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CCG 203769

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Catalog No. T10705Cas No. 410074-60-1
Alias Thiadiazolidinone (TDZD) deriv. 6, RGS4 inhibitor 11b, 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione

CCG 203769 (Thiadiazolidinone (TDZD) deriv. 6) is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.

CCG 203769

CCG 203769

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Purity: 99.88%
Catalog No. T10705Alias Thiadiazolidinone (TDZD) deriv. 6, RGS4 inhibitor 11b, 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dioneCas No. 410074-60-1
CCG 203769 (Thiadiazolidinone (TDZD) deriv. 6) is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$81-In Stock
5 mg$197In StockIn Stock
10 mg$278In StockIn Stock
25 mg$493In StockIn Stock
50 mg$692-In Stock
100 mg$993-In Stock
500 mg$1,980-In Stock
1 mL x 10 mM (in DMSO)$217-In Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.88%
Appearance:Liquid
Color:Transparent
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Product Introduction

Bioactivity
Description
CCG 203769 (Thiadiazolidinone (TDZD) deriv. 6) is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.
Targets&IC50
RGS16:6 μM, RGS8:79 μM, RGS4:17 nM, RGS19:140 nM, GSK-3β:5.4 μM
In vitro
CCG 203769 displays dramatic selectivity (8- to >5000-fold) for RGS4 over other RGS proteins with IC50s of 140 nM, 6 μM, and 79 μM for RGS19, RGS16, and RGS8. CCG 203769 inhibits GSK-3β with an IC50 of 5 μM. CCG 203769 enhances Gαq-dependent cellular Ca2+ signaling in an RGS4-dependent manner and inhibits RGS/Gαo binding in an RGS-selective manner. CCG 203769 also blocks the GTPase accelerating protein (GAP) activity of RGS4. CCG 203769 inhibits the effect of GTP hydrolysis stimulated by RGS4 with an IC50<1 μM in single-turnover and steady-state GTPase experiments[1].
In vivo
CCG 203769 (10 mg/kg, i.v.), administered immediately prior to Carbamoylcholine chloride(0.1 mg/kg, i.p.), significantly potentiates the bradycardic effect. CCG 203769 (1-10 mg/kg) reverses the increased hang time caused by raclopride administration in rats. CCG 203769 (0.1-10 mg/kg) reverses the raclopride-induced paw drag in mice[1].
SynonymsThiadiazolidinone (TDZD) deriv. 6, RGS4 inhibitor 11b, 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione
Chemical Properties
Molecular Weight202.27
FormulaC8H14N2O2S
Cas No.410074-60-1
SmilesCCCCn1c(=O)sn(CC)c1=O
Relative Density.1.179 g/cm3 (Predicted)
Storage & Solubility Information
StoragePure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 50 mg/mL (247.19 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (9.89 mM), Sonication is recommended.
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 mM4.9439 mL24.7194 mL49.4389 mL247.1943 mL
5 mM0.9888 mL4.9439 mL9.8878 mL49.4389 mL
10 mM0.4944 mL2.4719 mL4.9439 mL24.7194 mL
20 mM0.2472 mL1.2360 mL2.4719 mL12.3597 mL
50 mM0.0989 mL0.4944 mL0.9888 mL4.9439 mL
100 mM0.0494 mL0.2472 mL0.4944 mL2.4719 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

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