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Raltegravir

Raltegravir Struktur
518048-05-0
CAS-Nr.
518048-05-0
Englisch Name:
Raltegravir
Synonyma:
CS-1889;Raltegravir;Reg column wei;Raltegravir(R&D);Raltegravir, >=99%;Raltegravir USP/EP/BP;Raltegravir(free base);Raltegravir (free base) API;MK-0518 518048-05-0 CAS NO.518048-05-0;Raltegravir-d4Q: What is Raltegravir-d4 Q: What is the CAS Number of Raltegravir-d4
CBNumber:
CB61456530
Summenformel:
C20H21FN6O5
Molgewicht:
444.42
MOL-Datei:
518048-05-0.mol

Raltegravir Eigenschaften

Schmelzpunkt:
216 °C(Solv: isopropanol (67-63-0))
Dichte
1.46±0.1 g/cm3(Predicted)
storage temp. 
-20°C Freezer
L?slichkeit
DMSO (Slightly), Methanol (Very Slightly)
pka
4.50±1.00(Predicted)
Aggregatzustand
Solid
Farbe
White to Light Beige
CAS Datenbank
518048-05-0(CAS DataBase Reference)
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H315 Verursacht Hautreizungen. Hautreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P302+P352, P321,P332+P313, P362
H319 Verursacht schwere Augenreizung. Schwere Augenreizung Kategorie 2 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P280, P305+P351+P338,P337+P313P
Sicherheit
P264 Nach Gebrauch gründlich waschen.
P264 Nach Gebrauch gründlich waschen.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P302+P352 BEI BERüHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckm??ig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.
P305+P351+P338 BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach M?glichkeit entfernen. Weiter spülen.
P332+P313 Bei Hautreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen.
P337+P313 Bei anhaltender Augenreizung: ?rztlichen Rat einholen/?rztliche Hilfe hinzuziehen.

Raltegravir Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Joining maraviroc as a unique approach to battling HIV-1, raltegravir, an inhibitor of HIV-1 integrase, represents the first in its class to be developed and launched as a combination treatment with other antiretroviral agents (NRTIs, NNRTIs, and PIs). HIV-1 integrase is essential for replication of the virus as a virally encoded enzyme that integrates the viral DNA into the genome of the host cell. Inhibition of HIV-1 integrase prevents the two-step process of endonucleolytic removal of the terminal dinucleotide from each 3′end of the viral DNA followed by the covalent integration of the viral DNA, at these modified 3′ends, into the host DNA, thereby representing a viable intervention in the viral life cycle. In vitro, raltegravir inhibited the strand transfer activity of HIV-1 integrase with an IC50 of 2–7nM with > 1,000-fold selectivity over other phosphoryltransferases. In addition, its in vitro IC95 for HIV-1 in 10% fetal bovine serum and 50% human serum was 19 and 33 nM, respectively. Raltegravir was well tolerated with no dose-related toxicities and a safety profile comparable to placebo. The most common clinical adverse events were diarrhea, nausea, vomiting, fatigue, headache, flushing, pruritus, and injection-site reactions.

Verwenden

Raltegravir (MK-0518, Isentress) is a potent integrase (IN) inhibitor for WT and S217Q PFV IN with IC50 of 90 nM and 40 nM, respectively.

Acquired resistance

Several characteristic mutations leading to typical amino acid exchanges have been characterized in cell culture studies and confirmed in clinical trial participants with virological failure while receiving raltegravir in combination with other antiretrovirals. Virological failure has generally been associated with mutations at one of three residues – Y143, Q148 or N155 – usually in combination with at least one other mutation.

Pharmazeutische Anwendungen

Formulated as the potassium salt for oral administration.

Pharmakokinetik

Oral absorption: Not known/available
Cmax 400 mg twice daily: c. 2.17 mg/L
Plasma half-life: c. 9 h
Volume of distribution: Not known/available
Plasma protein binding: c. 83%
Absorption and distribution
It may be administered without regard to food. There are few data regarding its capacity to penetrate into genital secretions or breast milk. A study of 25 HIV-infected individuals receiving raltegravir as a component of combination antiretroviral therapy found that 24 had detectable levels and that 50% of these reached a level exceeding the 95% inhibitory concentration reported to inhibit HIV-1 strains fully susceptible to integrase inhibition.
Metabolism and excretion
It is not a substrate, and does not appear to inhibit or induce the cytochrome P450 enzyme complex. It is primarily metabolized through hepatic glucuronidation mediated by the UGT-1A1 enzyme. It is excreted in the feces (51%) and the urine (32%) as unaltered compound and its glucuronide. There are no recommended dose adjustments for weight, sex and race, or for hepatic or renal insufficiency. The pharmacokinetic handling in children has not been determined.

Clinical Use

Treatment of HIV infection (in combination with other antiretroviral drugs)

Nebenwirkungen

Its toxicity profile to date is remarkably benign. Clinical trial participants experienced similar types and frequencies of adverse events as those receiving placebo. The most frequently reported adverse events were nausea, diarrhea and headache and were mostly mild to moderate in intensity. Myopathy, rhabdomyolysis and elevations of creatinine phosphokinase have been noted in a few trial participants and it should be used cautiously in combination with drugs associated with muscle toxicity.

Raltegravir Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Raltegravir Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 268)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hubei Ipure Biology Co., Ltd
+8613367258412
ada@ipurechemical.com China 10319 58
Hebei Chuanghai Biotechnology Co,.LTD
+86-13131129325
sales1@chuanghaibio.com China 5889 58
BEIJING SJAR TECHNOLOGY DEVELOPMENT CO., LTD.
+86-18600796368 +86-18600796368
sales@sjar-tech.com China 474 58
HEBEI SHENGSUAN CHEMICAL INDUSTRY CO.,LTD
+8615350851019
admin@86-ss.com China 1001 58
Capot Chemical Co.,Ltd.
+86-(0)57185586718 +86-13336195806
sales@capot.com China 29791 60
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21634 55
Shanghai Yingrui Biopharma Co., Ltd.
+86-21-33585366 - 03@
sales03@shyrchem.com CHINA 738 60
career henan chemical co
+86-0371-86658258 +8613203830695
sales@coreychem.com China 29880 58
Jinan Chenghui-Shuangda Chemical Co.,Ltd
+86-531-58897082
ericqiao@jnchsd.com CHINA 158 58
TianYuan Pharmaceutical CO.,LTD
+86-755-23284190 13684996853
sales@tianpharm.com CHINA 304 58

518048-05-0()Verwandte Suche:


  • N-((4-Fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2
  • Raltegravir N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide
  • Raltegravir (free base) API
  • Raltegravir, >=99%
  • N-((4-Fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)carbonyl)amino)ethyl)-6-oxo-4-pyrimidinecarboxamide
  • N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazole-2-carboxamide
  • Raltegravir
  • N-(2-(4-(4-Fluorobenzylcarbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)p
  • Raltegravir(R&D)
  • Raltegravir(free base)
  • N-(4-fluorobenzyl)-5-hydroxy-1-methyl-2-(2-(2-methyl-1,3,4-oxadiazole-5-carboxamido)propan-2-yl)-6-oxo-1,6-dihydropyrimidine-4-carboxamide
  • N-((4-Fluorophenyl)methyl)-1,6-dihydro-5-hydroxy-1-methyl-2-(1-methyl-1-(((5-methyl-1,3,4-oxadiazol-2-yl)carbonyl)am
  • MK-0518 518048-05-0 CAS NO.518048-05-0
  • CS-1889
  • 4-Pyrimidinecarboxamide, N-[(4-fluorophenyl)methyl]-1,6-dihydro-5-hydroxy-1-methyl-2-[1-methyl-1-[[(5-methyl-1,3,4-oxadiazol-2-yl)carbonyl]amino]ethyl]-6-oxo-
  • N-[2-[4-[(4-fluorophenyl)methylcarbamoyl]-5-hydroxy-1-methyl-6-oxopyrimidin-2-yl]propan-2-yl]-5-methyl-1,3,4-oxadiazole-2-carboxamide
  • Reg column wei
  • Raltegravir USP/EP/BP
  • Raltegravir-13Cd3Q: What is Raltegravir-13Cd3 Q: What is the CAS Number of Raltegravir-13Cd3
  • Raltegravir-d4Q: What is Raltegravir-d4 Q: What is the CAS Number of Raltegravir-d4
  • N-[(4-fluorophenyl)methyl]-5-hydroxy-1-methyl-2-{2-[(5-methyl-1,3,4-oxadiazol-2-yl)formamido]propan-2-yl}-6-oxo-1,6-dihydropyrimidine-4-carboxamide
  • N-(2-(4-((4-Fluorobenzyl)carbamoyl)-5-hydroxy-1-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)propan-2-yl)-5-methyl-1,3,4-oxadiazol-2-carboxamide
  • 518048-05-0
  • 518048-05-0;1100750-83-1
  • C20H21FN6O5
  • Inhibitors
  • Isentress
  • API
  • 518048-05-0
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