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GC376 sodium

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Catalog No. T5188Cas No. 1416992-39-6

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

GC376 sodium

GC376 sodium

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🥰Excellent
Purity: 98%
Catalog No. T5188Cas No. 1416992-39-6
GC376 is an inhibitor of 3C-like proteases (3CLpro) with IC50 values range from 0.49~4.35 μM.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
10 mg$30In StockIn Stock
25 mg$40In StockIn Stock
50 mg$68In StockIn Stock
100 mg$123In StockIn Stock
1 mL x 10 mM (in DMSO)$39In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98%
Color:White
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Product Introduction

Bioactivity
Description
GC376 is an inhibitor of 3C-like proteases (3CLpro) with IC50 values range from 0.49~4.35 μM.
Targets&IC50
3CLpro:0.49~4.35 μM.
In vitro
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].
In vivo
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].
Cell Research
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].
Animal Research
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].
Chemical Properties
Molecular Weight507.53
FormulaC21H30N3NaO8S
Cas No.1416992-39-6
Smiles[Na+].[H][C@@](CC1CCNC1=O)(NC(=O)[C@H](CC(C)C)NC(=O)OCc1ccccc1)C(O)S([O-])(=O)=O
Relative Density.no data available
Storage & Solubility Information
Storagestore under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (88.66 mM), Sonication is recommended.
In Vivo Formulation
5% DMSO+95% Saline: 2.25 mg/mL (4.43 mM), Solution.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9703 mL9.8516 mL19.7033 mL98.5163 mL
5 mM0.3941 mL1.9703 mL3.9407 mL19.7033 mL
10 mM0.1970 mL0.9852 mL1.9703 mL9.8516 mL
20 mM0.0985 mL0.4926 mL0.9852 mL4.9258 mL
50 mM0.0394 mL0.1970 mL0.3941 mL1.9703 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

Keywords

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