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)

COA Datasheet HNMR HPLC MSDS Handing Instructions
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Biological Information

  • Product Name
    CCG 203769
  • Note
    Research use only, not for human use.
  • Brief Description
    CCG 203769 is a selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction.
  • Description
    CCG 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.
  • In Vitro
    CCG 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.
  • In Vivo
    To 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.
  • Synonyms
    Thiadiazolidinone (TDZD) deriv. 6 | RGS4 inhibitor 11b | 4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione
  • Pathway
    PI3K/Akt/mTOR signaling
  • Target
    GSK-3
  • Recptor
    5-HT1| 5-HT2A| 5-HT2C| D2| D4| α1 receptor
  • Research Area
    ——
  • Indication
    ——

Chemical Information

  • CAS Number
    410074-60-1
  • Formula Weight
    202.27
  • Molecular Formula
    C8H14N2O2S
  • Purity
    >98% (HPLC)
  • Solubility
    In Vitro:?DMSO : 62.5 mg/mL (308.99 mM)
  • SMILES
    O=C1SN(C(=O)N1CCCC)CC
  • Chemical Name
    ——

Shipping & Storage Information

  • Storage
    (-20℃)
  • Shipping
    With Ice Pack
  • 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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