Enfuvirtide
(Synonyms: 恩夫韦肽; T20; DP178) 目录号 : GC11162
A peptide inhibitor of HIV-1 fusion
Cas No.:159519-65-0
Sample solution is provided at 25 µL, 10mM.
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Enfuvirtide is an anti-HIV-1 fusion inhibitor peptide.
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].
Enfuvirtide has a T1/2 of 3.8 h[2].
Reference:
[1]. Figueira TN, et al. Quantitative analysis of molecular partition towards lipid membranes using surface plasmon resonance. Sci Rep. 2017 Mar 30;7:45647.
[2]. Cao P, et al. The improved efficacy of Sifuvirtide compared with Enfuvirtide might be related to its selectivity for the rigid biomembrane, as determined through surface plasmon resonance. PLoS One. 2017 Feb 16;12(2):e0171567.
[3]. Wang X, et al. IFN-λ Inhibits Drug-Resistant HIV Infection of Macrophages. Front Immunol. 2017 Mar 6;8:210.
Animal experiment: | 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: [1]. Figueira TN, et al. Quantitative analysis of molecular partition towards lipid membranes using surface plasmon resonance. Sci Rep. 2017 Mar 30;7:45647. | |
| Cas No. | 159519-65-0 | SDF | |
| 别名 | 恩夫韦肽; T20; DP178 | ||
| Canonical SMILES | CC[C@]([C@@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/C)([H])CC1=CC=C(O)C=C1)([H])[C@@](O)([H])C)([H])CO)([H])CC(C)C)([H])[C@@](CC)([H])C)([H])CC2=CN=CN2)([H])CO)([H])CC(C)C)([H])/C(O) | ||
| 分子式 | C204H301N51O64 | 分子量 | 4491.88 |
| 溶解度 | ≥ 149.7mg/mL in DMSO with gentle warming | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.2226 mL | 1.1131 mL | 2.2262 mL |
| 5 mM | 0.0445 mL | 0.2226 mL | 0.4452 mL |
| 10 mM | 0.0223 mL | 0.1113 mL | 0.2226 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet