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ChemicalBook > Produktkatalog >Aktive pharmazeutische Wirkstoffe (APIs) >Hormone und das endokrine System >Arzneimittel gegen erektile Dysfunktion >Tadalafil

Tadalafil Produkt Beschreibung

CAS-Nr.171596-29-5
Bezeichnung:
Englisch Name:Tadalafil
Synonyma:
IC 351;CIALIS;Calais;Adcirca;ICOS 351;TADALAFIL;GF 196960;UK 336017;tadanafei;Tadanafil
CBNumber:CB2236841
Summenformel:C22H19N3O4
Molgewicht:389.4
MOL-Datei:171596-29-5.mol
Tadalafil physikalisch-chemischer Eigenschaften
Schmelzpunkt:: 298-300°C
alpha : D20 +71.0°
Flammpunkt:: 2℃
storage temp. : Hygroscopic, -20?C Freezer, Under Inert Atmosphere
Löslichkeit: DMSO: soluble20mg/mL, clear
Aggregatzustand: powder
Farbe: white to beige
Optische Aktivität: [α]/D +68 to +78°, c = 1 in chloroform-d
InChIKey: WOXKDUGGOYFFRN-IIBYNOLFSA-N
CAS Datenbank: 171596-29-5(CAS DataBase Reference)
Sicherheit
Kennzeichnung gefährlicher: F,Xn
R-Sätze:: 11-20/21/22-36
S-Sätze:: 16-36/37
RIDADR : UN 1648 3 / PGII
WGK Germany : 2
RTECS-Nr.: UQ4431050
Giftige Stoffe Daten: 171596-29-5(Hazardous Substances Data)

Tadalafil Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Tadalafil (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.
Chemische Eigenschaften
White to Off-White Cyrstalline Solid
Originator
Lilly/ICOS (US)
Verwenden
analgesic, norepinephrine uptake blocker, mu-opiod receptor agonist
Definition
ChEBI: 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
Trademarks
Cialis (Lilly).
Allgemeine Beschreibung
Tadalafil, (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.
Clinical Use
Tadalafil 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.
Einzelnachweise
https://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 Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
Tadalafil Anbieter Lieferant Produzent Hersteller Vertrieb Händler.      Global( 388)Lieferanten     
Firmenname Telefon Fax E-Mail Land Produktkatalog Edge Rate
Hubei XinRunde Chemical Co., Ltd.
+8615102730682; +8618874586545
02783214688bruce@xrdchem.cn CHINA 541 55
Jinan Tenglong Chemical Co.,Ltd
Whatsapp:+8615563263311 Skype:live:smions7080
smions7080@gmail.com CHINA 43 58
Jinan Jianfeng Chemical Co., Ltd
15562555968
info@pharmachemm.com CHINA 294 58
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925Abel@chembj.com CHINA 3203 55
Hebei Guanlang Biotechnology Co., Ltd.
+86-0311-66562153 whatsapp +8615203118427
+86-0311-66562153sales@crovellbio.com CHINA 407 50
Hebei Minshang Biotechnology Co., Ltd
+86-13230167943
cathy@hbminshang.com CHINA 279 58
Kono Chem Co., Ltd
+86-132 8924 6953
info@konochemical.com CHINA 2144 58
Hebei Huanhao Biotechnology Co., Ltd.
86-0311-83975816 whatsapp +8618034554576
86-0311-83975816grace@hbhuanhao.com CHINA 701 58
Shaanxi Yikanglong Biotechnology Co., Ltd.
17791478691
yklbiotech@163.com CHINA 297 58
Hebei Jimi Trading Co., Ltd.
+86 017772612259 +86 319 5273535
admin@hebeijimi.com CHINA 317 58
 
171596-29-5(Tadalafil)Verwandte Suche:
2-Methyl-pyrazin Natriumhydrogensulfid le, Pflanzen-, hydriert Methylsalicylat Kresoxim-methyl Methyl Methylacetat vardenafil Cialis 11β,17,21-Trihydroxypregn-4-en-3,20-dion-17-butyrat Sildenafil Danazol Natriumhydrid Methyl-4-hydroxybenzoat Hydrocortison Thiophanat-methyl Kaliumhydrid Bensulfuron methyl
TADALAFIL CIALIS IC 351 (6r,12ar)-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 TADALAFIL(CIALIS) Taladafil (cialis) Cialis/taladafil (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 (6r,12ar)-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 (6R,12AR)-6-(benzo[d][1,3]dioxol-5-yl)-2-m Tadanafil/Cialis Natural Sex Steroid Hormones Powder Purity 99.5% Cialis ,98% Pyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione, 6-(1,3-benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-, (6R,12aR)- Africa and Ghana tadalafil powder extract (6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2,3,6,7,12,12a-hexahydro-2-methyl-pyrazino[1',2':1,6]pyridol[3,4-b]indole-1,4-dione 6-Benzo[1,3]dioxol-5-yl-2-Methyl-2,3,6,7,12,12a-hexahydro-pyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4-dione (6R,12aR)-6-(Benzo[d][1,3]dioxol-5-yl)-2-Methyl-2,3,12,12a-tetrahydropyrazino[1',2':1,6]pyrido[3,4-b]indole-1,4(6H,7H)-dione (2R,8R)-2-(2H-1,3-benzodioxol-5-yl)-6-Methyl-3,6,17-triazatetracyclo[8.7.0.0^{3,8}.0^{11,16}]heptadeca-1(10),11(16),12,14-tetraene-4,7-dione Tadalafil Citrate(Cialis) Calais Adcirca Tadalafil (Cliais) hanyuanjian tadanafei - 171596-29-5 171595-29-5 171596-29-4 171596-29-6 171596-21-9 C22H19N3O4 Cialis(IC351) Tadanafil TADALAFIL 99 % TADALAFIL (CIALIS,USP) CIALIS/TADALAFIL Tadalafei Tadalafil WS Cialis (6R,12aR)-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 Tadalafil solution Tadalafil (200 mg) Yang also base Cialis solution,1000ppm Huanyang Base Calais BPC tadinafei Cialis (Taffrail) (6R,12aR)-6-(1,3-Benzodioxol-5-yl)-2-methyl-2,3,6,7,12,12a-hexahydro pyrazino [1′,2′:1,6]-pyrido[3,4-b] indole-1,4-dione Tacrolimus,Tadalafil, Cialis CAS NO. 171596-29-5 Tadalafil / Tadalafil Cialis/tadilafil Raw Tadalafil Cialis Powder Legal Oral Steroids CAS 171596-29-5 For Erectile Dysfunction Hot sale Tadalafil CAS NO.171596-29-5 CAS NO.171596-29-5 Tadalafilyanshengwu
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