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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 Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $81 | In Stock | |
| 5 mg | $197 | In Stock | |
| 10 mg | $278 | In Stock | |
| 25 mg | $493 | In 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 |
| 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 | RGS4:17 nM, RGS19:140 nM, RGS8:79 μM, GSK-3β:5.4 μM, RGS16:6 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]. |
| Synonyms | Thiadiazolidinone (TDZD) deriv. 6, RGS4 inhibitor 11b, 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione |
| Molecular Weight | 202.27 |
| Formula | C8H14N2O2S |
| Cas No. | 410074-60-1 |
| Smiles | CCCCn1c(=O)sn(CC)c1=O |
| Relative Density. | 1.179 g/cm3 (Predicted) |
| Color | Transparent |
| Appearance | Liquid |
| Storage | Pure 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
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