CCG 203769
- CAS No.
- 410074-60-1
- Chemical Name:
- CCG 203769
- Synonyms
- CCG 203769;1,2,4-Thiadiazolidine-3,5-dione, 4-butyl-2-ethyl-
- CBNumber:
- CB04797029
- Molecular Formula:
- C8H14N2O2S
- Molecular Weight:
- 202.27
- MDL Number:
- MOL File:
- 410074-60-1.mol
CCG 203769 price
Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
---|---|---|---|---|---|---|---|
ChemScene | CS-0035365 | CCG203769 99.93% | 410074-60-1 | 5mg | $350 | 2021-12-16 | Buy |
ChemScene | CS-0035365 | CCG203769 99.93% | 410074-60-1 | 10mg | $600 | 2021-12-16 | Buy |
ChemScene | CS-0035365 | CCG203769 99.93% | 410074-60-1 | 25mg | $1200 | 2021-12-16 | Buy |
CCG 203769 Chemical Properties,Uses,Production
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.
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[1].
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[1].
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.
CCG 203769 Preparation Products And Raw materials
Raw materials
Preparation Products
CCG 203769 Suppliers
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 19892 | 58 |
ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 | sales-cpd@caerulumpharma.com | China | 3465 | 58 |
Fan De(Beijing) Biotechnology Co., Ltd. | 15911056312 | liming@bio-fount.com | China | 9730 | 58 |
DC Chemicals | 021-58447131 13564518121 | sales@dcchemicals.com | China | 9412 | 58 |
ChemeGen(Shanghai) Biotechnology Co.,Ltd. | 18818260767 | sales@chemegen.com | China | 11289 | 58 |
Shanghai hongqu biomedical technology co. LTD | 88888888888 | hongquchem@qq.com | China | 5132 | 58 |
Chunchuang (Wuhan) Technology Co., Ltd | 15342225168 | yutianchun2007@126.com | China | 10001 | 58 |
cjbscvictory | 13348960310 13348960310 | 3003867561@qq.com | China | 10000 | 58 |
Beijing Stronger Science Co., Ltd. | 0531-88924771 15614660963 | elsa.hang@strongerscience.com | China | 10624 | 58 |
TargetMol Chemicals Inc. | 4008200310 | marketing@tsbiochem.com | China | 24016 | 58 |