CCG 203769|cas:410074-60-1|西域试剂

CCG 203769,99.62%

产品编号：Bellancom-U00431| CAS NO：410074-60-1| 分子式：C₈H₁₄N₂O₂S| 分子量：202.27

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货号	价格	库存与货期
Bellancom-U00431	￥3500.00	杭州北京（现货）
Bellancom-U00431	￥6000.00	杭州北京（现货）
Bellancom-U00431	￥12000.00	杭州北京（现货）

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CCG 203769

产品介绍

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。

生物活性

CCG 203769 is a selective G protein signaling (RGS4) inhibitor, which blocks the RGS4-Gα_o protein-protein interaction in vitro with an IC₅₀ of 17 nM.

体外研究

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/Gα_o binding in an RGS-selective manner. CCG 203769 enhances Gα_q-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 Gα_o and Gα_i1, the rate of GTP hydrolysis is strongly stimulated by RGS4, and this effect is inhibited by CCG 203769 with an IC₅₀<1 μM.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

性状

Liquid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (308.99 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (10.28 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (10.28 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (10.28 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (10.28 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (10.28 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (10.28 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。