Abacavir

Abacavir Struktur
136470-78-5
CAS-Nr.
136470-78-5
Englisch Name:
Abacavir
Synonyma:
CS-107;1592u89;Abacavir;Abacavir >Abacavir(base);Abacavir Tablet;Abacavir, ≥ 98.0%;Abacavir USP/EP/BP;Abacavir Standard;Abacavir (see A105000)
CBNumber:
CB5698138
Summenformel:
C14H18N6O
Molgewicht:
286.33
MOL-Datei:
136470-78-5.mol

Abacavir Eigenschaften

Schmelzpunkt:
165°
alpha 
D20 -59.7°; 43620 -127.8°; 36520 -218.1° (c = 0.15 in methanol)
Siedepunkt:
636.0±65.0 °C(Predicted)
Dichte
1.70±0.1 g/cm3(Predicted)
storage temp. 
Sealed in dry,2-8°C
Löslichkeit
DMSO (Slightly, Heated), Methanol (Slightly)
pka
5.01(at 25℃)
Aggregatzustand
Solid
Farbe
Off-White to Pale Beige
Merck 
14,1
BCS Class
3
CAS Datenbank
136470-78-5(CAS DataBase Reference)
EPA chemische Informationen
2-Cyclopentene-1-methanol, 4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-, (1S,4R)- (136470-78-5)
Sicherheit
  • Risiko- und Sicherheitserklärung
  • Gefahreninformationscode (GHS)
RTECS-Nr. GY5979200
HS Code  2933.99.7500
Bildanzeige (GHS) GHS hazard pictograms
Alarmwort Achtung
Gefahrenhinweise
Code Gefahrenhinweise Gefahrenklasse Abteilung Alarmwort Symbol P-Code
H317 Kann allergische Hautreaktionen verursachen. Sensibilisierung der Haut Kategorie 1A Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" /> P261, P272, P280, P302+P352,P333+P313, P321, P363, P501
H334 Kann bei Einatmen Allergie, asthmaartige Symptome oder Atembeschwerden verursachen. Sensibilisierung der Atemwege Kategorie 1 Achtung GHS hazard pictogramssrc="/GHS08.jpg" width="20" height="20" /> P261, P285, P304+P341, P342+P311,P501
H341 Kann vermutlich genetische Defekte verursachen. Keimzellmutagenität Kategorie 2 Warnung P201,P202, P281, P308+P313, P405,P501
H361 Kann vermutlich die Fruchtbarkeit beeinträchtigen oder das Kind im Mutterleib schädigen. Reproduktionstoxizität Kategorie 2 Warnung P201, P202, P281, P308+P313, P405,P501
Sicherheit
P201 Vor Gebrauch besondere Anweisungen einholen.
P202 Vor Gebrauch alle Sicherheitshinweise lesen und verstehen.
P261 Einatmen von Staub vermeiden.
P272 Kontaminierte Arbeitskleidung nicht außerhalb des Arbeitsplatzes tragen.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.
P284 Atemschutz tragen.
P302+P352 BEI BERÜHRUNG MIT DER HAUT: Mit viel Wasser/... (Hersteller kann, falls zweckmäßig, ein Reinigungsmittel angeben oder, wenn Wasser eindeutig ungeeignet ist, ein alternatives Mittel empfehlen) waschen.
P308+P313 BEI Exposition oder falls betroffen: Ärztlichen Rat einholen/ärztliche Hilfe hinzuziehen.

Abacavir Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

The drug is extensively metabolized via stepwise phosphorylation to 5′-mono-, di-, and triphosphate. Abacavir is well absorbed (>75%) and penetrates the CNS. The drug can be taken without regard to meals. The drug does not show any clinically significant drug–drug interactions. Abacavir has been reported to produce life-threatening hypersensitivity reactions. The major use of abacavir appears to be in combination with other nucleoside RT inhibitors. A fixed-combination product has recently been approved by the U.S. FDA consisting of 300 mg of ABC, 150 mg of 3TC, and 300 mg of ZDV (Trizivar). The combination has been shown to be superior to other combinations in reducing viral load as well as to show improvement in CD4 cell count.

Verwenden

Abacavir is a commonly used nucleoside analogue with potent antiviral activity against HIV-1. - See more at: http://www.selleckchem.com/products/abacavir-sulfate.html#sthash.lApvcTNO.dpuf

Indications

Abacavir (Ziagen) is a guanosine nucleoside analogue indicated for the therapy of HIV-1 infection in adults and children. It is used as part of a multidrug regimen and is available in a fixed-dose combination with zidovudine and lamivudine (Trizivir). It is also used for postexposure HIV infection prophylaxis.

Antimicrobial activity

Abacavir has activity against HIV-1, HIV-2 and human T-cell lymphotrophic virus type-1 (HTLV-1).

Acquired resistance

Resistance is associated with specific changes in codons 184 with 65, 74 or 115 in the HIV reverse transcriptase codon region.

Allgemeine Beschreibung

Abacavir is a nucleoside reverse transcriptase inhibitorNRTI that has been approved for use in combination therapiesfor the treatment of HIV and AIDS. Once in the tissues,it is metabolized by stepwise phosphorylation to themonophosphate, diphosphate, and triphosphate. Abacavir ishighly bioavailable (>75%) and is effective by the oralroute. It penetrates the blood-brain barrier efficiently.Abacavir has been reported to produce life-threatening hypersensitivityreactions in some patients.

Pharmazeutische Anwendungen

A synthetic analog of guanine formulated for oral use.

Pharmakokinetik

Oral absorption: 83%
Cmax 300 mg oral, twice daily: 3.0 ± 0.89 mg/L
600 mg once daily: 4.26 mg/L
Plasma half-life: 1.5 h
Volume of distribution: 0.8 L/kg
Plasma protein binding: c. 49%
Absorption
After oral administration abacavir sulfate undergoes rapid and extensive absorption unaffected by food.
Distribution
It penetrates well into the cerebrospinal fluid (CSF) and is an NRTI of choice if this characteristic is thought desirable. Good penetration into the male genital tract has been observed. The drug is secreted into human breast milk.
Metabolism
It is primarily metabolized in the liver, mainly by alcohol dehydrogenase and glucuronidation.
Excretion
Around 83% of the dose is eliminated in the urine, <2% as unchanged drug; the remainder is excreted in the feces. Dose adjustment is unnecessary in renal impairment. It can be used in moderate hepatic impairment, but is contraindicated if dysfunction is severe.

Clinical Use

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

Nebenwirkungen

Life-threatening hypersensitivity reactions occur in 5–8% of all individuals, necessitating discontinuation of the drug. Typically patients present within the first 6 weeks of starting treatment with fever, rash or other symptoms that worsen in severity with continued drug exposure. Hypersensitivity is associated with carriage of the major histocompatibility complex class I allele HLA-B57*01 and screening for this allele can significantly reduce the incidence of this effect.
Current or recent (within the preceding 6 months) use of abacavir has been associated with a risk of myocardial infarction, but studies have yielded conflicting data.

Abacavir Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Abacavir Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 370)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Henan Fengda Chemical Co., Ltd
+86-371-86557731 +86-13613820652
info@fdachem.com China 7845 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21691 55
Hubei XinRunde Chemical Co., Ltd.
+8615102730682
bruce@xrdchem.cn CHINA 566 55
career henan chemical co
+86-0371-86658258
sales@coreychem.com China 29914 58
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28180 58
Chongqing Chemdad Co., Ltd
+86-023-61398051 +8613650506873
sales@chemdad.com China 39916 58
CONIER CHEM AND PHARMA LIMITED
+8618523575427
sales@conier.com China 49390 58
Shaanxi Dideu Medichem Co. Ltd
18192627656
1012@dideu.com China 3422 58
Guangzhou Yuheng Pharmaceutical Technology Co., Ltd
+8613580539051
joe@yuhengpharm.com CHINA 21149 58
Hebei Mojin Biotechnology Co., Ltd
+8613288715578
sales@hbmojin.com China 12456 58

136470-78-5()Verwandte Suche:


  • 1592u89
  • [(1s,4r)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]-1-cyclopent-2-enyl]methanol
  • [(1S,4R)-4-(2-AMINO-6-CYCLOPROPYLAMINO-PURIN-9-YL)-CYCLOPENT-2-ENYL]-METHANOL
  • 2-Cyclopentene-1-methanol, 4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-, (1S,4R)-
  • 2-Cyclopentene-1-methanol, 4-[2-amino-6-(cyclopropylamino)-9H-purin-9-yl]-, (1S-cis)-
  • (+/-)-4-[2-amino-6-(cyclopropylamino)-9h-purin-9-yl]-2-cyclopentene-1-methanol
  • Abacavir
  • Abacavir (see A105000)
  • Abacavir-(1R,trans)-isoMer
  • Abacavir-5'-tert-butyl ether
  • (1S-cis)-4-[2-AMino-6-(cyclopropylaMino)-9H-purin-9-yl]-2-cyclopentene-1-Methanol
  • Abacavir(base)
  • [(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9-purinyl]-1-cyclopent-2-enyl]methanol
  • CS-107
  • [(1S,4R)-4-[2-amino-6-(cyclopropylamino)purin-9-yl]cyclopent-2-en-1-yl]methanol
  • Abacavir >
  • ({(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9H-Purin-9- yl]cyclopent-2-en-l-yl} methanol)
  • Abacavir USP/EP/BP
  • Abacavir (1.0 mg/mL in Methanol)
  • {(1S,4R)-4-[2-amino-6-(cyclopropylamino)-9Hpurin-9-yl]cyclopent-2-en-1-yl}methanol
  • abacavir D5Q: What is abacavir D5 Q: What is the CAS Number of abacavir D5
  • Abacavir Tablet
  • Abacavir Standard
  • Abacavir Manufacturer/High quality/Best price/In stock CAS NO.136470-78-5
  • ((1S,4R)-4-(2-Amino-6-(cyclopropylamino)-9H-purin-9-yl)cyclopent-2-en-1-yl)methanol[Abacavir
  • Abacavir, ≥ 98.0%
  • 136470-78-5
  • C14H18N6O
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  • Inhibitors
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