Name | enfuvirtide |
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Synonyms |
T-20
Enfuvirtide Acetate (T-20) enfuvirtide UNII-19OWO1T3ZE Fuzeon DP178 acetyl-L-tyrosyl-L-threonyl-L-seryl-L-leucyl-L-isoleucyl-L-histidyl-L-seryl-L-leucyl-L-isoleucyl-L-a-glutamyl-L-a-glutamyl-L-seryl-L-glutaminyl-L-asparaginyl-L-glutaminyl-L-glutaminyl-L-a-glutamyl-L-lysyl-L-asparaginyl-L-a-glutamyl-L-glutaminyl-L-a-glutamyl-L-leucyl-L-leucyl-L-a-glutamyl-L-leucyl-L-a-aspartyl-L-lysyl-L-tryptophyl-L-alanyl-L-seryl-L-leucyl-L-tryptophyl-L-asparaginyl-L-tryptophyl-L-phenylalaninamide Pentafuside T 20 (peptide) Enfuvirtide Acetate |
Description | Enfuvirtide is an anti-HIV-1 fusion inhibitor peptide. 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. |
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Related Catalog | |
Target |
HIV fusion[1] |
In Vitro | A cell-cell fusion assay reveals that the effective concentration for achieving 50% inhibition (IC50) of Enfuvirtide is 23 ± 6 nM[2]. IFN-λs (1, 2, or 3) or the antiretrovirals (AZT, Efavirenz, Indinavir, and Enfuvirtide) significantly inhibita the expression of HIV p24 antigen and Gag gene in macrophages. IFN-λs (1, 2, or 3) also enhanced the anti-HIV (Bal) effect of AZT, Efavirenz, Indinavir, and Enfuvirtide[3]. |
In Vivo | Enfuvirtide has a T1/2 of 3.8 h[2]. |
Animal Admin | For infection with the resistant HIV strains, 7-day-cultured macrophages (105 cells/well in 96-well plates) are incubated with or without IFN-λ1, λ2, or λ3 (100 ng/mL each) and/or anti-HIV drugs: Azidothymidine (AZT) 10 pM; Efavirenz 100 pM; Indinavir 10-3 pM, and Enfuvirtide 10 nM for 24 h. Cells are then infected with different strains of HIV (6 ng p24/well) for 2 h. After washed three times with plain DMEM, cells are cultured with fresh 10% DMEM containing IFN-λs and/or antiretroviral drugs. For HIV Bal infection, culture supernatant is harvested at day 8 post infection for RT and p24 assays. Infected and untreated cells served as controls. HIV Gag gene expression in infected cells is also examined at day 8 post infection. For anti-HIV drug-resistant virus (A012 G691-6 or TC49) infection, culture supernatant is harvested for HIV p24 protein by ELISA at days 3, 5, 7, and 10 postinfection. The cell cultures are replaced with the fresh media supplemented with IFN-λ1, λ2, or λ3 and/or the antiretrovirals every 2–3 days. The culture supernatant collected at day 10 postinfection is also subjected to RT assay[3]. |
References |
Density | 1.59g/cm3 |
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Molecular Formula | C204H301N51O64 |
Molecular Weight | 4491.88000 |
Exact Mass | 4489.19000 |
PSA | 1902.89000 |
LogP | 5.69700 |
Storage condition | ?20°C |