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GC376 sodium
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
GC376 sodium图片
CAS NO:1416992-39-6
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议

产品介绍
GC376 sodium 是一种 3C 样蛋白酶 (3CLpro) 抑制剂,IC50 值范围为 0.49~4.35 μM。

产品描述

GC376 is an inhibitor of 3C-like proteases (3CLpro) with IC50 values range from 0.49~4.35 μM.

体外活性

GC376 was significantly effective against caliciviruses (NV and MNV-1), coronaviruses (TGEV, FIPV, MHV, 229E, and BCV), and picornaviruses (HRVs 18, 51, and 68, EV71, and PTV), with nanomolar or low micromolar IC50s, except for FCV and HAV. Interestingly, FCV was less sensitive to GC376, with IC50s of 35 μM, respectively [1].

体内活性

GC376 was administered subcutaneously every 12 h at a dose of 15 mg/kg. Results Nineteen of 20 cats treated with GC376 regained outward health within 2 weeks of initial treatment. However, disease signs recurred 1-7 weeks after primary treatment and relapses and new cases were ultimately treated for a minimum of 12 weeks. Relapses no longer responsive to treatment occurred in 13 of these 19 cats within 1-7 weeks of initial or repeat treatment(s) [2].

细胞实验

The toxic dose for 50% cell death (TD50) for each compound was determined for the various cells used in this study. Confluent cells grown in 96-well plates were treated with various concentrations (1 to 500 μM) of each compound for 72 h. Cell cytotoxicity was measured by a CytoTox 96 nonradioactive cytotoxicity assay kit and crystal violet staining. The in vitro therapeutic index was calculated by dividing the TD50 by the IC50 [1].

动物实验

GC376 was synthesized in a highly pure form and formulated at a concentration of 53 mg/ml in 10% ethanol and 90% polyethylene glycol 400, as described previously. GC376 was administered subcutaneously (SC) at a dosage of 15 mg/kg q12h SC, unless stated otherwise. The effective dosage for cats with experimentally induced FIP was 10 mg/kg/ q12h SC, but the dosage was raised to 15 mg/kg after the first cat (CT01) failed to respond to a lower dose of 10 mg/kg suggested by earlier pharmacokinetic studies. This was a clinical decision based on this one cat's response to treatment [2].

Cas No.

1416992-39-6

分子式

C21H30N3NaO8S

分子量

507.53

储存和溶解度

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years