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Tadalafil

Cialis is tadalafil, is an orally administrated drug developed by the pharmaceutical company Eli Lily for treatment of male erectile dysfunction disease. It belongs to the second generation of phosphodiesterase type 5 inhibitors. Study has shown that compared with sildenafil, the onset rate of Cialis is very rapid with about 15 ~ 20 min for onset and with long-term effects up to 36h.
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  • Tadalafil
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  • 2020-10-20
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  • 2020-10-12
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Tadalafil Basic information
Indications and uses Clinical Research Side effects Warnings and precautions
Product Name:Tadalafil
Synonyms:TADALAFIL;CIALIS;IC 351;(6R,12AR)-6-(benzo[d][1,3]dioxol-5-yl)-2-methyl-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido;GF 196960;ICOS 351;Tildenafil;UK 336017
CAS:171596-29-5
MF:C22H19N3O4
MW:389.4
EINECS:687-782-2
Product Categories:11;Steroid and Hormone;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals;API's;NUCYNTA;API;Tadalafil;Inhibitor;Pyridines ,Halogenated Heterocycles;Active Pharmaceutical Ingredients;Cnbio;Erectile Dysfunction
Mol File:171596-29-5.mol
Tadalafil Structure
Tadalafil Chemical Properties
Melting point 298-300°C
alpha D20 +71.0°
Boiling point 679.1±55.0 °C(Predicted)
density 1.51±0.1 g/cm3(Predicted)
Fp 2℃
storage temp. Hygroscopic, -20?C Freezer, Under Inert Atmosphere
solubility DMSO: soluble20mg/mL, clear
pka16.68±0.40(Predicted)
form powder
color white to beige
optical activity[α]/D +68 to +78°, c = 1 in chloroform-d
InChIKeyWOXKDUGGOYFFRN-IIBYNOLFSA-N
CAS DataBase Reference171596-29-5(CAS DataBase Reference)
Safety Information
Hazard Codes F,Xn
Risk Statements 11-20/21/22-36
Safety Statements 16-36/37
WGK Germany 3
RTECS UQ4431050
HS Code 2934990002
Hazardous Substances Data171596-29-5(Hazardous Substances Data)
MSDS Information
Tadalafil Usage And Synthesis
Indications and usesCialis (or Tadalafil) was developed by American pharmaceutical company Lilly. It is used to treat erectile dysfunction and belongs to a second generation of PDE5 inhibitors. Studies show that Cialis works very quickly, taking effect in around 15-20 minutes, and has a prolonged effect that can last for up to 36 hours. T1/2 is 17.5h.
Clinical ResearchIn a study of 348 cases of mild to severe erectile dysfunction, patients were randomly given 20mg of Cialis or a placebo. Results showed that in comparison to the placebo group, patients who took Cialis experienced improved intercourse success in the 24-36 hours following medication, with many patients achieving successful sexual intercourse twice in 36 hours. Side effect rate and severity were also no different from those of the placebo group. Over 5% of patients in the Cialis group experienced headaches and indigestion.
Side effectsNo severe negative reactions. No perceived facial flushing or sight abnormalities following medication. Rare cases of headache and indigestion.
Warnings and precautionsPatients currently taking nitrates, experiencing angina pectoris, suffering from heart disease, patients who have unregulated hypertension or hypotension, or patients who have had a stroke in the past 6 months should not take Cialis.
DescriptionTadalafil (market name “Cialis” or “Adcirca”) is a kind of PDE5 inhibitor used for the treatment of erectile dysfunction, benign prostatic hypertrophy and pulmonary arterial hypertension. The effect of Tadalafil is relaxing the blood vessels muscles and increasing the blood flow into the corpus cavernosum. The mechanism of action of tadalafil is through inhibiting the activity of the cGMP specific phosphodiesterase type 5 (PDE5). PDE5 degrades cGMP in the corpus cavernosum located around the penis. Therefore, tadalafi leads to the increased concentration of cGMP which further causes the smooth muscle relaxation and increased blood flow into the corpus cavernosum. Some clinical studies also implied that tadalafil could improve endothelia function in men with increased cardiovascular risk and lower the urinary tract symptoms secondary to benign prostatic hyperplasia.
Chemical PropertiesWhite to Off-White Cyrstalline Solid
OriginatorLilly/ICOS (US)
Usesanalgesic, norepinephrine uptake blocker, mu-opiod receptor agonist
DefinitionChEBI: A pyrazinopyridoindole that is 2,3,6,7,12,12a-hexahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione substituted at position 2 by a methyl group and at position 6 by a 1,3-benzodioxol-5-yl group (the 6R,12aR
Brand nameCialis (Lilly).
General DescriptionTadalafil, (6R-trans)-6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-pyrazino[1', 2' :1,6]pyrido[3,4-b]indole-1,4-dione (Cialis), is a potent PDE5 inhibitor.It received FDA approval for the treatment of erectiledysfunction in December 2003. Because of its half-life of17.5 hours, it is marketed as a 36-hour treatment. Tadalafil ispredominantly metabolized by hepatic enzymes, includingCYP3A4. The concomitant use of CYP3A4 inhibitors suchas ritonavir, indinavir, ketoconazole, as well as moderateCYP3A inhibitors such as erythromycin have been shown toresult in significant increases in tadalafil plasma levels.Much like sildenafil, tadalafil is under clinical investigationfor managing PAH.
Mechanism of actionTadalafil was the last agent to be released and can be taken on a full stomach without slowing the onset. It has a much longer duration of action, lasting up to 48 hours, compared with sildenafil and vardenafil, which last for approximately 4 hours. The longer half-life of tadalafil results in a lengthened period of responsiveness as compared to sildenafil and vardenafil. This longer therapeutic window requires fewer time constraints for the effectiveness of tadalafil and has been interpreted as being advantageous through providing the option for more spontaneous sexual activity. Because of its long half-life, however, tadalafil, has been detected in plasma even 5 days after oral administration. This suggests the possibility of accumulation if taken regularly and in short intervals, which may result in an increased risk of side effects with the excessive use of this PDE5 inhibitor. The 3,4-methylenedioxy substitution on the phenyl ring was significant for increasing its potency as PDE5 inhibitor. Optimization of the chain on the piperazinedione ring resulted in no significant change in IC50s. Tadalafil is a highly potent PDE5 inhibitor (IC50, 5 nM), with high selectivity for PDE5 versus PDE1 through PDE4. The PDE5/PDE6 selectivity ratio is 85.
PharmacokineticsTadalafil is different in structure from both sildenafil and vardenafil. It is rapidly absorbed and peaks in concentration (378 μg/L after a 20-mg dose) after 2 hours, displaying a long half-life of 17.5 hours. It also is metabolized by the liver (CYP3A4). Notably, its pharmacokinetics is not clinically influenced by alcohol or food intake or by factors such as diabetes or impaired hepatic or renal function.
Clinical UseTadalafil is one of the two new PDE5 inhibitors launched for the oral treatment of male erectile dysfunction. Tadalafil is a b-carboline derivative and it is structurally distinct from vardenafil (Levitraw) and sildenafil (Viagraw), both of which are PDE5 inhibitors based on a fused pyrimidine core structure. Tadalafil is synthesized in three steps starting from D-tryptophan methyl ester, by first condensing with piperonal in a Pictet-Spengler cyclization reaction to form the tetrahydro-β-carboline derivative, which is followed by chloroacetylation of the piperidine ring nitrogen and cyclization with methylamine. Tadalafil is a potent and highly selective inhibitor of PDE5 (IC50=1 nm). It shows >10,000-fold selectivity for PDE5 versus PDE1, 2, 3, 4, 7, 8 and 9, and >700-fold selectivity versus PDE6. Typically administered at 10 and 20 mg doses, tadalafil is rapidly absorbed and has a tmax of 2 h, which is slightly longer than those of sildenafil (1 h) and vardenafil (0.75 h). Clinically, all of these agents appear to have efficacy for many men within 30–60 min. However, tadalafil distinguishes itself from other PDE5 inhibitors in terms of significantly longer duration of action. The half-life of tadalafil dosed at 20 mg is 17.5 h as compared with 3.8 h for sildenafil (100 mg) and 4.7 h for vardenafil (20 mg). In clinical studies, significant rates of response were reported up to 36 h following drug ingestion. Tadalafil is predominantly metabolized in the liver by CYP3A4 to entities that are not active against PDE5 and excreted mainly as metabolites in the feces and the urine. The pharmacokinetics of tadalafil are unaffected by factors such as intake of food and alcohol, age, the presence of diabetes, and mild or moderate hepatic insufficiency. The most common drug-related adverse events are headache, back pain, dyspepsia, and myalgia. At 10 and 20 mg doses, Tadalafil does not have a significant effect on blood pressure and heart rate and does not result in increased instances of myocardial infarction. Rare reports of prolonged erections greater than 4 h and priapism have been noted with the use of tadalafil. Priapism, if not treated properly, can result in irreversible damage to the erectile tissue. Patients who have an erection lasting greater than 4 h are advised to seek emergency medical attention. Tadalafil has a modest synergistic effect on the nitrate-induced reduction in blood pressure and, as with sildenafil and vardenafil, it is contraindicated for use in patients on nitrate therapy. In diabetic patients, improvement of erectile function by tadalafil is irrespective of the type of diabetes and the type of diabetic therapy.
Side effectsAdverse effects related to oral therapy for erectile function are primarily concerned with adverse cardiovascular effects, because PDE5 inhibitors promote vasodilation and, therefore, have an inherent potential to cause hypotension. This is a particular concern for elderly patients with a preexisting condition.
Referenceshttps://www.drugs.com/tadalafil.html
https://www.drugbank.ca/drugs/DB00820
Roehrborn, C. G., et al. "Tadalafil administered once daily for lower urinary tract symptoms secondary to benign prostatic hyperplasia: a dose finding study." Journal of Urology 180.4(2008):1228.
Rosano, Giuseppe M. C., et al. "Chronic Treatment with Tadalafil Improves Endothelial Function in Men with Increased Cardiovascular Risk." European Urology 47.2(2005):214-222.
Tadalafil Preparation Products And Raw materials
Tag:Tadalafil(171596-29-5) Related Product Information
2-Methylpyrazine Sodium hydrosulfide Hydrogenated Vegetable Oil Methyl salicylate Kresoxim-methyl Methyl Methyl acetate vardenafil Tadalafil Hydrocortisone-17-butyrate Sildenafil Danazol Sodium hydride Methylparaben Hydrocortisone Thiophanate-methyl Potassium hydride Bensulfuron methyl