Remdesivir (GS-5734)

For research use only. Not for use in humans.

製品コードS8932

Remdesivir (GS-5734)化学構造

CAS No. 1809249-37-3

Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV.

サイズ 価格(税別)  
JPY 34600
JPY 82200
JPY 242400
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文献中Selleckの製品使用例(41)

製品安全説明書

Antiviral阻害剤の選択性比較

生物活性

製品説明 Remdesivir (GS-5734), a monophosphoramidate prodrug of an adenosine analog, is an investigational broad-spectrum antiviral agent with in vitro activity against multiple RNA viruses, including Ebola and CoV.
体外試験

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]

細胞データ
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Hep2 MXzBcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? M3n0[FQh\GG7cx?= M{S2d2VEPTBiPTCwMlAyPSEQvF2= NXj1XIVJRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNlQ6ODdpPkK4NVI1QTB5PD;hQi=>
TERT-immortalized HMVEC NVX6Umg3SW62aY\pdoFtKGGldHn2bZR6KGG|c3H5 NHfUO24{KHSxIESg[IF6ew>? MmHxSWM2OCB;IECuNFU{KM7:TR?= MWm8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF{NEmwO{c,OjhzMkS5NFc9N2F-
HuH7 MXvBcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? MYCzJIRigXN? NFiyN3JGSzVyIE2gNE4xPTdizszN NIXqXpI9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGyOFkxPyd-MkixNlQ6ODd:L3G+
HuH7 NHzLR4ZCdnSrdnnyZYwh[WO2aY\peJkh[XO|YYm= NWK0SJl2OyCmYYnz MoXwSWM2OCB;IECuNFch|ryP NGLoWYg9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEe5Nlc3Oyd-Mki3PVI4PjN:L3G+
macrophages NEPXeGpCdnSrdnnyZYwh[WO2aY\peJkh[XO|YYm= M{PwbFQ5KGh? Ml23SWM2OCB;IECuNFg3KM7:TR?= MnzNQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjhzMkS5NFcoRjJ6MUK0PVA4RC:jPh?=
macrophages Mn;WRY51cX[rcnHsJIFkfGm4aYT5JIF{e2G7 NXTle4pCPDhiaB?= NELJOpdGSzVyIE2gNE4xQDZizszN NUHUVXZpRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMki3PVI4PjNpPkK4O|kzPzZ|PD;hQi=>
HeLa MXXBcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? MnTvOFghcA>? NWnLO21OTUN3MDC9JFAvOSEQvF2= MUi8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8zQDF{NEmwO{c,OjhzMkS5NFc9N2F-
HeLa MXHBcpRqfmm{YXygZYN1cX[rdImgZZN{[Xl? M2fGR|Q5KGh? NYnMcnFWTUN3MDC9JFAvOTRizszN MmnaQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOjh5OUK3OlMoRjJ6N{myO|Y{RC:jPh?=
MT4 Mn7KR5l1d3SxeHnjbZR6KGG|c3H5 NHHmb3k1KHSxIEWg[IF6ew>? MljqR2M2OCB;IEGuO{DPxE1? NYD4WFI1RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNlQ6ODdpPkK4NVI1QTB5PD;hQi=>
Hep2 MUPDfZRwfG:6aXPpeJkh[XO|YYm= MVS0JJRwKDViZHH5dy=> NVrnfIlyS0N3MDC9JFYvOSEQvF2= NWHIepNrRGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxMkixNlQ6ODdpPkK4NVI1QTB5PD;hQi=>
HuH7 M4TOe2N6fG:2b4jpZ4l1gSCjc4PhfS=> M3HTNFMh\GG7cx?= NFXFNnZESzVyIE2gN|Yh|ryP NEO0eWU9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9{OEGyOFkxPyd-MkixNlQ6ODd:L3G+

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アッセイ
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
体内試験

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]

お薦めの試験操作(参考用のみ)

動物試験:

[1]

- 合併
  • 動物モデル: Rhesus monkeys (Macaca mulatta)
  • 投薬量: 3 mg / kg, 10 mg / kg
  • 投与方法: IV
    (参考用のみ)

溶解度 (25°C)

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

* 溶解度測定はSelleck技術部門によって行われており、その他文献に示されている溶解度と差異がある可能性がありますが、同一ロットの生産工程で起きる正常な現象ですからご安心ください。

化学情報

分子量 602.58
化学式

C27H35N6O8P

CAS No. 1809249-37-3
Storage powder
in solvent
別名 N/A
Smiles CCC(CC)COC(=O)C(C)NP(=O)(OCC1C(C(C(O1)(C#N)C2=CC=C3N2N=CN=C3N)O)O)OC4=CC=CC=C4

投与溶媒組成計算器(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)
投与量 mg/kg 動物平均体重 g 投与体積(動物毎) ul 動物数
ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)
% DMSO % % Tween 80 % ddH2O
計算リセット

便利ツール

モル濃度計算器

モル濃度計算器

求めたい質量、体積または濃度を計算してください。

質量 (mg) = 濃度 (mM) x 体積 (mL) x 分子量 (g/mol)

モル濃度計算器方程式

  • 質量
    濃度
    体積
    分子量

*貯蔵液を準備するとき、常に、オンであるとわかる製品のバッチに特有の分子量を使って、を通してラベルとSDS/COA(製品ページで利用可能な)。

希釈計算器

希釈計算器

貯蔵液を準備するために必要な希釈率を計算してください。Selleck希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積

希釈の計算式

この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 入力 出力 )

  • C1
    V1
    C2
    V2

常に貯蔵液を準備するとき、小びんラベルとSDS/COA(オンラインで利用できる)で見つかる製品のバッチに特有の分子量を使ってください。

連続希釈計算器方程式

  • 連続希釈剤

  • 計算結果

  • 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):
分子量計算器

分子量计算器

そのモル質量と元素組成を計算するために、合成物の化学式を入力してください:

総分子量:g/mol

チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2

モル濃度計算器

質量 濃度 体積 分子量

臨床試験

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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Handling Instructions

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細胞株 試験類型 濃度 培養時間 溶剤類型 活性叙述 PMID