Enfuvirtide acetate
A peptide inhibitor of HIV-1 fusion
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包装价格促销价数量
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5mg￥650.00520.00- +
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10mg￥987.00790.00- +
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25mg￥2062.001650.00- +
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50mg￥3662.002930.00- +
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100mg￥0.000.00- +
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200mg￥0.000.00- +
- 货号: ajcx14330
- CAS: 914454-00-5
- 别名: 醋酸恩夫韦地; T20 acetate; DP178 acetate
- 分子式: C206H305N51O66
- 分子量: 4551.93
- 纯度: ＞98%
- 溶解度: Soluble in DMSO
- 储存: Store at -20°C
- 库存: 现货
Background
Enfuvirtide is a biomimetic peptide inhibitor of HIV-1 fusion with CD4+ cells.1 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).2 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).3 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.4 Formulations containing enfuvirtide have been used in combination therapy for the treatment of HIV-1/AIDS.
1.Ingallinella, P., Bianchi, E., Ladwa, N.A., et al.Addition of a cholesterol group to an HIV-1 peptide fusion inhibitor dramatically increases its antiviral potencyProc. Natl. Acad. Sci. USA106(14)5801-5806(2009) 2.McElrath, M.J., Ballweber, L., Terker, A., et al.Ex vivo comparison of microbicide efficacies for preventing HIV-1 genomic integration in intraepithelial vaginal cellsAntimicrob. Agents Chemother.54(2)763-772(2010) 3.Champagne, K., Shishido, A., and Root, M.J.Interactions of HIV-1 inhibitory peptide T20 with the gp41 N-HR coiled coilJ. Biol. Chem.284(6)3619-3627(2009) 4.Sun, S.B., Gong, W.H., Gao, J.L., et al.T20/DP178, an ectodomain peptide of human immunodeficiency virus type 1 gp41, is an activator of human phagocyte N-formyl peptide receptorBlood93(11)3885-3892(1999)
