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NELFINAVIR

NELFINAVIR Struktur
159989-64-7
CAS-Nr.
159989-64-7
Englisch Name:
NELFINAVIR
Synonyma:
AG 1341;nefinavir;NELFINAVIR;NELFINAVIR-12;Nelfinavir D5;8a-beta))-a-bet;NELFINAVIR iMpurity;NELFINAVIR USP/EP/BP;Nelfinavir (AG-1341);Nelfinavir Regeoisomer
CBNumber:
CB8213806
Summenformel:
C32H45N3O4S
Molgewicht:
567.78
MOL-Datei:
159989-64-7.mol

NELFINAVIR Eigenschaften

Schmelzpunkt:
185-186 °C
Siedepunkt:
786.8±60.0 °C(Predicted)
alpha 
D -119.23° (c = 0.26 in methanol)
Dichte
1.22±0.1 g/cm3(Predicted)
storage temp. 
under inert gas (nitrogen or Argon) at 2–8 °C
L?slichkeit
≥ 20.45mg/mL in Ethanol
Aggregatzustand
Powder
pka
pKa1 6.0; pKa2 11.06(at 25℃)
Farbe
White to off-white
Wasserl?slichkeit
7g/L(temperature not stated)
Sicherheit
  • Risiko- und Sicherheitserkl?rung
  • Gefahreninformationscode (GHS)
Toxizit?t rat,LD,oral,> 5gm/kg (5000mg/kg),Toxicologist. Vol. 42, Pg. 55, 1998.
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Warnung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H302 Gesundheitssch?dlich bei Verschlucken. Akute Toxizit?t oral Kategorie 4 Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P264, P270, P301+P312, P330, P501
Sicherheit
P264 Nach Gebrauch gründlich waschen.
P264 Nach Gebrauch gründlich waschen.
P270 Bei Gebrauch nicht essen, trinken oder rauchen.
P501 Inhalt/Beh?lter ... (Entsorgungsvorschriften vom Hersteller anzugeben) zuführen.

NELFINAVIR Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden

Antiviral.

Definition

ChEBI: An aryl sulfide that is used (as its mesylate salt) for treatment of HIV and also exhibits some anticancer properties.

Indications

Nelfinavir (Viracept) is probably the most commonly used protease inhibitor because of its low incidence of serious adverse effects. Its most common side effects are diarrhea and flatulence; these may resolve with continued use. In addition to the drugs contraindicated for use with all protease inhibitors, amiodarone, rifampin, and quinidine are contraindicated in patients taking nelfinavir.

Antimicrobial activity

Nelfinavir inhibits HIV-1 and HIV-2 proteases. Bioavailability is affected to only a limited degree by combination with lowdose ritonavir.

Acquired resistance

Resistance is most frequently selected through a D30N mutation in the HIV protease. An L90M mutation also confers resistance.

Pharmazeutische Anwendungen

A synthetic chemical formulated as the mesylate for oral administration.

Pharmakokinetik

Oral absorption: c. 70–80% (with food)
Cmax 750 mg thrice daily: c. 3–4 mg/L
1250 mg twice daily: c. 4 mg/L
Cmin 750 mg thrice daily: c. 1–3 mg/L
1250 mg twice daily: c. 0.7–2.2 mg/L
Plasma half-life: c. 3.5 h
Volume of distribution: c. 2–7 L/kg
Plasma protein binding: >98%
Absorption and distribution
Food improves the bioavailability and the drug should be administered with a light meal. The semen:plasma ratio is 0.07. It is distributed into breast milk.
Metabolism and excretion
One major and several minor oxidative metabolites are found in plasma. Most of an oral dose is recovered in feces as unchanged drug (22%) and metabolites (78%). The remainder is recovered in urine, mainly unchanged.
An increase in the area under the time–concentration curve (AUC) has been observed in patients with hepatic impairment, but specific dose recommendations have not been made.

Clinical Use

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

Nebenwirkungen

The most common adverse effect is diarrhea of mild to moderate severity. Other side effects include nausea, fatigue, vomiting and headache. It is associated with less dyslipidemia in comparison with ritonavir-boosted protease inhibitors.

Stoffwechsel

Following oral administration, nelfinavir peak levels in plasma ranged from 0.34 mg/mL (10 mg/kg in the dog) to 1.7 mg/mL (50 mg/kg in the rat). In the dog, nelfinavir was slowly absorbed, and bioavailability was 47%. The drug appeared to be metabolized in the liver, and the major excretory route was in feces.

NELFINAVIR Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


NELFINAVIR Anbieter Lieferant Produzent Hersteller Vertrieb H?ndler.

Global( 104)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49374 58
TargetMol Chemicals Inc.
+1-781-999-5354 +1-00000000000
marketing@targetmol.com United States 31991 58
Career Henan Chemica Co
+86-0371-86658258 +8613203830695
laboratory@coreychem.com China 30241 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD
86-571-88216897,88216896 13588875226
sales@hzclap.com CHINA 6312 58
Dideu Industries Group Limited
+86-29-89586680 +86-15129568250
1026@dideu.com China 23325 58
AFINE CHEMICALS LIMITED
+86-0571-85134551
sales@afinechem.com China 15361 58
Hefei Hirisun Pharmatech Co., Ltd
+8615056975894
shawn@hirisunpharm.com CHINA 9911 58
Sinoway Industrial co., ltd.
0592-5800732; +8613806035118
xie@china-sinoway.com China 988 58
Nextpeptide Inc
+86-0571-81612335 +8613336028439
sales@nextpeptide.com China 19908 58
InvivoChem
+1-708-310-1919 +1-13798911105
sales@invivochem.cn United States 6391 58

159989-64-7()Verwandte Suche:


  • 3-isoquinolinecarboxamide,n-(1,1-dimethylethyl)decahydro-2-(2-hydroxy-3-((3-hy
  • 8a-beta))-a-bet
  • nefinavir
  • NELFINAVIR
  • (3S,4aS,8aS)-N-(1,1-Dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-3-isoquinolinecarboxamide
  • Nelfinavir & Nelfinavir Mesylate
  • AG 1341
  • NELFINAVIR-12
  • Nelfinavir Regeoisomer
  • N-tert-butyl-2-[2-hydroxy-3-[[(3-hydroxy-2-methylphenyl)-oxomethyl]amino]-4-(phenylthio)butyl]-3,4,4a,5,6,7,8,8a-octahydro-1H-isoquinoline-3-carboxamide
  • AG 1341; AG-1341; AG1341
  • 3-Isoquinolinecarboxamide, N-(1,1-dimethylethyl)decahydro-2-[(2R,3R)-2-hydroxy-3-[(3-hydroxy-2-methylbenzoyl)amino]-4-(phenylthio)butyl]-, (3S,4aS,8aS)-
  • NELFINAVIR USP/EP/BP
  • (3S,4aS,8aS)-N-(tert-Butyl)-2-((2R,3R)-2-hydroxy-3-(3-hydroxy-2-methylbenzamido)-4-(phenylthio)butyl)decahydroisoquinoline-3-carboxamide
  • Nelfinavir (AG-1341)
  • Nelfinavir D5
  • NELFINAVIR iMpurity
  • 159989-64-7
  • C32H45N3O4SCH4O3S
  • C32H45N3O4SC32H45N3O4SCH3SO3H
  • peptides
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