadalafil is rapidly absorbed after oral administration with an onset time of 30-120mins post-dose. Only about 36% of the dose is absorbed from an oral solution.
Scientific studies showed this research liquid increases the blood flow throughout some tissues in the body of animal test subjects, such as the genitalia. It increased blood flow to the penis, allowing the test subject to gain and sustain an erection.
Tadalafil’s benefit results from its multifactorial mechanism of action on various organs in animal test subjects. Its effects include the following:
- It improves erectile dysfunction in research subjects sufficient for satisfactory sexual performance.
- It improves depression and cognitive functions in experimental animals with neurodegenerative diseases like Alzheimer’s.
- It prevents the formation of urethral strictures after a urethral injury in animal test subjects.
- It reduces inflammation in endothelial cells of pulmonary arteries in rats lowering the effects of pulmonary arterial hypertension.
- It relaxes vascular smooth muscle and increases blood perfusion and oxygenation of the prostatic tissue of animal test subjects.
- It demonstrates cardio-protection in experimental myocardial infarction.
TADALAFIL SIDE EFFECTS
The side effects of tadalafil seen in animal test subjects are dose-related. The higher the dose, the more severe the side effects. They include:
- Headache that may be severe and requires discontinuation
- Dyspepsia is possibly related to the relaxation of lower esophageal smooth muscle tone
- Back pain and myalgia is a frequent adverse events of unknown origin requiring discontinuation in some subjects
- Rhinitis/ nasal congestion and vasodilation (flushing)
- Gastroesophageal reflux disease (GERD)
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- National Center for Biotechnology Information. PubChem Database. Tadalafil, CID=110635, https://pubchem.ncbi.nlm.nih.gov/compound/Tadalafil (accessed on Dec. 7, 2019)
- Washington SL 3rd, Shindel AW. A once-daily dose of tadalafil for erectile dysfunction: compliance and efficacy. Drug Des Devel Ther. 2010;4:159–171. Published 2010 Sep 7. doi:10.2147/dddt.s9067
- Urios, A., Ordoño, F., García-García, R. et al. Tadalafil Treatment Improves Inflammation, Cognitive Function, And Mismatch Negativity Of Patients With Low Urinary Tract Symptoms And Erectile Dysfunction. Sci Rep 9, 17119 (2019) doi:10.1038/s41598-019-53136-y
- Sesti, C., Florio, V., Johnson, E. et al. The phosphodiesterase-5 inhibitor tadalafil reduces myocardial infarct size. Int J Impot Res 19, 55–61 (2007) doi:10.1038/sj.ijir.3901497
- Seftel, A., Farber, J., Fletcher, J. et al. A three-part study to investigate the incidence and potential etiologies of tadalafil-associated back pain or myalgia. Int J Impot Res 17, 455–461 (2005) doi:10.1038/sj.ijir.3901374
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