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CCG 203769

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Purity:99.46%

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COA HNMR HPLC

CCG 203769

Catalog No. T10705Cas 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.

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Pack Size	Price	Availability
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

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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.
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].
Alias	4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione, RGS4 inhibitor 11b, Thiadiazolidinone (TDZD) deriv. 6

Chemical Properties

Molecular Weight	202.27
Formula	C8H14N2O2S
Cas No.	410074-60-1

Storage & Solubility Information

Storage

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

Solubility Information

DMSO: 50 mg/mL (247.2 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	4.9439 mL	24.7194 mL	49.4389 mL	247.1943 mL
5 mM	0.9888 mL	4.9439 mL	9.8878 mL	49.4389 mL
10 mM	0.4944 mL	2.4719 mL	4.9439 mL	24.7194 mL
20 mM	0.2472 mL	1.2360 mL	2.4719 mL	12.3597 mL
50 mM	0.0989 mL	0.4944 mL	0.9888 mL	4.9439 mL
100 mM	0.0494 mL	0.2472 mL	0.4944 mL	2.4719 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 mother liquor preparation method and in vivo formula preparation method:

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DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

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Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O TargetMol | reagent

mix well and clarify

Dose Conversion

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Tech Support

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