| Bioactivity | GC376 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. |
| 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) |
| Invitro | GC376 分别与 NV 3CLpro、PV 3Cpro 和 TGEV 3CLpro 的 Cys 139、Cys 147 和 Cys 144 共价结合。GC376 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 不太敏感，IC50 为 35 μM。GC376 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 抑制。GC376 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 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 交叉抗性[3]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> GC376 sodium 相关抗体: |
| In Vivo | GC376 在猫中表现出良好的生物利用度和安全性。GC376 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 (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 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. |
| CAS | 1416992-39-6 |
| Formula | C21H30N3NaO8S |
| Molar Mass | 507.53 |
| Appearance | 固体 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, stored under nitrogen *In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen) |
| Reference | [1]. Kim Y, et al. Broad-spectrum antivirals against 3C or 3C-like proteases of picornaviruses, noroviruses, and coronaviruses. J Virol. 2012 Nov;86(21):11754-62. [2]. Takahashi D, et al. Structural and inhibitor studies of norovirus 3C-like proteases. Virus Res. 2013 Dec 26;178(2):437-44. [3]. Yunjeong Kim, et al. Reversal of the Progression of Fatal Coronavirus Infection in Cats by a Broad-Spectrum Coronavirus Protease Inhibitor. PLoS Pathog. 2016 Mar 30;12(3):e1005531. [4]. Pedersen NC, et al. Efficacy of a 3C-like protease inhibitor in treating various forms of acquired feline infectious peritonitis. J Feline Med Surg. 2017 Sep 1:1098612X17729626. |
GC376 sodium
CAS: 1416992-39-6 F: C21H30N3NaO8S W: 507.53
GC376 is a 3CLpro inhibitor; inhibits the replication of viruses TGEV, FIPV and PTV with IC50 values of 0.15, 0.2 and 0.
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