Molnupiravir (EIDD-2801)

製品コードS8969 バッチS896901

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)
		Ethanol	22 mg/mL (66.8 mM)
		Water	20 mg/mL (60.73 mM)
* <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	EIDD-2801 is an orally bioavailable NHC-prodrug. NHC is potently antiviral against SARS-CoV-2, MERS-CoV and SARS-CoV in primary human epithelial cell cultures without cytotoxicity. NHC is effective against remdesivir (RDV)-resistant vi-rus and multiple distinct zoonotic CoV. NHC antiviral activity is associated with increased viral mutation rates.^[1]
in vivo	EIDD-2801 is efficiently hydrolyzed in vivo after absorption, resulting in detection of only free NHC in plasma.^[2] Therapeutic EIDD-2801 is potently antiviral against SARS-CoV in vivo but the degree of clinical benefit is dependent on the time of initiation post-infection. EIDD-2801 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

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

in vivo

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

Therapeutic EIDD-2801 is potently antiviral against SARS-CoV in vivo but the degree of clinical benefit is dependent on the time of initiation post-infection. EIDD-2801 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

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：

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
The MEK1/2 Inhibitor ATR-002 (Zapnometinib) Synergistically Potentiates the Antiviral Effect of Direct-Acting Anti-SARS-CoV-2 Drugs [ Pharmaceutics, 2022, 14(9)1776]	PubMed: 36145524
Use of Human Lung Tissue Models for Screening of Drugs against SARS-CoV-2 Infection [ Viruses, 2022, 14(11)2417]	PubMed: 36366514
Integrative multiomics and in silico analysis revealed the role of ARHGEF1 and its screened antagonist in mild and severe COVID-19 patients [ J Cell Biochem, 2022, 10.1002/jcb.30213]	PubMed: 35037717

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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