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Remdesivir [1809249-37-3]

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Referência HY-104077-5mg

Tamanho : 5mg

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Description

Remdesivir (GS-5734), a nucleoside analogue with effective antiviral activity, has EC₅₀s of 3.3 μM, 4.7 μM, 32 μM, 3.7 μM and 9.2 μM for SARS-CoV-2 and its variants alpha, beta, gamma and delta, respectively. Remdesivir is highly effective in the control of SARS-CoV-2 (COVID-19) infection in vitro^[1]^[2]^[3].

IC₅₀ & Target

EC₅₀: 30 nM (murine hepatitis virus, delayed brain tumor cell), 74 nM (SARS-CoV, HAE cell), 74 nM (MERS-CoV, HAE cell)^[1]
EC₅₀: 3.3 μM (SARS-CoV-2), 4.7 μM (SARS-CoV-2 alpha), 32 μM (SARS-CoV-2 beta), 3.7 μM (SARS-CoV-2 gamma) and 9.2 μM (SARS-CoV-2 delta)^[3]

Cellular Effect

Cell Line	Type	Value	Description	References
16HBE14o-	CC₅₀	41 μM Compound: Remdesivir	Cytotoxicity against human 16HBE14o- after 72 hrs by MTT assay Cytotoxicity against human 16HBE14o- after 72 hrs by MTT assay	[PMID: 34408808]
A549	CC₅₀	43 μM Compound: Remdesivir	Cytotoxicity against human A549 cells overexpressing ACE2 and TMPRSS2 incubated for 48 hrs by MTS assay Cytotoxicity against human A549 cells overexpressing ACE2 and TMPRSS2 incubated for 48 hrs by MTS assay	[PMID: 36097498]
Caco-2	IC₅₀	0.76 μM Compound: REMDESIVIR	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
Caco-2	CC₅₀	2584.38 μM Compound: REMDESIVIR	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	CC₅₀	80 μM Compound: Remdesivir	Cytotoxicity against human Caco2 cells infected with SARS-COV-2 assessed as reduction in cell viability by celltiter-glo luminescent cell viability assay Cytotoxicity against human Caco2 cells infected with SARS-COV-2 assessed as reduction in cell viability by celltiter-glo luminescent cell viability assay	[PMID: 34273661]
Calu-3	CC₅₀	> 100 μM Compound: Remdesivir	Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability incubated for 48 hrs by PrestoBlue reagent based assay Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability incubated for 48 hrs by PrestoBlue reagent based assay	[PMID: 36399766]
Calu-3	CC₅₀	> 50 μM Compound: RDV	Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability after 48 hrs by Cell-Tox green based fluorescence assay Cytotoxicity against human Calu-3 cells assessed as reduction in cell viability after 48 hrs by Cell-Tox green based fluorescence assay	[PMID: 34583312]
Calu-3	CC₅₀	97 μM Compound: Remdesivir	Cytotoxicity against human Calu-3 cells infected with SARS-COV-2 by celltiter-glo luminescent cell viability assay Cytotoxicity against human Calu-3 cells infected with SARS-COV-2 by celltiter-glo luminescent cell viability assay	[PMID: 34273661]
HCT-8	CC₅₀	53.18 μM Compound: Remdesivir	Cytotoxicity against human HCT-8 cells assessed as redcution in cell viability incubated for 96 hrs by PrestoBlue reagent based assay Cytotoxicity against human HCT-8 cells assessed as redcution in cell viability incubated for 96 hrs by PrestoBlue reagent based assay	[PMID: 36399766]
HEK-293T	CC₅₀	> 100 μM Compound: Remdesivir	Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay Cytotoxicity against human HEK293T cells assessed as reduction in cell viability incubated for 24 hrs by CCK8 assay	[PMID: 34147744]
HEL 299	CC₅₀	> 10 μM Compound: Remdesivir	Cytotoxicity against human HEL 299 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter96 Aqueous One Solution cell proliferation assay Cytotoxicity against human HEL 299 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter96 Aqueous One Solution cell proliferation assay	[PMID: 37252100]
HeLa	CC₅₀	> 20 μM Compound: 3; GS-5734	Cytotoxicity against human HeLa after 4 to 5 days by Cell-Titer Glo viability assay Cytotoxicity against human HeLa after 4 to 5 days by Cell-Titer Glo viability assay	[PMID: 28792763]
HeLa	EC₅₀	0.1 μM Compound: 4b	Antiviral activity against Ebolavirus Kikwit infected in human HeLa cells assessed as reduction in viral glycoprotein levels preincubated with cells for 2 hrs followed by viral infection measured after 48 hrs by immunostaining based assay Antiviral activity against Ebolavirus Kikwit infected in human HeLa cells assessed as reduction in viral glycoprotein levels preincubated with cells for 2 hrs followed by viral infection measured after 48 hrs by immunostaining based assay	[PMID: 28124907]
HeLa	EC₅₀	0.14 μM Compound: 3; GS-5734	Antiviral activity against Ebolavirus infected in human HeLa cells after 48 hrs by immuno-staining assay Antiviral activity against Ebolavirus infected in human HeLa cells after 48 hrs by immuno-staining assay	[PMID: 28792763]
HEp-2	IC₅₀	0.11 μM Compound: 1; GS-5734	Drug metabolism in human HEp-2 cells assessed as 1-NTP metabolite concentration at EC50 over 48 hrs by LC-MS/MS analysis Drug metabolism in human HEp-2 cells assessed as 1-NTP metabolite concentration at EC50 over 48 hrs by LC-MS/MS analysis	[PMID: 33835812]
HEp-2	CC₅₀	6.1 μM Compound: 4b	Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay	[PMID: 28124907]
HEp-2	CC₅₀	6.1 μM Compound: 1; GS-5734	Cytotoxicity against human HEp-2 cells assessed as reduction in cell viability incubated for 4 to 5 days by CellTiter Glo viability assay Cytotoxicity against human HEp-2 cells assessed as reduction in cell viability incubated for 4 to 5 days by CellTiter Glo viability assay	[PMID: 33835812]
HepG2	CC₅₀	52.62 μM Compound: Remdesivir	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by PrestoBlue reagent based assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by PrestoBlue reagent based assay	[PMID: 36399766]
Huh-7	CC₅₀	> 10 μM Compound: RDV; GS-5734	Cytotoxicity against human Huh7 cells incubated for 6 days by cellTiter-Glo assay Cytotoxicity against human Huh7 cells incubated for 6 days by cellTiter-Glo assay	[PMID: 32845145]
Huh-7	CC₅₀	> 10 μM Compound: RDV; GS-5734	Cytotoxicity against human Huh-7 cells by CellTiter-Glo assay Cytotoxicity against human Huh-7 cells by CellTiter-Glo assay	[PMID: 32845145]
Huh-7	CC₅₀	> 10 μM Compound: GS-5734; 8b	Cytotoxicity against human Huh-7 cells by celltiter-glo Assay Cytotoxicity against human Huh-7 cells by celltiter-glo Assay	[PMID: 32563812]
Huh-7	CC₅₀	> 10 μM Compound: Remdesivir	Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter96 Aqueous One Solution cell proliferation assay Cytotoxicity against human Huh-7 cells assessed as inhibition of cell growth incubated for 72 hrs by CellTiter96 Aqueous One Solution cell proliferation assay	[PMID: 37252100]
Huh-7	CC₅₀	> 20 μM Compound: 3; GS-5734	Cytotoxicity against human HuH7 after 4 to 5 days by Cell-Titer Glo viability assay Cytotoxicity against human HuH7 after 4 to 5 days by Cell-Titer Glo viability assay	[PMID: 28792763]
Huh-7	CC₅₀	> 50 μM Compound: RDV	Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 24 hrs by CellTiter-Glo analysis Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 24 hrs by CellTiter-Glo analysis	[PMID: 34583312]
Huh-7	CC₅₀	10.37 μM Compound: Remdesivir	Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 24 hrs by Celltiter-glo luminescent cell viability assay Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability incubated for 24 hrs by Celltiter-glo luminescent cell viability assay	[PMID: 34242027]
Huh-7	CC₅₀	36 μM Compound: 4b	Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 3 days by calcein-AM dye based fluorescence assay Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 3 days by calcein-AM dye based fluorescence assay	[PMID: 28124907]
Huh-7	CC₅₀	77 μM Compound: Remdesivir	Cytotoxicity against human Huh-7 cells infected with SARS-COV-2 assessed as reduction in cell viability by celltiter-glo luminescent cell viability assay Cytotoxicity against human Huh-7 cells infected with SARS-COV-2 assessed as reduction in cell viability by celltiter-glo luminescent cell viability assay	[PMID: 34273661]
Macrophage	CC₅₀	> 20 μM Compound: 3; GS-5734	Cytotoxicity against human primary macrophages after 4 to 5 days by Cell-Titer Glo viability assay Cytotoxicity against human primary macrophages after 4 to 5 days by Cell-Titer Glo viability assay	[PMID: 28792763]
MRC5	CC₅₀	> 100 μM Compound: Remdesivir	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 24 hrs by Celltiter-glo luminescent cell viability assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 24 hrs by Celltiter-glo luminescent cell viability assay	[PMID: 34242027]
MRC5	CC₅₀	> 100 μM Compound: Remdesivir	Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 48 hrs by PrestoBlue reagent based assay Cytotoxicity against human MRC5 cells assessed as reduction in cell viability incubated for 48 hrs by PrestoBlue reagent based assay	[PMID: 36399766]
MT4	CC₅₀	1.7 μM Compound: 4b	Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay	[PMID: 28124907]
Vero	CC₅₀	> 100 μM Compound: RDV	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay	[PMID: 36764470]
Vero	CC₅₀	> 100 μM Compound: Remdesivir	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 48 hrs by PrestoBlue reagent based assay Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability incubated for 48 hrs by PrestoBlue reagent based assay	[PMID: 36399766]
Vero	CC₅₀	> 25 μM Compound: Remdesivir	Cytotoxicity against African green monkey Vero cells infected with SARS-CoV-2 betaCoV/KOR/KCDC03/2020 assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay Cytotoxicity against African green monkey Vero cells infected with SARS-CoV-2 betaCoV/KOR/KCDC03/2020 assessed as reduction in cell viability measured after 72 hrs by CellTiter-Glo Luminescent Cell Viability Assay	[PMID: 33160024]
Vero	CC₅₀	> 25 μM Compound: Remdesivir	Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr	10.1101/2020.03.20.999730
Vero	CC₅₀	> 40 μM Compound: Remdesivir	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by coulter counter method Cytotoxicity against African green monkey Vero cells assessed as reduction in cell viability by coulter counter method	[PMID: 34571172]
Vero	CC₅₀	> 40 μM Compound: Remdesivir	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth by coulter counter analysis Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth by coulter counter analysis	[PMID: 33479570]
Vero	IC₅₀	11.41 μM Compound: Remdesivir	Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr	10.1101/2020.03.20.999730
Vero	CC₅₀	70.6 μM Compound: Remdesivir	Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth by Coulter counter analysis Cytotoxicity against African green monkey Vero cells assessed as reduction in cell growth by Coulter counter analysis	[PMID: 36332548]
Vero C1008	CC₅₀	> 100 μM Compound: Remdesivir	Cytotoxicity against african green monkey Vero E6 cells assessed as reduction in cell viability after 26 hrs by MTS assay Cytotoxicity against african green monkey Vero E6 cells assessed as reduction in cell viability after 26 hrs by MTS assay	[PMID: 36475694]
Vero C1008	CC₅₀	> 200 μM Compound: Remdesivir	Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay	[PMID: 34749200]
Vero C1008	EC₅₀	0.62 μM Compound: Remdesivir	Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs	[PMID: 32511357]
Vero C1008	EC₅₀	1.65 μM Compound: Remdesivir	Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days Antiviral efficacy against SARS-CoV-2 (strain BavPat1) in Vero E6 cells assessed by inhibition of viral RNA replication measured by RT-PCR after 2 days	10.1101/2020.04.03.023846
Vero C1008	CC₅₀	100 μM Compound: RDV; GS-5734	Cytotoxicity against African green monkey Vero E6 cells by the CCK8 assay Cytotoxicity against African green monkey Vero E6 cells by the CCK8 assay	[PMID: 32845145]
Vero C1008	CC₅₀	166 μM Compound: Remdesivir	Cytotoxicity against African green monkey Vero E6 cells infected with SARS-COV-2 by celltiter-glo luminescent cell viability assay Cytotoxicity against African green monkey Vero E6 cells infected with SARS-COV-2 by celltiter-glo luminescent cell viability assay	[PMID: 34273661]
Vero C1008	CC₅₀	373 μM Compound: RMV	Cytotoxicity against African green monkey Vero E6 cells assessed as reduction of cell viability measured after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero E6 cells assessed as reduction of cell viability measured after 72 hrs by MTT assay	[PMID: 34534839]
Vero C1008	CC₅₀	608.3 μM Compound: Cpd III	Cytotoxicity against African green monkey Vero E6 cells measured after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero E6 cells measured after 72 hrs by MTT assay	[PMID: 37252103]
Vero C1008	CC₅₀	72 μM Compound: Remdesivir	Cytotoxicity against African green monkey Vero E6 cells after 72 hrs by MTT assay Cytotoxicity against African green monkey Vero E6 cells after 72 hrs by MTT assay	[PMID: 34408808]

In Vitro

Remdesivir (GS-5734) inhibits murine hepatitis virus (MHV) with an EC₅₀ of 30 nM, and blocks SARS-CoV and MERS-CoV in HAE cells with EC₅₀s of both 74 nM in HAE cells after treatment for 24 h^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Solvant et solubilité

In Vitro:

DMSO : 100 mg/mL (165.95 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.6595 mL	8.2977 mL	16.5953 mL
5 mM	0.3319 mL	1.6595 mL	3.3191 mL
10 mM	0.1660 mL	0.8298 mL	1.6595 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.15 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 2

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (3.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.17 mg/mL (3.60 mM); Clear solution

This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 900 μL Corn oil, and mix evenly.

Pureté et documentation

Purity: 99.95%

Fiche technique (275 KB) SDS (557 KB)

COA (250 KB) LCMS (94 KB)

Instruction de manipulation (2659 KB)

Références

[1]. Agostini ML, et al. Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease. MBio. 2018 Mar 6;9(2). pii: e00221-18. [Content Brief]

[2]. Wang M, et al. Remdesivir and chloroquine effectively inhibit the recently emerged novel coronavirus (2019-nCoV) in vitro. Cell Res. 2020 Mar;30(3):269-271. [Content Brief]

[3]. Hu H, et al. Optimization of the Prodrug Moiety of Remdesivir to Improve Lung Exposure/Selectivity and Enhance Anti-SARS-CoV-2 Activity. J Med Chem. 2022 Sep 22;65(18):12044-12054. [Content Brief]

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Remdesivir [1809249-37-3]

Referência HY-104077-5mg

Contactar o distribuidor local :

Marca : MedChemExpress

Contactar o distribuidor local :

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