标签归档：rgs

CCG-63802

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

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

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
5 mg ￥660 In-stock
10 mg ￥1100 In-stock
50 mg ￥4400 In-stock
100 mg ￥7900 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

CCG-63802 相关产品

•相关化合物库:

  • Covalent Screening Library Plus
  • Bioactive Compound Library Plus
  • GPCR/G Protein Compound Library
  • Immunology/Inflammation Compound Library
  • Anti-Cancer Compound Library
  • Covalent Screening Library
  • Targeted Diversity Library

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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务