Remdesivir (GS-5734)

製品コードS8932 バッチS893204

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₂₇H₃₅N₆O₈P

分子量

602.58

CAS No.

1809249-37-3

Solubility (25°C)*

体外

DMSO

100 mg/mL (165.95 mM)

Ethanol

16 mg/mL (26.55 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension

CMC-NA

≥5mg/ml

Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

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.
in vitro	Remdesivir (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] This compound 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]
in vivo	Regardless of the time of initiation, treatment with Remdesivir (GS-5734) confers improved survival when administered at 3 mg/kg. All animals in which 10 mg/kg treatment 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 doses. The 10 mg/kg D3 (administered beginning 3 days after virus exposure) regimen is associated with amelioration of EVD-related clinical disease signs and markers of coagulopathy and end organ pathophysiology.^[1]

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.

in vitro

Remdesivir (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]

This compound 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]

in vivo

Regardless of the time of initiation, treatment with Remdesivir (GS-5734) confers improved survival when administered at 3 mg/kg. All animals in which 10 mg/kg treatment 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 doses. The 10 mg/kg D3 (administered beginning 3 days after virus exposure) regimen is associated with amelioration of EVD-related clinical disease signs and markers of coagulopathy and end organ pathophysiology.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HeLa cells
	濃度	0.14 uM
	反応時間	72 h
	実験の流れ	Cells were treated with various concentrations of Remdesivir (GS-5734).
動物実験	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

https://pubmed.ncbi.nlm.nih.gov/26934220/
https://pubmed.ncbi.nlm.nih.gov/29511076/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Exploring the Therapeutic Potential of Cordyceps Mushroom on SARS-CoV-2 Using Virtual Screening against Mpro and In Vitro Validation of Cordycepin [ J Microbiol Biotechnol, 2025, 35:e2411063]	PubMed: 40147924
Design, Synthesis, and Anti-SARS-CoV-2 Activity of Amodiaquine Analogs [ Chem Pharm Bull (Tokyo), 2025, 73(4):355-368]	PubMed: 40240159
Andrographolide attenuates SARS-CoV-2 infection via an up-regulation of glutamate-cysteine ligase catalytic subunit (GCLC) [ Phytomedicine, 2024, 136:156279]	PubMed: 39631298
The host-targeted antiviral drug Zapnometinib exhibits a high barrier to the development of SARS-CoV-2 resistance [ Antiviral Res, 2024, 225:105840]	PubMed: 38438015
Unveiling the Antiviral Properties of Panduratin A through SARS-CoV-2 Infection Modeling in Cardiomyocytes [ Int J Mol Sci, 2024, 25(3)1427]	PubMed: 38338708
Unveiling the Antiviral Properties of Panduratin A through SARS-CoV-2 Infection Modeling in Cardiomyocytes [ Int J Mol Sci, 2024, 24;25(3):1427.]	PubMed: 38338708
Development of a Měnglà virus minigenome and comparison of its polymerase complexes with those of other filoviruses [ Virol Sin, 2024, 39(3):459-468]	PubMed: 38782261
The PKA-CREB1 axis regulates coronavirus proliferation by viral helicase nsp13 association [ J Virol, 2024, 98(4):e0156523]	PubMed: 38445884
Novel Pan-Coronavirus 3CL Protease Inhibitor MK-7845: Biological and Pharmacological Profiling [ Viruses, 2024, 16(7)1158]	PubMed: 39066320
A high-throughput response to the SARS-CoV-2 pandemic [ SLAS Discov, 2024, 29(5):100160]	PubMed: 38761981

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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