
CCG 203769
CAS No. 410074-60-1
CCG 203769( Thiadiazolidinone (TDZD) deriv. 6 | RGS4 inhibitor 11b | 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione )
Catalog No. M26093 CAS No. 410074-60-1
CCG 203769 is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.
Purity : >98% (HPLC)






Size | Price / USD | Stock | Quantity |
2MG | 152 | Get Quote |
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5MG | 260 | Get Quote |
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10MG | 447 | Get Quote |
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25MG | 714 | Get Quote |
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50MG | 1017 | Get Quote |
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100MG | 1368 | Get Quote |
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200MG | Get Quote | Get Quote |
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500MG | Get Quote | Get Quote |
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1G | Get Quote | Get Quote |
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Biological Information
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Product NameCCG 203769
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NoteResearch use only, not for human use.
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Brief DescriptionCCG 203769 is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.
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DescriptionCCG 203769 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.(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.
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In VitroCCG 203769 also displays dramatic selectivity (8- to >5000-fold) for RGS4 over other RGS proteins.CCG 203769 inhibits RGS19 with an IC50 of 140 nM (8-fold selective for RGS4) and 6 μM for RGS16 (350-fold selective for RGS4). The closely related RGS8 is very weakly inhibited (IC50>60 μM) providing >4500-fold selectivity for RGS4. CCG 203769 inhibits GSK-3β with an IC50 value of 5 μM. CCG 203769 does not inhibit the cysteine protease papain at 100 μM. CCG 203769 does not inhibit RGS7, which lacks cysteines in the RGS domain. CCG 203769 inhibits RGS/Gαo binding in an RGS-selective manner. CCG 203769 enhances Gαq-dependent cellular Ca2+ signaling in an RGS4-dependent manner. CCG 203769 also blocks the GTPase accelerating protein (GAP) activity of RGS4. In single-turnover and steady-state GTPase experiments with Gαo and Gαi1, the rate of GTP hydrolysis is strongly stimulated by RGS4, and this effect is inhibited by CCG 203769 with an IC50<1 μM.
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In VivoTo determine whether this genetic disruption of RGS4 function can be replicated pharmacologically, CCG 203769 is tested for effects on Carbamoylcholine chloride-mediated bradycardia in conscious, unrestrained rats. Carbamoylcholine chloride (0.1 mg/kg, IP) produces a modest decrease in heart rate compared to that of a saline vehicle control. CCG 203769 (10 mg/kg, IV) has no significant effect upon heart rate when given alone. However, CCG 203769, administered immediately prior to Carbamoylcholine chloride, significantly potentiates the bradycardic effect (p < 0.05). Given the functional role of RGS4 in Parkinson’s disease models, CCG 203769 is tested in a pharmacologic model of D2 antagonist-induced bradykinesia. Raclopride administration in rats causes increased hang time in the bar test, which is rapidly reversed by doses of CCG 203769 ranging from 0.1 to 10 mg/kg. The lowest dose, 0.01 mg/kg has no effect, while 0.1 mg/kg produces a submaximal effect. The higher doses, 1 and 10 mg/kg, produce equivalent effects. Similarly, the raclopride-induced paw drag in mice is reversed by 0.1-10 mg/kg CCG 203769.
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SynonymsThiadiazolidinone (TDZD) deriv. 6 | RGS4 inhibitor 11b | 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione
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PathwayPI3K/Akt/mTOR signaling
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TargetGSK-3
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Recptor5-HT1| 5-HT2A| 5-HT2C| D2| D4| α1 receptor
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Research Area——
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Indication——
Chemical Information
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CAS Number410074-60-1
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Formula Weight202.27
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Molecular FormulaC8H14N2O2S
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Purity>98% (HPLC)
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SolubilityIn Vitro:?DMSO : 62.5 mg/mL (308.99 mM)
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SMILESO=C1SN(C(=O)N1CCCC)CC
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Chemical Name——
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1.Erik Buntinx, MD, et al. Selective Serotonergic Properties of Low-Dose Pipamperone May Enhance Antidepressant Effect: Preclinical Evidence.
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