Remdesivir (GS-5734) [1809249-37-3]
Référence B8398-5
Conditionnement : 5mg
Marque : APExBIO Technology
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Remdesivir (GS-5734)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Remdesivir (GS-5734) is an antiviral nucleoside analogue that inhibits murine hepatitis virus (MHV) with similar EC50 as SARS-CoV and MERS-CoV.
Coronaviruses (CoVs) are positive-sense, single-stranded RNA viruses that infect a wide range of animal hosts. In humans, CoVs were recognized as typically causing colds and pneumonia until the emergence of severe acute respiratory syndrome coronavirus (SARS-CoV) in 2002 and Middle East respiratory syndrome coronavirus (MERS-CoV) in 2012 from zoonotic sources.
GS-5734 is the monophosphoramidate prodrug of the C-adenosine nucleoside analogue GS-441524. In delayed brain tumor (DBT) cells infected with MHV, GS-5734 inhibited MHV more potently than GS-441524, with a GS-5734 EC50 of 0.03 μM. Furthermore, EC50 values were determined after treatment with GS-441524 and GS-5734 in SARS-CoV- and MERS-CoV-infected primary human airway epithelial cell (HAE) cultures. Mean EC50 values for both viruses were approximately 0.86 μM for GS-441524 and 0.074 μM for GS-5734.
In vivo, GS-5734-resistant SARS-CoV is attenuated in its ability to cause disease and replicates less efficiently than WT virus in robust mouse models of human SARS-CoV disease. Moreover, Remdesivir (GS-5734) is in clinical trail for the treatment of people with Ebola Virus disease.
Reference:
Agostini ML, Andres EL, Sims AC, Graham RL, Sheahan TP, Lu X, Smith EC, Case JB, Feng JY, Jordan R, Ray AS, Cihlar T, Siegel D, Mackman RL, Clarke MO, Baric RS, Denison MR. Coronavirus Susceptibility to the Antiviral Remdesivir (GS-5734) Is Mediated by the Viral Polymerase and the Proofreading Exoribonuclease. mBio. 2018 Mar 6;9(2). PMID: 29511076.
| Storage | Store at -20°C |
| M.Wt | 602.58 |
| Cas No. | 1809249-37-3 |
| Formula | C27H35N6O8P |
| Solubility | insoluble in H2O; insoluble in EtOH; ≥51.4 mg/mL in DMSO |
| Chemical Name | 2-ethylbutyl ((((2R,3S,4R,5R)-5-(4-aminopyrrolo[2,1-f][1,2,4]triazin-7-yl)-5-cyano-3,4-dihydroxytetrahydrofuran-2-yl)methoxy)(phenoxy)phosphoryl)-L-alaninate |
| SDF | Download SDF |
| Canonical SMILES | NC1=NC=NN2C1=CC=C2[C@@]3(C#N)[C@H](O)[C@H](O)[C@@H](COP(OC4=CC=CC=C4)(N[C@@H](C)C(OCC(CC)CC)=O)=O)O3 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
| Cell experiment:[1] | |
| Cell lines | Murine astrocytoma delayed brain tumor (DBT) cells |
| Reaction Conditions | 24 h incubation |
| Applications | In DBT cells infected with murine hepatitis virus (MHV), treatment with increasing concentrations of GS-5734 resulted in up to a 6-log10 decrease in viral titer, and virus was undetectable by plaque assay at concentrations above 0.5 μM GS-5734. GS-5734 inhibited MHV more potently than GS-441524, with an EC50 value of 0.03 μM. In addition, GS-5734 only exhibited minimal cytotoxicity within the tested range. |
| Animal experiment:[2] | |
| Animal models | A rhesus monkey model of Ebola virus (EBOV) disease (EVD) |
| Dosage form | 10 mg/kg Once daily by intravenous route for 12 days |
| Applications | GS-5734 resulted in profound suppression of EBOV replication and protected 100% of EBOV-infected animals against lethal disease, ameliorating clinical disease signs and pathophysiological markers, even when treatments were initiated three days after virus exposure when systemic viral RNA was detected in two out of six treated animals. |
| Note | The technical data provided above is for reference only. |
| References: 1. Agostini ML, Andres EL, Sims AC, et al. Coronavirus susceptibility to the antiviral remdesivir (GS-5734) Is mediated by the viral polymerase and the proofreading exoribonuclease. mBio, 2018, 9(2): e00221-18. 2. Warren TK, Jordan R, Lo MK, et al. Therapeutic efficacy of the small molecule GS-5734 against Ebola virus in rhesus monkeys. Nature, 2016, 531(7594): 381-385. | |