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Purity: ≥98%
CCG 203769 is a novel, potent and selective G protein signaling (RGS4) inhibitor with an IC50 of 17 nM for blocking the RGS4-Gαo protein-protein interaction in vitro.
| 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].
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| 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].
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| References |
[1]. Blazer LL, et al. Selectivity and anti-Parkinson's potential of thiadiazolidinone RGS4 inhibitors. ACS Chem Neurosci. 2015 Jun 17;6(6):911-9
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| Molecular Formula |
C8H14N2O2S
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|---|---|
| Molecular Weight |
202.274
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| CAS # |
410074-60-1
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| SMILES |
O=C(N1CCCC)N(CC)SC1=O
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| Synonyms |
CCG-203769; CCG203769; CCG 203769
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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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