2. Anti-infection
  3. Virus Protease
  4. GC376 sodium

GC376 sodium 是 3CLpro 的抑制剂，抑制 TGEV，FIPV 和 PTV 病毒复制的 IC50 值分别为 0.15, 0.2 和 0.15 μM。

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GC376 sodium Chemical Structure

GC376 sodium Chemical Structure

CAS No. : 1416992-39-6

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Other Forms of GC376 sodium:

GC376 sodium 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GC376 sodium is a 3CLpro inhibitor; inhibits the replication of viruses TGEV, FIPV and PTV with IC50 values of 0.15, 0.2 and 0.15 μM, respectively.

IC50 & Target

IC50: 0.15 μM (TGEV), 0.2 μM (FIPV), 0.15 μM (PTV), 0.15 μM (229E), 1.1 μM (MHV), 5.3 μM (MNV-1), 0.6 μM (BCV)[1]
体外研究
(In Vitro)

GC376 sodium 分别与 NV 3CLpro、PV 3Cpro 和 TGEV 3CLpro 的 Cys 139、Cys 147 和 Cys 144 共价结合。GC376 sodium 对杯状病毒 (NV 和 MNV-1)、冠状病毒 (TGEV、FIPV、MHV、229E 和 BCV) 和小核糖核酸病毒 (HRV 18、51 和 68、EV71 和 PTV) 显著有效，具有纳摩尔或低微摩尔浓度IC50，FCV 和 HAV 除外。有趣的是，FCV 对 GC376 sodium 不太敏感，IC50 为 35 μM。GC376 sodium 对 HAV 在细胞中的复制没有作用或作用较弱[1]。
来自 NV、MD145 或 MNV-1 的蛋白酶被具有相似效力的 GC376 sodium 抑制。GC376 sodium 对来自 NV、MD145 和 MNV-1 的 3CLpro 的 IC50 值在测试病毒中具有可比性[2]。
GC376 sodium 有效抑制 NPI52 抗性病毒在细胞培养物中作为野生型病毒的复制，表明该突变不赋予 GC376 sodium 交叉抗性[3]。

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

GC376 sodium 相关抗体:
体内研究
(In Vivo)

GC376 sodium 在猫中表现出良好的生物利用度和安全性。GC376 sodium 在皮下给药后被迅速吸收，并在注射后 2 小时内达到峰值血浆水平。注射后 18 小时内，平均血浆药物浓度仍高于醛形式 GC376 sodium (8 ng/mL) 的 50% 有效浓度 (EC50) 值。被病毒感染的猫表现出态度和退烧的改善。在接受抗病毒处理之前，在所有猫身上观察到的严重绝对淋巴细胞减少症也会在一周后的下一次血液检测前恢复正常[3]。接受 GC376 sodium 处理的 20 只猫中有 19 只在初始处理后 2 周内恢复了外在健康。然而，疾病体征在主要处理后 1-7 周复发，新病例最终需要接受至少 12 周的处理[4]。

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

507.53

Formula

C21H30N3NaO8S
CAS 号
性状

固体

颜色

Off-white to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

纯度 & 产品资料

纯度: 99.96%

COA (290 KB) HNMR (228 KB) RP-HPLC (385 KB)

产品使用指南 (1538 KB)
参考文献
Kinase Assay
[2]

The stock solution (10 mM) of GC376 is prepared in DMSO and further diluted in assay buffer. The final concentrations of DMSO in the assay did not exceed 1.5% (vol/vol). The 3CLpro from NV, MD145 or MNV-1 are incubated with various concentrations (0.01 to 50 µM) of GC376 in 25 µL of assay buffer for 30 min at 37 °C. Following incubation, 25 µL of assay buffer containing substrate is added, and the mixtures are incubated in a 96-well black plate at 37 °C for 60 min. The fluorescence signals are detected using an excitation and emission wavelength of 490 and 520 nm on a fluorescence microplate reader. The RFU are calculated for each well, and the dose-dependent FRET inhibition curves are fitted with variable slope (four parameters) using GraphPad Prism software in order to determine the IC50 values of GC376[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[4]

Twenty cats from 3.3-82 months of age (mean 10.4 months) with various forms of feline infectious peritonitis are accepted into a field trial. Fourteen cats presented with wet or dry-to-wet FIP and six cats presented with dry feline infectious peritonitis. GC376 is administered subcutaneously every 12 h at a dose of 15 mg/kg. Cats with neurologic signs are excluded from the study. Responses to treatment are monitored[4].

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

GC376 sodium 相关分类

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  • 稀释计算器

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  • Do most proteins show cross-species activity?

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Keywords:

GC3761416992-39-6GC 376GC-376Virus ProteaseInhibitorinhibitorinhibit

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产品名称：
GC376 sodium
目录号：
HY-100721
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