CCG-63802

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CCG-63802  纯度: 98.38%

CCG-63802 是一种选择性，可逆变构的 G 蛋白信号调节子 RGS4 抑制剂。CCG-63802 与 RGS4 特异性结合并阻断 RGS4-Gαo 相互作用，IC50 值为 1.9 μM。

CCG-63802

CCG-63802 Chemical Structure

CAS No. : 620112-78-9

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100 mg ￥7900 In-stock
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CCG-63802 相关产品

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生物活性

CCG-63802 is a selective, reversible and allosteric RGS4 inhibitor. CCG-63802 specifically binds to RGS4 and blocks the RGS4-Gαo interaction, with an IC50 value of 1.9 μM[1].

IC50 & Target[1]

RGS4

1.9 μM (IC50)

体外研究
(In Vitro)

CCG-63802 (5 μM) inhibits regulators of G-protein signaling (RGS) proteins in the presence of BK (bradykinin) and 8-Br-cGMP (membrane-permeable analogue of cGMP), HEK-293 cells start to depolarize again[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究
(In Vivo)

CCG-63802 (0.05 mg/kg; intratracheal administration; once per week; 90 days) reduces RGS4 protein expression, leading to partially abrogate the attenuating effect of PGZ on airway inflammation, hyperresponsiveness (AHR), and remodeling[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Forty female BALB/c mice aged 6-8 week old[3]
Dosage: 0.05 mg/kg
Administration: Intratracheal administration; once per week; 90 days
Result: CCG 63802 treatment in OVA +PGZ + CCG group significantly reduced RGS4 protein expression compared to OVA + PGZ group (P < 0.05)

分子量

450.51

Formula

C26H18N4O2S
CAS 号

620112-78-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 1.67 mg/mL (3.71 mM; Need ultrasonic and warming)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2197 mL 11.0985 mL 22.1971 mL
5 mM — — —
10 mM — — —

*

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:
  • 1.

    CCG-63802 is dissolved in DMSO and diluted with 0.9% NaCl[3].
参考文献

  • [1]. Levi L Blazer, et al. Reversible, allosteric small-molecule inhibitors of regulator of G protein signaling proteins. Mol Pharmacol. 2010 Sep;78(3):524-33.

    [2]. Marina Dobrivojević, et al. Interaction between bradykinin and natriuretic peptides via RGS protein activation in HEK-293 cells. Am J Physiol Cell Physiol. 2012 Dec 15;303(12):C1260-8.

    [3]. Xia Meng, et al. PPARγ Agonist PGZ Attenuates OVA-Induced Airway Inflammation and Airway Remodeling via RGS4 Signaling in Mouse Model. Inflammation. 2018 Dec;41(6):2079-2089.

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