Remdesivir (GS-5734)

For research use only. Not for use in humans.

目录号:S8932 中文名称:瑞德西韦,伦地西韦

Remdesivir (GS-5734) Chemical Structure

CAS No. 1809249-37-3

Remdesivir (GS-5734)是腺苷类似物的单磷酰胺酸盐前药,是一种研究性的广谱抗病毒剂,对多种RNA病毒(包括埃博拉病毒和CoV病毒)具有体外活性。

规格 价格 库存 购买数量  
10mM (1mL in DMSO) RMB 7945.1 现货
RMB 1859.45 现货
RMB 4562.14 现货
RMB 13677.3 现货
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客户使用Selleck生产的Remdesivir (GS-5734)发表文献37篇:

产品安全说明书

Antiviral抑制剂选择性比较

生物活性

产品描述 Remdesivir (GS-5734)是腺苷类似物的单磷酰胺酸盐前药,是一种研究性的广谱抗病毒剂,对多种RNA病毒(包括埃博拉病毒和CoV病毒)具有体外活性。
体外研究

GS-5734 exhibits antiviral activity against multiple variants of EBOV in cell-based assays(EC50=0.06-0.14 μM) and broad-spectrum antiviral activity in vitro against other pathogenic RNA viruses. [1]GS-5734 acts as a broad-spectrum therapeutic to protect against CoVs with EC50 of 0.03 μM for murine hepatitis virus in delayed brain tumor cells and 0.074 μM for SARS-CoV and MERS-CoV in HAE cells.[2]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hep2 NGT6[m5CdnSrdnnyZYwh[WO2aY\peJkh[XO|YYm= Mlf2OEBl[Xm| MoX5SWM2OCB;IECuNFE2KM7:TR?= MUG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF{NEmwO{c,OjhzMkS5NFc9N2F-
TERT-immortalized HMVEC M2f1SmFvfGm4aYLhcEBi[3Srdnn0fUBie3OjeR?= NH;jZY8{KHSxIESg[IF6ew>? NGWweFRGSzVyIE2gNE4xPTNizszN M3u0[|xiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUK0PVA4Lz5{OEGyOFkxPzxxYU6=
HuH7 MmnTRY51cX[rcnHsJIFkfGm4aYT5JIF{e2G7 MUmzJIRigXN? MnnwSWM2OCB;IECuNFU4KM7:TR?= M4LU[lxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUK0PVA4Lz5{OEGyOFkxPzxxYU6=
HuH7 MVHBcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? NELMdJY{KGSjeYO= MUfFR|UxKD1iMD6wO{DPxE1? NV3y[GZKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjNpPkK4O|kzPzZ|PD;hQi=>
macrophages MnXVRY51cX[rcnHsJIFkfGm4aYT5JIF{e2G7 M2\6[|Q5KGh? MUHFR|UxKD1iMD6wPFYh|ryP MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF{NEmwO{c,OjhzMkS5NFc9N2F-
macrophages M3S4N2FvfGm4aYLhcEBi[3Srdnn0fUBie3OjeR?= MmjnOFghcA>? NXz0W5JQTUN3MDC9JFAvODh4IN88US=> NIr2UZM9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe5Nlc3Oyd-Mki3PVI4PjN:L3G+
HeLa MV3BcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? M2r3flQ5KGh? NW\GWYJETUN3MDC9JFAvOSEQvF2= M2rkZlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6MUK0PVA4Lz5{OEGyOFkxPzxxYU6=
HeLa M33DSGFvfGm4aYLhcEBi[3Srdnn0fUBie3OjeR?= MUi0PEBp MoPHSWM2OCB;IECuNVQh|ryP M4fIcFxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzJ6N{myO|Y{Lz5{OEe5Nlc3OzxxYU6=
MT4 MmLGR5l1d3SxeHnjbZR6KGG|c3H5 NGnTdoY1KHSxIEWg[IF6ew>? MWDDR|UxKD1iMT63JO69VQ>? MUm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF{NEmwO{c,OjhzMkS5NFc9N2F-
Hep2 NXuz[mZFS3m2b4TvfIlkcXS7IHHzd4F6 MoPiOEB1dyB3IHThfZM> NV7C[3RuS0N3MDC9JFYvOSEQvF2= NXHURmtKRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNlQ6ODdpPkK4NVI1QTB5PD;hQi=>
HuH7 NEfadVREgXSxdH;4bYNqfHliYYPzZZk> NI[3eIo{KGSjeYO= MY\DR|UxKD1iM{[g{txO NWCxSnRLRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNlQ6ODdpPkK4NVI1QTB5PD;hQi=>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
delayed chain termination of RNA synthesis; 

PubMed: 30987343     


Effective delayed chain termination of RNA synthesis by remdesivir. (A) Remdesivir-MP-dependent delayed chain termination of RNA synthesis was studied with purified EBOV RdRp. RNA synthesis was monitored in the presence of [α-32P]GTP, CTP, and ATP or remdesivir-TP, supplemented with increasing concentrations of UTP for incorporation at position i+6, representing a 12-nt RNA product labeled 12.

tGFP-BlaR / Actin; 

PubMed: 33835389     


Thirty-six hours post-transfection, Western blot for tGFP-BlaR expression is carried out with remdesivir treated cells.

ACE2 / Actin; 

PubMed: 32793908     


(C) Remdesivir alone increased ACE2 protein expression. H1299 human NSCLC cells, MSTO-211H human mesothelioma cells, and Calu-3 human NSCLC type II alveolar cells were treated with remdesivir and VS-6766 for 48 hours. ACE2 was probed with Abnova PAB13444 antibody, and β-Actin was probed with Sigma A5441 antibody as a loading control.

VP0 / VP2; 

PubMed: 32595613     


(C) Western blot of EV71 VP2 protein expression in HeLa cells. HeLa cells were infected with EV71 (MOI = 0.5). After adsorption, the cells were treated with the indicated concentrations of remdesivir and collected at 24 hpi. Then, the proteins were resolved by SDS-PAGE and western blotting.

30987343 33835389 32793908 32595613
Growth inhibition assay
Cell viability; 

PubMed: 33835389     


293 T cells are transfected with SARS-CoV-2-GFP replicon, remdesivir is added to culture media 10 h post transfection or just before transfection respectively, the green fluorescence intensity is determined thirty-six hours post-transfection, and dose responsive curves are drawn and EC50 value of remdesivir (B) was calculated by four-parameter nonlinear regression respectively.

Cell viability; 

PubMed: 33186749     


Remdesivir inhibits SARS-CoV-2 infection of PSC-HIOs. (B) Effect of remdesivir on metabolic activity of Caco-2 cells was assessed by CellTiter-Glo assay. Shown are technical triplicates from one representative experiment. Error bars represent SEM.

Cell viability; 

PubMed: 32595613     


(B) Cell viability after culture with different doses of remdesivir at 24 hpi assessed using a CCK8 assay (mean ± SD, n = 6).

33835389 33186749 32595613
Pharmacokinetics
plasma concentration; 

PubMed: 32589775     


Plasma concentration‐vs‐time profiles following RDV single‐dose administration; mean (±SD) values are plotted. LLOQ, lower limit of quantification; RDV, remdesivir.

plasma concentration; 

PubMed: 33782830     


Mean (standard deviation) of remdesivir (RDV) plasma concentration vs time by dose following 30-min intravenous infusion(s) of a single 200-mg dose or multiple 100-mg remdesivir doses in healthy subjects.

32589775 33782830
Immunofluorescence
MERS-CoV S Protein; 

PubMed: 33376043     


Dose-dependent inhibition of MERS-CoV infection by lycorine. (B) The confocal microscope images showed cell nuclei (red) and MERS-CoV spike (S) protein (green) at the indicated lycorine concentration or 8.3 μM remdesivir (RDV) after MERS-CoV infection. Scale bar = 100 μM.

viral S protein and E-caherin; 

PubMed: 33186749     


(C) PSC-HIOs were infected with SARS-CoV-2 and treated with indicated concentrations of remdesivir. Two days later, infection was analyzed by viral S protein and E-caherin (Ecad, green) staining. Nuclei are stained with DAPI in blue. Scale bar = 50 μM. Images are representative for at least 3 independent experiments.

SARS-CoV-2 / E‐cadherin / VE‐cadherin; 

PubMed: 33173719     


Evaluation of potential antiviral efficacy of remdesivir on the chip system. B) Confocal immunofluorescent microscopy images of epithelium (E‐cadherin) and endothelium (VE‐cadherin) of alveolus chip treated without or with 1 × 10−6 m remdesivir at day 2 post‐infection.

SARS-CoV-2; 

PubMed: 32869028     


Antiviral SARS-CoV-2 activity and cytotoxicity of PF-00835231, and remdesivir in A549+ACE2 cells. f. Representative images of SARS-CoV-2 USA-WA1/2020 syncytia formation at 48 hpi in A549+ACE2 cells under treatment with 0.33 μM PF-00835231, or remdesivir.

viral dsRNA replication intermediates; 

PubMed: 32595613     


(D) Fluorescence microscopy examination of EV71-infected HeLa cells treated with different amounts of remdesivir (24 hpi). The dsRNA-specific antibody J2 (red) was used for staining viral dsRNA replication intermediates, and nuclei were labeled with Hoechst 33258 (blue). Bar = 100 μm.

33376043 33186749 33173719 32869028 32595613
Viral loads and virus titers
SARS-CoV-2; 

PubMed: 32516797     


Viral loads and virus titers in swabs collected from rhesus macaques infected with SARS-CoV-2 and treated with remdesivir. Panel A shows viral loads and Panel B shows infectious virus titers in nose, throat and rectal swabs collected daily from animals treated with remdesivir (n=6) or vehicle solution (n=6). Statistical analysis was performed using a 2-way ANOVA with Sidak’s multiple comparisons test.

32516797
体内研究

Regardless of the time of initiation, GS-5734 treatment confers improved survival when administered by 3 mg/kg GS-5734. All animals in which 10 mg/kg GS-5734 treatments is initiated 3 days after virus exposure survive to the end of the in-life phase. However, the antiviral effects are consistently greater in animals administered repeated 10 mg/kg GS-5734 doses. The 10 mg/kg D3 (administered beginning 3 days after virus exposure) GS-5734 regimen is associated with amelioration of EVD-related clinical disease signs and markers of coagulopathy and end organ pathophysiology.[1]

推荐的实验操作(此推荐来自于公开的文献所以Selleck并不保证其有效性)

动物实验:

[1]

- 合并
  • Animal Models: Rhesus monkeys (Macaca mulatta)
  • Dosages: 3 mg / kg, 10 mg / kg
  • Administration: IV
    (Only for Reference)

溶解度 (25°C)

体外 DMSO 100 mg/mL (165.95 mM)
Water Insoluble
Ethanol ''''16 mg/mL

* 溶解度检测是由Selleck技术部门检测的,可能会和文献中提供的溶解度有所差异,这是由于生产工艺和批次不同产生的正常现象。请按照顺序依次加入各个纯溶剂。

化学数据

分子量 602.58
化学式

C27H35N6O8P

CAS号 1809249-37-3
储存条件 粉状
溶于溶剂
别名 N/A

动物体内配方计算器 (澄清溶液)

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
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Selleck为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % ddH2O
计算重置

计算器

摩尔浓度计算器

摩尔浓度计算器

本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系,公式为:

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)

摩尔浓度计算公式

  • 质量
    浓度
    体积
    分子量

*在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。

稀释计算器

稀释计算器

用本工具协助配置特定浓度的溶液,使用的计算公式为:

开始浓度 x 开始体积 = 最终浓度 x 最终体积

稀释公式

稀释公式一般简略地表示为: C1V1 = C2V2 ( 输入 输出 )

  • C1
    V1
    C2
    V2

在配置溶液时,请务必参考Selleck产品标签上、SDS / COA(可在Selleck的产品页面获得)批次特异的分子量使用本工具。.

连续稀释计算器方程

  • 连续稀释

  • 计算结果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):
分子量计算器

分子量计算器

通过输入化合物的化学式来计算其分子量:

总分子量:g/mol

注:化学分子式大小写敏感。C10H16N2O2 c10h16n2o2

摩尔浓度计算器

质量 浓度 体积 分子量
计算

临床试验信息

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02818582 Completed Drug: GS-5734|Other: Placebo Comparator Ebola National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health Clinical Center (CC) July 1 2016 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID