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CCG-63802

RGS蛋白抑制剂,CCG-63802是可逆的G蛋白信号调节子（RGS）抑制剂，对RGS4抑制性尤其高。

目录号: PC10597 纯度: ≥98%

CAS No. :620112-78-9

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中文名称

CCG-63802

中文别名

alpha-[[9-甲基-2-(3-甲基苯氧基)-4-氧代-4H-吡啶并[1,2-a]嘧啶-3-基]亚甲基]-2-苯并噻唑乙腈

英文名称

CCG-63802

英文别名

(E)-2-(Benzo[d]thiazol-2-yl)-3-(9-methyl-4-oxo-2-(m-tolyloxy)-4H-pyrido[1,2-a]pyrimidin-3-yl)acrylonitrile;(2E)-2-(1,3-Benzothiazol-2-yl)-3-[9-methyl-2-(3-methylphenoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl]acrylonitrile;2-Benzothiazoleacetonitrile, α-[[9-methyl-2-(3-methylphenoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl]methylene]-, (alphaE)-;(2E)-2-Benzothiazol-2-yl-3-[9-methyl-2-(3-methylphenoxy)-4-oxo(5-hydropyridino[1,2-a]pyrimidin-3-yl)]prop-2-enenitrile;CCG-63802;(E)-2-(Benzo[d]thiazol-2-yl)-3-(9-methyl-4-oxo-2-(m-tolyloxy)-4H-pyrido[1,2-a]pyrimidin-3-yl)a...;CCG 63802;AC1O107Z;CHEMBL1476646;HMS1804I11;MolPort-000-250-364;STK705022;STOCK4S-75157;alpha-[[9-Methyl-2-(3-methylphenoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl]methylene]-2-benzothiazoleacetonitrile

Cas No.

620112-78-9

分子式

C₂₆H₁₈N₄O₂S

分子量

450.51

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

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

性状

Solid

IC50 & Target[1][2]

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.

Medlife 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.

Medlife 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
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)

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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. [Information]

[2]. Marina Dobrivojevi?, 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. [Information]

[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. [Information]

溶解度数据

体外研究:

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

配制储备溶液

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	---	---	---

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

1.

CCG-63802 is dissolved in DMSO and diluted with 0.9% NaCl.

搜索质检报告(COA)

产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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