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GC376 sodium

产品编号 T5188 CAS 1416992-39-6

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

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GC376 sodium, CAS 1416992-39-6

规格	价格/CNY	货期
1 mg	￥ 339	现货
5 mg	￥ 792	现货
10 mg	￥ 1,170	现货
25 mg	￥ 1,800	现货
50 mg	￥ 2,780	现货
100 mg	￥ 3,970	现货
500 mg	￥ 8,590	现货
1 mL * 10 mM (in DMSO)	￥ 897	现货

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纯度: 95%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	GC376 is an inhibitor of 3C-like proteases (3CLpro) with IC50 values range from 0.49~4.35 μM.
靶点活性	3CLpro: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].

化合物与蛋白结合的复合物	Complex structure of PEDV 3CLpro with GC376
分子量	507.53
分子式	C21H30N3NaO8S
CAS No.	1416992-39-6

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 45 mg/mL (88.66 mM)

溶液配制表

可选溶剂	浓度体积质量	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.9703 mL	9.8516 mL	19.7033 mL	49.2582 mL
	5 mM	0.3941 mL	1.9703 mL	3.9407 mL	9.8516 mL
	10 mM	0.197 mL	0.9852 mL	1.9703 mL	4.9258 mL
	20 mM	0.0985 mL	0.4926 mL	0.9852 mL	2.4629 mL
	50 mM	0.0394 mL	0.197 mL	0.3941 mL	0.9852 mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

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. Pedersen NC, et al. Efficacy of a 3C-like protease inhibitor in treating various forms of acquired feline infectious peritonitis. J Feline Med Surg. 2018 Apr;20(4):378-392. 3. Theerawatanasirikul S, Kuo C J, Phecharat N, et al. Structural-based virtual screening and in vitro assays for small molecules inhibiting the feline coronavirus 3CL protease as a surrogate platform for coronaviruses[J]. Antiviral research,. 2020, 182: 104927. 4. Wang Y C, Yang W H, Yang C S, et al. Structural basis of SARS-CoV-2 main protease inhibition by a broad-spectrum anti-coronaviral drug[J]. American Journal of Cancer Research. 2020, 10(8): 2535. 5. Fu L, Ye F, Feng Y, et al. Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. Nature communications. 2020, 11(1): 1-8.

文献引用

1. Hahn F, Wangen C, Häge S, et al.The Trimeric Artesunate Analog TF27, a Broadly Acting Anti-Infective Model Drug, Exerts Pronounced Anti-SARS-CoV-2 Activity Spanning Variants and Host Cell Types.Pharmaceutics.2022, 15(1): 115. 2. Mohseni N, Royster A, Ren S, et al.A novel compound targets the feline infectious peritonitis virus nucleocapsid protein and inhibits viral replication in cell culture.Journal of Biological Chemistry.2023: 102976. 3. Ye X, Li Y, Guo L, et al.Synthesis and enzymatic inhibition effects of thiazolidinedione 3C-like protease inhibitors.Journal of Chemical Research.2023, 47(1): 17475198231152556. 4. Bai Y, Ye F, Feng Y, et al. Structural basis for the inhibition of the SARS-CoV-2 main protease by the anti-HCV drug narlaprevir. Signal Transduction and Targeted Therapy. 2021, 6(1): 1-3 5. Theerawatanasirikul S, Kuo C J, Phecharat N, et al. Structural-based virtual screening and in vitro assays for small molecules inhibiting the feline coronavirus 3CL protease as a surrogate platform for coronaviruses. Antiviral research, 2020, 182: 104927. 6. Herrmann A, Jungnickl D, Cordsmeier A, et al. Cloning of a Passage-Free SARS-CoV-2 Genome and Mutagenesis Using Red Recombination. International Journal of Molecular Sciences. 2021, 22(19): 10188. 7. Wang Y C, Yang W H, Yang C S, et al. Structural basis of SARS-CoV-2 main protease inhibition by a broad-spectrum anti-coronaviral drug. American Journal of Cancer Research. 2020, 10(8): 2535 8. Fu L, Ye F, Feng Y, et al Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. Nature communications. 2020 Sep 4;11(1):4417. doi: 10.1038/s41467-020-18233-x. 9. Chen Y, Li X, Wang M, et al.A cysteine protease inhibitor GC376 displays potent antiviral activity against coxsackievirus infection.Current Research in Microbial Sciences.2023: 100203.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

GC376 sodium 1416992-39-6 Microbiology/Virology SARS-CoV GC-376 sodium Inhibitor inhibitor inhibit

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GC376 sodium

存储

溶解度

溶液配制表

计算器

输入分子式，点击计算，可计算出产品的分子量。

参考文献

文献引用

相关产品

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剂量换算

体内实验配液计算器

技术支持

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