| CAS NO: | 1809249-37-3 |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 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 |
| 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 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
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.
| 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-log10decrease 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. | |
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