GC376

製品コードS0475 バッチS047502

印刷

化学情報

Chemical Structure 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
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 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 this compound (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

  • https://pubmed.ncbi.nlm.nih.gov/32098094/
  • https://pubmed.ncbi.nlm.nih.gov/35889194/
  • https://pubmed.ncbi.nlm.nih.gov/33691601/

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：

Differential tropisms of old and new world hantaviruses influence virulence and developing host-directed antiviral candidates [ PLoS Pathog, 2025, 21(8):e1013401] PubMed: 40857262
Characterization of an unusual SARS-CoV-2 main protease natural variant exhibiting resistance to nirmatrelvir and ensitrelvir [ Commun Biol, 2025, 8(1):1061] PubMed: 40676153
Cullin 3-mediated ubiquitination restricts enterovirus D68 replication and is counteracted by viral protease 3C [ J Virol, 2025, 99(6):e0035425] PubMed: 40396757
Development of a Biosafety Level 1 Cellular Assay for Identifying Small-Molecule Antivirals Targeting the Main Protease of SARS-CoV-2: Evaluation of Cellular Activity of GC376, Boceprevir, Carmofur, Ebselen, and Selenoneine [ Int J Mol Sci, 2024, 25(11)5767] PubMed: 38891954
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
An efficient trans complementation system for in vivo replication of defective poliovirus mutants [ J Virol, 2024, 98(7):e0052324] PubMed: 38837378
Design of novel and highly selective SARS-CoV-2 main protease inhibitors [ Antimicrob Agents Chemother, 2024, 68(10):e0056224] PubMed: 39225484
Characterization of alternate encounter assemblies of SARS-CoV-2 main protease [ J Biol Chem, 2024, S0021-9258(24)02176-8] PubMed: 39128719
SARS-CoV-2 Mpro inhibitor identification using a cellular gain-of-signal assay for high-throughput screening [ SLAS Discov, 2024, S2472-5552(24)00043-1] PubMed: 39173830

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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