Remdesivir [1809249-37-3]

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Remdesivir (GS-5734), un analogue nucléosidique avec une activité antivirale efficace, a des EC50s de 74 nM pour SARS-CoV et MERS-CoV dans les cellules AOH et 30 nM pour le virus de l'hépatite murine dans les cellules tumorales cérébrales retardées. Remdesivir est très efficace dans le contrôle de l’infection par le SRAS-CoV-2 (COVID-19) in vitro.

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.

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Remdesivir Chemical Structure

Remdesivir Chemical Structure

CAS No. : 1809249-37-3

This product is a controlled substance and not for sale in your territory.

Based on 161 publication(s) in Google Scholar

Other Forms of Remdesivir:

  • GS-441524 Obtenir un devis
  • Remdesivir-d5 Obtenir un devis
  • Remdesivir-d4 Obtenir un devis
  • Remdesivir impurity 9-d4 Obtenir un devis
  • GS-443902 Obtenir un devis
  • Remdesivir-13C6 Obtenir un devis
  • Remdesivir maleate Obtenir un devis
  • Remdesivir (Standard) Obtenir un devis
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]

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.

Essai clinique
Masse moléculaire

602.58

Formule

C27H35N6O8P

CAS No.

1809249-37-3

Appearance

Solid

Color

Off-white to yellow

SMILES

C[C@H](N[P@@](OC1=CC=CC=C1)(OC[C@H]2O[C@@](C#N)(C3=CC=C4C(N)=NC=NN43)[C@H](O)[C@@H]2O)=O)C(OCC(CC)CC)=O

Livraison

Room temperature in continental US; may vary elsewhere.

Stockage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
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
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.

  • Calculateur de molarité

  • Calculateur de dilution

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureté et documentation

Purity: 99.95%

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]

  • [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.

    [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.

    [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.

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.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6595 mL 8.2977 mL 16.5953 mL 41.4883 mL
5 mM 0.3319 mL 1.6595 mL 3.3191 mL 8.2977 mL
10 mM 0.1660 mL 0.8298 mL 1.6595 mL 4.1488 mL
15 mM 0.1106 mL 0.5532 mL 1.1064 mL 2.7659 mL
20 mM 0.0830 mL 0.4149 mL 0.8298 mL 2.0744 mL
25 mM 0.0664 mL 0.3319 mL 0.6638 mL 1.6595 mL
30 mM 0.0553 mL 0.2766 mL 0.5532 mL 1.3829 mL
40 mM 0.0415 mL 0.2074 mL 0.4149 mL 1.0372 mL
50 mM 0.0332 mL 0.1660 mL 0.3319 mL 0.8298 mL
60 mM 0.0277 mL 0.1383 mL 0.2766 mL 0.6915 mL
80 mM 0.0207 mL 0.1037 mL 0.2074 mL 0.5186 mL
100 mM 0.0166 mL 0.0830 mL 0.1660 mL 0.4149 mL
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Remdesivir Related Classifications

  • Cell Cycle/DNA Damage Anti-infection
  • DNA/RNA Synthesis SARS-CoV
Help & FAQs

Keywords:

Remdesivir1809249-37-3GS-5734GS5734GS 5734DNA/RNA SynthesisSARS-CoVSARS coronavirusantiviralMERS-CoV2019-nCoVCOVID-19infectionInhibitorinhibitorinhibit

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