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

中文名称:

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

中文同义词:

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;RGS抑制剂(CCG-63802)

英文名称:

alpha-[[9-Methyl-2-(3-methylphenoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl]methylene]-2-benzothiazoleacetonitrile

英文同义词:

α-[[9-Methyl-2-(3-methylphenoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl]methylene]-2-benzothiazoleacetonitrile;(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;(E)-2-(Benzo[d]thiazol-2-yl)-3-(9-methyl-4-oxo-2-(m-tolyloxy)-4H-pyrido[1,2-a]pyrimidin-3-yl)acry;alpha-[[9-Methyl-2-(3-methylphenoxy)-4-oxo-4H-pyrido[1,2-a]pyrimidin-3-yl]methylene]-2-benzothiazoleacetonitrile;CCG 63802; CCG63802;(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]-

CAS号:

620112-78-9

分子式:

C26H18N4O2S

分子量:

450.51

EINECS号:

相关类别:

细胞生物学试剂;G蛋白偶联受体G蛋白

Mol文件:

620112-78-9.mol

沸点 

547.9±60.0 °C(Predicted)

密度 

1.31

储存条件 

Sealed in dry,Store in freezer, under -20°C

酸度系数(pKa)

-0.42±0.70(Predicted)

生物活性

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。

靶点

RGS4 1.9 μM (IC 50 )

RGS4 1.9 μM (IC 50 )

体外研究

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.

体内研究

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. 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)

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)

危险品标志 

T

危险类别码 

25

安全说明 

45