產(chǎn)品描述: | GC376 是一種 3CLpro (3C-like protease) 的抑制劑,對于PEDV 3CLpro的IC50值約為1.11 μM。GC376 對多種冠狀病毒(包括SARS-CoV)的3CLpro有活性 |
靶點: |
PEDV 3CLpro(Cell-free assay):1.11 μM;SARS-CoV |
體外研究: |
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 |
體內(nèi)研究: |
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. |
細(xì)胞實驗: |
Cell lines: Vero E6 cells Concentrations: 0.21-16.7 μM Incubation Time: 48 and 72 h Method: 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. |
動物實驗: |
Animal Models: Female BALB/c mice Dosages: 111 or 55.5 mg/kg Administration: i.m. |
參考文獻: |
1. Gang Ye, et al. Structural Basis for Inhibiting Porcine Epidemic Diarrhea Virus Replication with the 3C-Like Protease Inhibitor GC376. Viruses. 2020 Feb 21;12(2):240. 2. Gidari A, et al. The Combination of Molnupiravir with Nirmatrelvir or GC376 Has a Synergic Role in the Inhibition of SARS-CoV-2 Replication In Vitro. Microorganisms. 2022 Jul 21;10(7):1475. 3. Shi Y, et al. The preclinical inhibitor GS441524 in combination with GC376 efficaciously inhibited the proliferation of SARS-CoV-2 in the mouse respiratory tract. Emerg Microbes Infect. 2021 Dec;10(1):481 |
溶解性: |
Soluble in DMSO、Ethanol |
保存條件: |
-20℃,充氮保存 |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
1.97 ml |
9.852 ml |
19.703 ml |
5 mM |
0.394 ml |
1.97 ml |
3.941 ml |
10 mM |
0.197 ml |
0.985 ml |
1.97 ml |
50 mM |
0.039 ml |
0.197 ml |
0.394 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |