标签归档：enfuvirtide

Enfuvirtide acetate(Synonyms: 醋酸恩夫韦地 T20 acetate DP178 acetate)

发表于由

Enfuvirtide acetate;(Synonyms: 醋酸恩夫韦地; T20 acetate; DP178 acetate) 纯度: 97.22%

Enfuvirtide (T20; DP178) acetate 是一种抗 HIV-1 融合的抑制肽。

Enfuvirtide acetateamp;;(Synonyms: 醋酸恩夫韦地; T20 acetate; DP178 acetate)

Enfuvirtide acetate Chemical Structure

CAS No. : 914454-00-5

规格 价格 是否有货 数量
5 mg ￥600 In-stock
10 mg ￥900 In-stock
25 mg ￥1900 In-stock
50 mg ￥3400 In-stock
100 mg ; 询价 ;
200 mg ; 询价 ;

* Please select Quantity before adding items.

Enfuvirtide acetate 相关产品

bull;相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Peptide Library

生物活性

Enfuvirtide (T20; DP178) acetate is an anti-HIV-1 fusion inhibitor peptide.

IC50 Target

HIV fusion[1]
体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Enfuvirtide has a T1/2 of 3.8 h[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

4551.93

Formula

C2H4O2
CAS 号

914454-00-5
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
Sequence Shortening

Ac-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-NH2
中文名称

醋酸恩夫韦肽；醋酸恩夫韦地
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Sealed storage, away from moisture

Powder -80deg;C 2 years
-20deg;C 1 year

*In solvent : -80deg;C, 6 months; -20deg;C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro:;

DMSO : 100 mg/mL (21.97 mM; Need ultrasonic)

H2O : 2 mg/mL (0.44 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 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

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂：;10% DMSO ;; 40% PEG300 ;; 5% Tween-80 ;; 45% saline

    Solubility: 2.5 mg/mL (0.55 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (0.55 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂：;10% DMSO ;; 90% (20% SBE-β-CD in saline)

    Solubility: 2.5 mg/mL (0.55 mM); Suspended solution; Need ultrasonic

    此方案可获得 2.5 mg/mL (0.55 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
  • 3.

    请依序添加每种溶剂：;10% DMSO ;; 90% corn oil

    Solubility: ≥ 2.5 mg/mL (0.55 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (0.55 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [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.

Enfuvirtide(Synonyms: 恩夫韦肽 T20 DP178)

发表于由

Enfuvirtide (Synonyms: 恩夫韦肽; T20; DP178) 纯度: 99.56%

Enfuvirtide (T20;DP178) 是一种抗 HIV-1 融合的抑制肽。

Enfuvirtide (Synonyms: 恩夫韦肽; T20; DP178)

Enfuvirtide Chemical Structure

CAS No. : 159519-65-0

规格 价格 是否有货 数量
5 mg ￥1000 In-stock
10 mg ￥1600 In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Enfuvirtide 相关产品

•相关化合物库:

  • Drug Repurposing Compound Library Plus
  • FDA-Approved Drug Library Plus
  • Bioactive Compound Library Plus
  • Anti-Infection Compound Library
  • FDA-Approved Drug Library
  • Antiviral Compound Library
  • Drug Repurposing Compound Library
  • FDA Approved & Pharmacopeial Drug Library
  • Drug-Induced Liver Injury (DILI) Compound Library
  • Rare Diseases Drug Library
  • Peptide Library

生物活性

Enfuvirtide (T20;DP178) is an anti-HIV-1 fusion inhibitor peptide.

IC50 & Target

HIV fusion[1]
体外研究
(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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

Enfuvirtide has a T1/2 of 3.8 h[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial

分子量

4491.88

Formula

C204H301N51O64
CAS 号

159519-65-0
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
Sequence Shortening

Ac-YTSLIHSLIEESQNQQEKNEQELLELDKWASLWNWF-NH2
中文名称

恩夫韦肽
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -80°C 2 years
-20°C 1 year
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 20 mg/mL (4.45 mM; Need ultrasonic)

H2O : 0.67 mg/mL (0.15 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 0.2226 mL 1.1131 mL 2.2262 mL
5 mM — — —
10 mM — — —

*

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, 6 months; -20°C, 1 month。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: 2 mg/mL (0.45 mM); Suspended solution; Need ultrasonic

    此方案可获得 2 mg/mL (0.45 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

  • 2.

    请依序添加每种溶剂： 10% DMSO    90% corn oil

    Solubility: ≥ 2 mg/mL (0.45 mM); Clear solution

    此方案可获得 ≥ 2 mg/mL (0.45 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例，取 100 μL 20.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

  • [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 Administration
[3]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献

  • [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.

  • [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.