CCG 203769 free base · Synonyms: CCG-203769 · CCG203769
CCG 203769 is a selective G protein signaling inhibitor.
For research use only. Not for human or veterinary use.
CCG 203769 structure
CAS No.: 410074-60-1
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 50 mg | USD 450.00 | BP-02070-50mg | In stock | Get quote |
| 100 mg | USD 650.00 | BP-02070-100mg | In stock | Get quote |
| 250 mg | USD 950.00 | BP-02070-250mg | In stock | Get quote |
| 500 mg | USD 1,350.00 | BP-02070-500mg | In stock | Get quote |
| 1 g | USD 1,850.00 | BP-02070-1g | In stock | Get quote |
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Description
CCG 203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gαo protein-protein interaction in vitro with an IC50 of 17 nM.
Biological activity
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.
Identifiers
- SMILES
-
O=C1SN(CC)C(N1CCCC)=O - InChIKey
-
WTFFYZGCISALRI-UHFFFAOYSA-N
Specifications
- MW (average)
- 202.2740
- Formula
- C8H14N2O2S
- CAS No.
- 410074-60-1
- Physical state
- Liquid
- Color
- colorless to light yellow
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20°C, 3 years , 4°C, 2 years ; In solvent -20°C, 1 month
Solubility
Soluble in DMSO : 62.5 mg/mL