1. Anti-infection
  2. SARS-CoV
  3. GC-78-HCl

GC-78-HCl 是一种具有口服活性的、非多肽的 SARS-CoV-2 Mpro 抑制剂,酶的IC50 为 0.19 μM。GC-78-HCl 具有良好的抗冠状病毒活性和药代动力学特性。

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GC-78-HCl Chemical Structure

GC-78-HCl Chemical Structure

CAS No. : 3022242-53-8

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GC-78-HCl is an orally and nonpeptidic SARS-CoV-2 Mpro inhibitor, with an IC50 of 0.19 μM for enzyme. GC-78-HCl has excellent antiviral activity and favorable pharmacokinetic properties[1].

IC50 & Target

EC50 Tatget: SARS-CoV[1] EC50: 0.40 μM (SARS-CoV-2), 0.21 ± 0.030 μM (wild-type), 0.21 ± 0.080 μM (Alpha), 0.24 ± 0.080 μM (Delta), 0.25 ± 0.060 μM (Omicron B.1)[1]

体外研究
(In Vitro)

GC-78-HCl (0.01-10 μM) 在 Vero E6 细胞中具有低细胞毒性[1]
GC-78-HCl 在 MRC-5 和 Vero E6 细胞中对 SARS-CoV-2 变体及人类其他冠状病毒表现出有效的抗病毒活性,表明其具有潜在的广谱抗冠状病毒活性[1]
GC-78-HCl (50 μM) 对人组织蛋白酶 B、F、K、L 和 Caspase 3 无抑制活性,表明对冠状病毒蛋白酶具有很高的靶向特异性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

GC-78-HCl (800 mg/kg, 口服, 单独给药) 对Kunming 小鼠无急性毒性[1]

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Sprague−Dawley rats[1]
Dosage: 2 mg/kg
Administration: Intravenous injection (i.v.)
Result: With the clearance rate (CL) of 4343 mL/h/kg.
With half-life (t1/2) of 0.46 h.
Animal Model: Sprague−Dawley rats[1]
Dosage: 10 mg/kg
Administration: Oral gavage (p.o.)
Result: With half-life (t1/2) of 1.64 h.
With time-to-maximum concentration (Tmax) of 1.17 h.
With maximum concentration (Cmax) of 148 ng/mL.
With an area under curve (AUC0‑t) of 465 ng•h/mL.
Animal Model: Kunming rats[1]
Dosage: 800 mg/kg
Administration: Oral gavage (p.o.)
Result: Exhibited no significant change in mice weight.
分子量

551.85

Formula

C25H25Cl3N4O4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献

GC-78-HCl 相关分类

  • 摩尔计算器

  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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GC-78-HCl
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HY-149774
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