GC376

製品コードS0475 バッチS047502

化学情報

	Synonyms	N/A	Storage (From the date of receipt)	3 years -20°C powder
	化学式	C₂₁H₃₀N₃NaO₈S
	分子量	507.53	CAS No.	1416992-39-6
Solubility (25°C)*	体外	DMSO	100 mg/mL (197.03 mM)
		Ethanol	100 mg/mL (197.03 mM)
		Water	Insoluble
* <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	GC376 is a 3CLpro (3C-like protease) inhibitor with IC50 of ~ 1.11 μM for the PEDV 3CLpro. GC376 is active against the 3CLpro of multiple coronaviruses, including SARS-CoV.
in vitro	Molnupiravir and GC376 show a synergistic activity on SARS-CoV-2 at 48 h, and an additive activity on SARS-CoV-2 at 72 h.^[2]
in vivo	GC376, a dipeptidyl bisulfite adduct salt, is a 3CLpro (3C-like protease) inhibitor that exerts strong inhibitory effects on picornaviruses and coronaviruses, including SARS-CoV.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	Vero E6 cells
	濃度	0.21-16.7 μM
	反応時間	48 and 72 h
	実験の流れ	Vero E6 cells (3000 cells/well) were seeded in 96-well clear flat-bottom plates and incubated at 37°C with 5% CO₂ for 24 h. After incubation, cells were infected using a multiplicity of infection (MOI) of 0.1. SARS-CoV-2 was allowed to adsorb for one hour at 37°C. Subsequently, virus inoculum was removed, and cells were overlaid with media containing 3-fold serial dilutions of molnupiravir (0.62-50 μM), nirmatrelvir (0.62-50 μM) and GC376 (0.21-16.7 μM). Negative controls (compounds alone), infected positive controls (SARS-CoV-2 alone) and mock-infected cells were included in each plate. Plates were incubated at 37°C with 5% CO₂ for 48 and 72 h and then, cell viability was measured using an MTT reduction assay. (Data sourced from selleck products)
動物実験	動物モデル	Female BALB/c mice
	投薬量	111 or 55.5 mg/kg
	投与方法	i.m.

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：

Enterovirus D68 3C protease antagonizes type I interferon signaling by cleaving signal transducer and activator of transcription 1 [ J Virol, 2024, 98(2):e0199423]	PubMed: 38240591
An RNA replicon system to investigate promising inhibitors of feline coronavirus [ J Virol, 2024, e0121623.]	PubMed: 38236006
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
Insights into the mechanism of SARS-CoV-2 main protease autocatalytic maturation from model precursors [ Commun Biol, 2023, 10.1038/s42003-023-05469-8]	PubMed: 37957287
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int J Mol Sci, 2023, 24(7)6062]	PubMed: 37047038
Stabilization of the Dimeric State of SARS-CoV-2 Main Protease by GC376 and Nirmatrelvir [ Int. J. Mol. Sci, 2023, 10.3390/ijms24076062]	PubMed: None
Enterovirus D68 Infection Induces TDP-43 Cleavage, Aggregation, and Neurotoxicity [ J Virol, 2023, 97(4):e0042523]	PubMed: 37039659
Lichen or Associated Micro-Organism Compounds Are Active against Human Coronaviruses [ Viruses, 2023, 15(9)1859]	PubMed: 37766264
Construction and characterization of two SARS-CoV-2 minigenome replicon systems [ J Med Virol, 2022, 10.1002/jmv.27650]	PubMed: 35137972
Modulation of the monomer-dimer equilibrium and catalytic activity of SARS-CoV-2 main protease by a transition-state analog inhibitor [ Commun Biol, 2022, 5(1):160]	PubMed: 35233052

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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