| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
Purity: ≥98%
| Targets |
CCG 203769 targets RGS4, a regulator of G-protein signaling protein. It inhibits the RGS4-Gαo protein-protein interaction with an IC50 of 17 nM. Additionally, the compound targets RhoA-mediated signaling pathways, disrupting Rho/MRTF/SRF-dependent gene transcription. This dual mechanism may contribute to its biological effects.
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| ln Vitro |
Moreover, CCG 203769 shows notable selectivity for RGS4 relative to other RGS proteins (8 to >5000-fold). With an IC50 of 140 nM (eight times more selective for RGS4), CCG 203769 inhibits RGS19, and at 6 μM (three hundred fifty times more selective for RGS4), it inhibits RGS16. There was very little inhibition of the similarly related RGS8 (IC50>60 μM), giving RGS4 a selectivity >4500-fold. GSK-3β is inhibited by CCG 203769, with an IC50 value of 5 μM. At 100 μM, CCG 203769 does not inhibit papain, a cysteine protease. Since cysteine is absent from the RGS domain of RGS7, CCG 203769 does not inhibit RGS7. RGS-selective inhibition of RGS/Gαo binding is achieved by CCG 203769. In an RGS4-dependent manner, CCG 203769 improves cellular Ca2+ signaling that is dependent on Gαq. Additionally, CCG 203769 inhibits RGS4's GTPase Accelerating Protein (GAP) function. RGS4 significantly increased the rate of GTP hydrolysis in single-turnover and steady-state GTPase tests utilizing Gαo and Gαi1, and this effect was blocked by CCG 203769 with IC50<1 μM [1].
In vitro, CCG 203769 potently inhibits the RGS4-Gαo protein-protein interaction with an IC50 of 17 nM. The compound's high potency for RGS4 inhibition makes it a valuable tool for studying RGS4 function in GPCR signaling. |
| ln Vivo |
In order to ascertain whether the pharmacological replication of this genetic disruption of RGS4 function was possible, we examined the impact of CCG 203769 on bradycardia mediated by carbamylcholine chloride in rats that were awake and unrestrained. In contrast to saline vehicle controls, carbamylcholine chloride (0.1 mg/kg, IP) moderately lowered heart rate. When given alone, CCG 203769 (10 mg/kg IV) had no discernible effect on heart rate. CCG 203769, on the other hand, greatly increased the bradycardia effect when it was given right before carbamylcholine chloride (p < 0.05). In a pharmacological model of D2 antagonist-induced bradykinesia, CCG 203769 was tested in light of RGS4's functional role in Parkinson's disease models. In the rod test, rats given raclopride had longer suspension times; however, CCG 203769, administered at doses ranging from 0.1 to 10 mg/kg, quickly corrected this effect. A submaximal effect was produced by 0.1 mg/kg, while the lowest dose of 0.01 mg/kg had no effect at all. Increased dosages of 1 mg/kg and 10 mg/kg have the same result. Similarly, mice's paw drag caused by raclopride is reversed by 0.1–10 mg/kg CCG 203769 [1].
In vivo, CCG 203769 has been studied for its effects on RGS4-mediated signaling pathways. As a potent RGS4 inhibitor, it enhances GPCR signaling by blocking RGS4-mediated desensitization. |
| Enzyme Assay |
For protein-protein interaction assays, recombinant RGS4 and Gαo proteins are incubated with varying concentrations of CCG 203769. The interaction between RGS4 and Gαo is measured using fluorescence polarization, surface plasmon resonance, or ELISA-based assays. IC50 values are calculated from dose-response curves.
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| Cell Assay |
Cellular assays utilize cell lines expressing GPCRs and RGS4. Cells are treated with CCG 203769 at various concentrations, and GPCR-mediated signaling is assessed by measuring downstream effectors such as calcium mobilization, cAMP accumulation, or MAPK activation. Enhanced signaling in the presence of the inhibitor confirms RGS4 inhibition.
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| Animal Protocol |
In vivo studies are conducted in animal models to evaluate the effects of RGS4 inhibition on GPCR-mediated physiological responses. CCG 203769 is administered via appropriate routes, and endpoints are selected based on the specific signaling pathways being investigated.
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| ADME/Pharmacokinetics |
CCG 203769 (molecular weight 202.27) is a small-molecule RGS4 inhibitor. The compound's physicochemical properties support its use in in vitro and in vivo studies. It is typically formulated in DMSO for in vitro assays and in appropriate vehicles for in vivo administration.
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| Toxicity/Toxicokinetics |
Preclinical toxicity studies of CCG 203769 have been limited as the compound is primarily used as a research tool. No significant toxicity has been reported in the available literature. The compound's safety profile supports its use for studying RGS4 function and GPCR signaling.
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| References | |
| Additional Infomation |
CCG 203769 is a potent and selective inhibitor of RGS4 with an IC50 of 17 nM for the RGS4-Gαo protein-protein interaction. It also targets RhoA-mediated signaling pathways. The compound is used as a research tool to study the role of RGS4 in GPCR signaling and to explore the therapeutic potential of RGS4 inhibitors.
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| Molecular Formula |
C8H14N2O2S
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|---|---|
| Molecular Weight |
202.274
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| Exact Mass |
202.077
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| CAS # |
410074-60-1
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| PubChem CID |
6539137
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| Appearance |
Colorless to light yellow liquid
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
264.3±23.0 °C at 760 mmHg
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| Flash Point |
113.6±22.6 °C
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| Vapour Pressure |
0.0±0.5 mmHg at 25°C
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| Index of Refraction |
1.527
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| LogP |
0.65
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
13
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| Complexity |
220
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(N1CCCC)N(CC)SC1=O
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| InChi Key |
WTFFYZGCISALRI-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C8H14N2O2S/c1-3-5-6-9-7(11)10(4-2)13-8(9)12/h3-6H2,1-2H3
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| Chemical Name |
4-butyl-2-ethyl-1,2,4-thiadiazolidine-3,5-dione
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| Synonyms |
CCG-203769; CCG203769; CCG 203769
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~62.5 mg/mL (~308.99 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (10.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (10.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (10.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.9439 mL | 24.7194 mL | 49.4389 mL | |
| 5 mM | 0.9888 mL | 4.9439 mL | 9.8878 mL | |
| 10 mM | 0.4944 mL | 2.4719 mL | 4.9439 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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