| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
HIV-1
Enfuvirtide targets the HIV-1 envelope glycoprotein gp41. It binds to gp41, preventing the conformational changes required for the fusion of the viral and cellular membranes. This inhibits the entry of the HIV-1 virus into the host cell. |
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| ln Vitro |
According to a cell-cell fusion assay, 23 ± 6 nM is the effective concentration required to achieve 50% inhibition (IC50) of enfuvirtide[2]. The expression of the HIV p24 antigen and the Gag gene in macrophages is significantly inhibited by IFN-λs (1, 2, or 3) or antiretrovirals (AZT, Efavirenz, Indinavir, and Enfuvirtide). The anti-HIV (Bal) effects of AZT, Efavirenz, Indinavir, and Enfuvirtide were also improved by IFN-λs (1, 2, or 3)[3].
In vitro, Enfuvirtide potently inhibits HIV-1 infectivity. It inhibits the HIV-1 HXB2 strain in HeLa cells stably expressing CD4 with an IC50 of 692 pM. It also inhibits clinical isolates with IC90s ranging from 6.1 to 61 nM in a single-cycle infectivity assay. It inhibits HIV p24 antigen and Gag gene expression in macrophages. |
| ln Vivo |
Enfuvirtide has a T1/2 of 3.8 h[2].
In vivo, Enfuvirtide is used to treat HIV-1 infection. It is administered by subcutaneous injection and is used in combination with other antiretroviral medications. It is effective in reducing viral load and increasing CD4+ T cell counts in patients with multi-drug resistant HIV. |
| Enzyme Assay |
In vitro assays for Enfuvirtide typically measure its ability to inhibit HIV-1 entry and replication. A common assay is a single-cycle infectivity assay, where pseudotyped viruses are used to infect cells, and viral entry is measured by reporter gene expression. The IC50 is calculated from the inhibition curve.
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| Cell Assay |
Cellular assays are performed using cells susceptible to HIV-1 infection, such as HeLa cells expressing CD4. Cells are treated with Enfuvirtide and then exposed to the virus. Viral replication is measured by quantifying viral proteins like p24 antigen or by measuring reporter gene activity.
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| Animal Protocol |
Seven days after being cultured (105 cells/well in 96-well plates), the macrophages are incubated with or without IFN-λ1, λ2, or λ3 (100 ng/mL each) and/or anti-HIV medications for 24 hours. These medications include Azidothymidine (AZT) 10 pM, Efavirenz 100 pM, Indinavir 10-3 pM, and Enfuvirtide 10 nM. Following that, cells are infected for two hours with various HIV strains (6 ng p24/well). Following three rounds of basic DMEM washing, cells are cultivated in new 10% DMEM supplemented with IFN-λs and/or antiretroviral medications.Day 8 post-infection is when culture supernatant for HIV Bal infection is collected for RT and p24 assays. The controls were untreated and infected cells. On day eight after infection, the expression of the HIV Gag gene in infected cells is also analyzed. At days 3, 5, 7, and 10 after infection, the culture supernatant is collected for HIV p24 protein analysis by ELISA in order to detect the anti-HIV drug-resistant virus (A012 G691-6 or TC49). Every two to three days, the cell cultures are swapped out for fresh media supplemented with IFN-λ1, λ2, or λ3 and/or antiretrovirals. The RT assay is additionally performed on the culture supernatant that was obtained on day 10 postinfection[3].
In vivo efficacy is evaluated in HIV-1 infected patients. The compound is administered subcutaneously, and its effects on viral load (plasma HIV-1 RNA) and CD4+ T cell counts are monitored. It is typically used in combination with other antiretroviral drugs. |
| ADME/Pharmacokinetics |
Enfuvirtide is a 36-amino acid peptide with a molecular weight of 4491.88 g/mol. As a peptide, it is not orally bioavailable and is administered by subcutaneous injection. It is metabolized by proteolytic degradation and has a relatively short half-life, requiring twice-daily dosing.
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| Toxicity/Toxicokinetics |
Enfuvirtide is generally well-tolerated. The most common side effect is injection site reactions. It can also cause hypersensitivity reactions and an increased risk of bacterial pneumonia. Its safety profile is well-established from its clinical use.
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| References | |
| Additional Infomation |
Enfuvirtide is the first of a new class of HIV therapeutics that interferes with the entry of HIV-1 by inhibiting fusion of viral and cellular membranes. It is a biomimetic peptide of HIV-1 fusion inhibitor. It is a valuable treatment option for patients with multi-drug resistant HIV.
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| Molecular Formula |
C204H301N51O64
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|---|---|
| Molecular Weight |
4491.87603999996
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| Exact Mass |
4489.19
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| Elemental Analysis |
C, 54.55; H, 6.75; N, 15.90; O, 22.79
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| CAS # |
159519-65-0
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| Related CAS # |
Enfuvirtide acetate;914454-00-5
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| PubChem CID |
16130199
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| Appearance |
White to off-white solid powder
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| Density |
1.59g/cm3
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| LogP |
5.697
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| Hydrogen Bond Donor Count |
63
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| Hydrogen Bond Acceptor Count |
67
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| Rotatable Bond Count |
151
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| Heavy Atom Count |
319
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| Complexity |
11200
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| Defined Atom Stereocenter Count |
39
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| InChi Key |
PEASPLKKXBYDKL-FXEVSJAOSA-N
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| Synonyms |
Enfuvirtide; DP178; DP-178; DP 178
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~20 mg/mL (~4.45 mM)
H2O : ~0.67 mg/mL (~0.15 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (0.45 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2 mg/mL (0.45 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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