Enfuvirtide

Enfuvirtide Struktur
159519-65-0
CAS-Nr.
159519-65-0
Englisch Name:
Enfuvirtide
Synonyma:
Enf;Aids059486;Enfvectide;Aids-059486;Enfuvirtide;Pentafuside;Fuzeon (tm);Gp41 127-162 aa;Enfuvirtide; T-2;T20, Pentafuside
CBNumber:
CB7358557
Summenformel:
C204H301N51O64
Molgewicht:
4491.92
MOL-Datei:
159519-65-0.mol

Enfuvirtide Eigenschaften

storage temp. 
-20°C
Löslichkeit
DMF: 5 mg/ml; DMSO: 5 mg/ml; PBS (pH 7.2): 2 mg/ml
Aggregatzustand
powder
Farbe
white to off-white
Sequenz
Ac-Tyr-Thr-Ser-Leu-Ile-His-Ser-Leu-Ile-Glu-Glu-Ser-Gln-Asn-Gln-Gln-Glu-Lys
Sicherheit
  • Risiko- und Sicherheitserklärung
  • Gefahreninformationscode (GHS)
WGK Germany  3
HS Code  3504009000
Giftige Stoffe Daten 159519-65-0(Hazardous Substances Data)
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
H335 Kann die Atemwege reizen. Spezifische Zielorgan-Toxizität (einmalige Exposition) Kategorie 3 (Atemwegsreizung) Warnung GHS hazard pictogramssrc="/GHS07.jpg" width="20" height="20" />
Sicherheit
P261 Einatmen von Staub vermeiden.
P271 Nur im Freien oder in gut belüfteten Räumen verwenden.
P280 Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

Enfuvirtide Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung

Enfuvirtide is a biomimetic peptide inhibitor of HIV-1 fusion with CD4+ cells. It inhibits HIV-1 infectivity of HeLa cells stably expressing CD4 by the HXB2 strain (IC50 = 692 pM) and by clinical isolates (IC90s = 6.1-61 nM) in a single-cycle infectivity assay. It also inhibits genomic integration of HIV-1 into human intraepithelial vaginal cells and peripheral blood mononuclear cells (PBMCs; IC50s = 51.2 and 13.58 μM, respectively). Enfuvirtide binds to a recombinant molecular mimic of HIV-1 glycoprotein gp41 that contains three N-terminal heptad and two C-terminal heptad repeat regions (Kd = 32 nM). It also binds to recombinant formyl peptide receptors (FPR) expressed in rat basophilic leukemia cells (IC50 = 5 nM) and attracts and activates human peripheral blood phagocytes, but not T lymphocytes, in vitro when used at a concentration of 100 nM. Formulations containing enfuvirtide have been used in combination therapy for the treatment of HIV-1/AIDS.

Verwenden

Antiviral (blockade of gp-41 mediated membrane fusion). Fuzeon (Roche) [Note—The trivial name, pentafuside, has appeared in literature.

Definition

ChEBI: A synthetic 36-amino acid peptide consisting of N-acetyltyrosyl, threonyl, seryl, leucyl, isoleucyl, histidyl, seryl, leucyl, isoleucyl, alpha-glutamyl, alpha-glutamyl, seryl, glutaminyl, asparaginyl, glutaminyl, glutamin l, alpha-glutamyl, lysyl, asparaginyl, alpha-glutamyl, alpha-glutamyl, alpha-glutamyl, leucyl, leucyl, alpha-glutamyl, leucyl, alpha-aspartyl, lysyl, tryp ophyl, alanyl, seryl, leucyl, tryptophyl, asparaginyl, tryptophyl, and phenylalaninamide residues joined in sequence. An HIV fusion inhibitor, it was the first of a novel class of antiretroviral drugs used in combination therapy for the treatment of HIV-1 nfection. It interferes with entry of HIV into cells by binding to the gp41 sub-unit of the viral envelope glycoprotein, so inhibiting fusion of viral and cellular membranes.

Biologische Funktion

Enfuvirtide is used in combination with other antiretrovirals and works against a variety of HIV-1 variants, but it is not active against HIV-2. Resistance to enfuvirtide can develop when the virus produces changes in a 10-amino-acid domain between residues 36 to 45 in the gp41 HIV surface glycoprotein.

Acquired resistance

Resistance is mediated by amino acid substitutions within the first heptad repeat region of gp41 at amino acids 36–45. Resistance emerges fairly rapidly in patients experiencing virological failure with an enfuvirtide-containing antiretroviral regimen, and is associated with the return of the plasma HIV load toward baseline within a few weeks.

Allgemeine Beschreibung

Enfuvirtide acetate salt is a linear synthetic peptide made of 36 amino acids. It has an acetylated N-terminus and a carboxamide C-terminus. Enfuvirtide is catabolized with the help of proteolytic enzymes.

Pharmazeutische Anwendungen

A linear 36-amino acid synthetic peptide with an acetylated N-terminus and a carboxamide C-terminus. It is formulated as a lyophilized powder to be reconstituted for subcutaneous injection.

Pharmakokinetik

Subcutaneous absorption c. 84.3%
Cmax 90 mg s/c twice daily c. 4.59 mg/L
Plasma half-life c. 3.8 h
Volume of distribution 5.5 L
Plasma protein binding c. 92%
Absorption and distribution
Absorption of the 90 mg dose is comparable when injected into the subcutaneous tissue of the abdomen, thigh or arm. It does not penetrate the CSF or semen. Distribution into breast milk has not been described.
Metabolism and excretion
It probably undergoes catabolism to its constituent amino acids, with subsequent recycling of the amino acids in the body pool.

Clinical Use

Treatment of HIV infection (in combination with other antiretroviral drugs) in adults and children older than 6 years who show evidence of HIV-1 replication despite ongoing antiretroviral therapy

Nebenwirkungen

It does not seem to have any long-term toxicities (including the HIV lipodystrophy syndrome) associated with other commonly used antiretrovirals. Reaction at the injection site, variously characterized by local pain, erythema, pruritus, induration, ecchymosis, nodules or cysts, is experienced by more than 90% of patients and may lead to treatment fatigue.

Enfuvirtide Upstream-Materialien And Downstream Produkte

Upstream-Materialien

Downstream Produkte


Enfuvirtide Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

Global( 224)Lieferanten
Firmenname Telefon E-Mail Land Produktkatalog Edge Rate
Hebei Yanxi Chemical Co., Ltd.
+8617531190177
peter@yan-xi.com China 5993 58
Henan Bao Enluo International TradeCo.,LTD
+86-17331933971 +86-17331933971
deasea125996@gmail.com China 2503 58
Zibo Hangyu Biotechnology Development Co., Ltd
+86-0533-2185556 +8617865335152
Mandy@hangyubiotech.com China 11013 58
Nantong Guangyuan Chemicl Co,Ltd
+undefined17712220823
admin@guyunchem.com China 616 58
Alpha Biopharmaceuticals Co., Ltd
+86-411-39042497 +8613921981412
sales@alphabiopharm.com China 886 58
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512
info@tianfuchem.com China 21691 55
Rixing Chemical CO.,LTD
+86-13237129059 -13237129059
sales@rixingchemi.com CHINA 229 55
career henan chemical co
+86-0371-86658258
sales@coreychem.com China 29914 58
Shenzhen Nexconn Pharmatechs Ltd
+86-755-89396905 +86-15013857715
admin@nexconn.com China 10248 58
Hubei Jusheng Technology Co.,Ltd.
18871490254
linda@hubeijusheng.com CHINA 28180 58

159519-65-0()Verwandte Suche:


  • Enfuvirtide; T-2
  • Enfuvirtide Acetate (T-20)
  • ENFUVIRTIDE(T-20) 98+%
  • Enfurvitide(T-20)
  • Pentafuside
  • Ac-Tyr-Thr-Ser-Leu-Ile-His-Ser-Leu-Ile-Glu-Glu-Ser-Gln-Asn-Gln-Gln-Glu-Lys-Asn-Glu-Gln-Glu-Leu-Leu-Glu-Leu-Asp-Lys-Trp-Ala-Ser-Leu-Trp-Asn-Trp-Phe-NH{2}
  • Enfuvirtide
  • Aids059486
  • Aids-059486
  • Enf
  • Fuzeon (tm)
  • Gp41 127-162 aa
  • Enfuvirtide & Enfuvirtide Acetate
  • Ac-Tyr-Thr-Ser-Leu-Ile-His-Ser-Leu-Ile-Glu-Glu-Ser-Gln-Asn-Gln-Gln-Glu-Lys-Asn-Glu-Gln-Glu-Leu-Leu-Glu-Leu-Asp-Lys-Trp-Ala-Ser-Leu-Trp-Asn-Trp-Asn-Trp-Phe-NH2
  • T20, Pentafuside
  • Enfuvirtide acetate salt
  • T-20 acetate salt
  • Enfuvirtide(T-20) Acetate
  • Enfuvirtide,Ac-Tyr-Thr-Ser-Leu-Ile-His-Ser-Leu-Ile-Glu-Glu-Ser-Gln-Asn-Gln-Gln-Glu-Lys-Asn-Glu-Gln-Glu-Leu-Leu-Glu-Leu-Asp-Lys-Trp-Ala-Ser-Leu-Trp-Asn-Trp-Phe-NH2,Ac-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-NH2?, >95%
  • Enfuvirtide impurity
  • Well, wei peptide
  • Enfuvirtide USP/EP/BP
  • 159519-65-0 Enfuvirtide Acetate (T-20)
  • Enfvectide
  • Ticagrelor Impurity 227
  • Enfuvirtide,Ac-Tyr-Thr-Ser-Leu-Ile-His-Ser-Leu-Ile-Glu-Glu-Ser-Gln-Asn-Gln-Gln-Glu-Lys-Asn-Glu-Gln-Glu-Leu-Leu-Glu-Leu-Asp-Lys-Trp-Ala-Ser-Leu-Trp-Asn-Trp-Phe-NH2,Ac-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-NH2
  • Rabbit Anti-Enfuvirtide/Bio Conjugated antibody
  • Enfuvirtide, Pentafuside
  • Enfuvirtide, Pentafuside, T20
  • 159519-65-0
  • C204H301N51O64
  • proteins
  • Peptide
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