S83222 |
GC376 |
源叶(MedMol) | 98% |
- 产品描述:
GC376 是一种 3CLpro (3C-like protease) 的抑制剂,对于PEDV 3CLpro的IC50值约为1.11 μM。GC376 对多种冠状病毒(包括SARS-CoV)的3CLpro有活性
- 靶点: PEDV 3CLpro(Cell-free assay):1.11 μM;SARS-CoV
- 体外研究:
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
- 体内研究:
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.
- 细胞实验: 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.
- 动物实验: Animal Models: Female BALB/c mice Dosages: 111 or 55.5 mg/kg Administration: i.m.
- 参考文献:
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
- 保存条件: -20℃,充氮保存
- 配置溶液浓度参考:
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
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质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)