Enfuvirtide (T20; DP178) acetate is an anti-HIV (Human Immunodeficiency Virus)-1 fusion inhibitory peptide.

Physicochemical Properties

Molecular Formula	C206H305N51O66
Molecular Weight	4551.93
CAS #	914454-00-5
Related CAS #	Enfuvirtide;159519-65-0
Appearance	White to off-white solid powder
HS Tariff Code	2934.99.9001
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)

Biological Activity

Targets	HIV fusion[1]
ln Vitro	The effective concentration required to achieve 50% inhibition (IC50) of enfuvirtide, as revealed by cell-cell fusion, is 23 ± 6 nM[2]. HIV p24 antigen and Gag gene expression in macrophages is markedly inhibited by IFN-λs (1, 2, or 3) or antiretrovirals (AZT, Efavirenz, Indinavir test, and Enfuvirtide). Additionally, AZT, Efavirenz, Indinavir, and Enfuvirtide's anti-HIV (Bal) effects are strengthened by IFN-λs (1, 2, or 3)[3].
ln Vivo	T1/2 for enfuvirtide is 3.8 hours[2].
References	[1]. Quantitative analysis of molecular partition towards lipid membranes using surface plasmon resonance. Sci Rep. 2017 Mar 30;7:45647. [2]. 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]. IFN-λ Inhibits Drug-Resistant HIV Infection of Macrophages. Front Immunol. 2017 Mar 6;8:210.

Solubility Data

Solubility (In Vitro)

DMSO : 100 mg/mL (21.97 mM) H2O : 2 mg/mL (0.44 mM)

Solubility (In Vivo)

Solubility in Formulation 1: 2.5 mg/mL (0.55 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 25.0 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: 2.5 mg/mL (0.55 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. Solubility in Formulation 3: ≥ 2.5 mg/mL (0.55 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 25.0 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	0.2197 mL	1.0984 mL	2.1969 mL
	5 mM	0.0439 mL	0.2197 mL	0.4394 mL
	10 mM	0.0220 mL	0.1098 mL	0.2197 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.