Enfuvirtide

Enfuvirtide (T-20)
Cat. No.
BT1553
Source
Synonyms
Appearance
Sterile Filtered White lyophilized (freeze-dried) powder.
Purity

Greater than 98.0% as determined by RP-HPLC.

Usage

THE BioTek's products are furnished for LABORATORY RESEARCH USE ONLY. The product may not be used as drugs, agricultural or pesticidal products, food additives or household chemicals.

Shipped with Ice Packs
In Stock

Description

Enfuvirtide has an amino acid sequence 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, molecular formula of C204H301N51O64 and a molecular weight of 4488.9 Dalton.

Product Specs

Introduction
Enfuvirtide, also known as human immunodeficiency fusion inhibitor, prevents HIV from infecting healthy CD4 cells. It can decrease the viral load in the blood and boost the CD4 cell count. Enfuvirtide works by disrupting HIV-1's molecular machinery during the final stage of fusion with the target cell, thus preventing uninfected cells from becoming infected. By mimicking components of the HIV-1 fusion apparatus and displacing them, Enfuvirtide prevents normal fusion. HIV attaches to the host CD4+ cell receptor using the viral protein GP120; upon binding, GP120 undergoes conformational changes allowing the viral protein GP41 to insert itself into the host cell's plasma membrane. Entry inhibitors like Enfuvirtide bind to GP41, preventing the formation of an entry pore for the virus's capsid, effectively keeping it out of the cell.
Description
Enfuvirtide possesses the amino acid sequence 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, a molecular formula of C204H301N51O64, and a molecular weight of 4488.9 Daltons.
Physical Appearance
Sterile Filtered White Lyophilized Powder
Formulation
The protein (1 mg/ml) was lyophilized without any additives.
Solubility
Enfuvirtide lyophilized powder readily dissolves in water, achieving a concentration of 1 mg/ml.
Stability
Lyophilized Enfuvirtide, while stable at room temperature for up to 3 weeks, should be stored desiccated at a temperature below -18°C. After reconstitution, Enfuvirtide should be stored at 4°C for 2-7 days. For future use, store below -18°C. For long-term storage, adding a carrier protein (0.1% HSA or BSA) is recommended. Avoid repeated freeze-thaw cycles.
Purity
Greater than 98.0% as determined by RP-HPLC.

Product Science Overview

Development and History

Enfuvirtide was developed by researchers at Duke University, who later formed a pharmaceutical company called Trimeris. The development of enfuvirtide began in 1996, and it was initially designated as T-20. In 1999, Trimeris partnered with Hoffmann-La Roche to complete the development of the drug .

Mechanism of Action

Enfuvirtide is a 36-amino acid biomimetic peptide that mimics the structure of HIV proteins responsible for the fusion of the virus to cell membranes. The drug works by binding to the gp41 transmembrane protein of the HIV envelope, which is crucial for the fusion of the viral and host cell membranes. By interfering with the conformational changes required for membrane fusion, enfuvirtide effectively blocks the entry of the virus into the host cell .

Clinical Significance

Enfuvirtide represents the first of a new class of antiretroviral drugs known as fusion inhibitors. Its development marked a significant advancement in the treatment of HIV, particularly for patients who have developed resistance to other classes of antiretroviral drugs. The introduction of enfuvirtide provided a new option for heavily treated patients with advanced HIV disease .

Pharmacokinetics

Enfuvirtide is administered subcutaneously and has a bioavailability of approximately 84.3%. It is highly protein-bound (92%) and is metabolized in the liver. The elimination half-life of enfuvirtide is around 3.8 hours .

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