Molnupiravir (EIDD-2801)

製品コードS8969 バッチS896904

印刷

化学情報

Synonyms

MK-4482

Storage
(From the date of receipt)

3 years -20°C powder

化学式

C₁₃H₁₉N₃O₇

分子量

329.31

CAS No.

2349386-89-4

Solubility (25°C)*

体外

DMSO

66 mg/mL (200.41 mM)

Water

66 mg/mL (200.41 mM)

Ethanol

66 mg/mL (200.41 mM)

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.
	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	3.300mg/ml (10.02mM)
	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.330mg/ml (1.00mM)

* <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	Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N⁴-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19.
in vitro	Molnupiravir (EIDD-2801) is an orally bioavailable NHC-prodrug. This compound is potently antiviral against SARS-CoV-2, MERS-CoV and SARS-CoV in primary human epithelial cell cultures without cytotoxicity. It is effective against remdesivir (RDV)-resistant vi-rus and multiple distinct zoonotic CoV. Its antiviral activity is associated with increased viral mutation rates.^[1]
in vivo	Molnupiravir (EIDD-2801) is efficiently hydrolyzed in vivo after absorption, resulting in detection of only free NHC in plasma.^[2] This compound is potently antiviral against SARS-CoV in vivo but the degree of clinical benefit is dependent on the time of initiation post-infection. It robustly reduces MERS-CoV infectious titers, viral RNA, and pathogenesis under both prophylactic and early therapeutic conditions.^[1]

製品説明

Molnupiravir (EIDD-2801, MK-4482) is an orally bioavailable prodrug of the ribonucleoside analog β-d-N⁴-hydroxycytidine (NHC; EIDD-1931) with broad-spectrum antiviral activity against SARS-CoV-2, MERS-CoV, SARS-CoV, and the causative agent of COVID-19.

in vitro

Molnupiravir (EIDD-2801) is an orally bioavailable NHC-prodrug. This compound is potently antiviral against SARS-CoV-2, MERS-CoV and SARS-CoV in primary human epithelial cell cultures without cytotoxicity. It is effective against remdesivir (RDV)-resistant vi-rus and multiple distinct zoonotic CoV. Its antiviral activity is associated with increased viral mutation rates.^[1]

in vivo

Molnupiravir (EIDD-2801) is efficiently hydrolyzed in vivo after absorption, resulting in detection of only free NHC in plasma.^[2]

This compound is potently antiviral against SARS-CoV in vivo but the degree of clinical benefit is dependent on the time of initiation post-infection. It robustly reduces MERS-CoV infectious titers, viral RNA, and pathogenesis under both prophylactic and early therapeutic conditions.^[1]

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Huh-7 & Caco-2 cells
	濃度	IC50 values of 2.84, 25.4, and 1.62 µM for hCoV-229E, -NL63, and -OC43, respectively
	反応時間	7 days
	実験の流れ
動物実験	動物モデル	20-29 week old SPF C57BL/6J mice, 10-14 week old C57BL/6J hDPP4 mice
	投薬量	50 mg/kg, 150 mg/kg, 500 mg/kg
	投与方法	Oral gavage

参考

https://pubmed.ncbi.nlm.nih.gov/32253226/
https://pubmed.ncbi.nlm.nih.gov/31645453/
https://pubmed.ncbi.nlm.nih.gov/35598779/

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：

Selective Inhibition of Vascular Smooth Muscle Cell Function by COVID-19 Antiviral Drugs: Impact of Heme Oxygenase-1 [ Antioxidants (Basel), 2025, 14(8)945]	PubMed: 40867841
Possible involvement of neuropeptide Y sub-receptor 1 (NPY-Y1) in the anti-viral response of SARS-CoV-2 infection in Syrian hamster [ Biomed Res, 2025, 46(2):37-50]	PubMed: 40189329
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
Clinical efficacy of Fufang Yinhua Jiedu (FFYH) granules in mild COVID-19 and its anti-SARS-CoV-2 mechanism by blocking autophagy through inhibiting the AKT/mTOR signaling pathway [ Front Pharmacol, 2024, 15:1431617]	PubMed: 39351097
Exploring the therapeutic potential of Thai medicinal plants: in vitro screening and in silico docking of phytoconstituents for novel anti-SARS-CoV-2 agents [ BMC Complement Med Ther, 2024, 24(1):274]	PubMed: 39030504
A bat MERS-like coronavirus circulates in pangolins and utilizes human DPP4 and host proteases for cell entry [ Cell, 2023, 186(4):850-863.e16]	PubMed: 36803605
Preclinical development of kinetin as a safe error-prone SARS-CoV-2 antiviral able to attenuate virus-induced inflammation [ Nat Commun, 2023, 14(1):199]	PubMed: 36639383
Efferocytosis of SARS-CoV-2-infected dying cells impairs macrophage anti-inflammatory functions and clearance of apoptotic cells [ Elife, 2022, 11e74443]	PubMed: 35666101
Immunodetection assays for the quantification of seasonal common cold coronaviruses OC43, NL63, or 229E infection confirm nirmatrelvir as broad coronavirus inhibitor [ Antiviral Res, 2022, 203:105343]	PubMed: 35598779
In vitro and in vivo efficacy of a novel nucleoside analog H44 against Crimean-Congo hemorrhagic fever virus [ Antiviral Res, 2022, 199:105273]	PubMed: 35257725

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。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。