CCG 203769 是一种选择性的 G 蛋白信号调节因子 (RGS4) 抑制剂，CCG 203769 阻断 RGS4-Gα_o 蛋白-蛋白相互作用，IC₅₀ 为 17 nM。

CCG 203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gα o protein-protein interaction in vitro with an IC 50 of 17 nM.

Liquid

RGS4 17 nM (IC50) RGS19 140 nM (IC50

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 Ca 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 Gα

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 lo

Room temperature in continental US; may vary elsewhere.

Pure form -20°C 3 years；4°C 2 years

[1]. Blazer LL, et al. Selectivity and anti-Parkinsons potential of thiadiazolidinone RGS4 inhibitors. ACS Chem Neurosci. 2015 Jun 17;6(6):911-9.

In Vitro: DMSO : 62.5 mg/mL (308.99 mM; Need ultrasonic)配制储备液