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1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮用途

ODQ 是一种有效的选择性可溶性鸟苷酰环化酶 (sGC) 抑制剂。ODQ 增强顺铂促人间皮瘤细胞凋亡的作用。

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮名称

[ CAS 号 ]:
41443-28-1

[ 中文名 ]:
1H-[1,2,4]恶草灵并[4,3-a]喹喔啉-1-酮

[ 英文名 ]:
ODQ

[中文别名 ]:

[英文别名 ]:

[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one
Lopac-O-3636
T B566 BNVON HNJ
1H-[1,2,4]oxadiazolol[4,3,-a]quinoxalin-1-one
Tocris-0880
1H-(1,2,4)oxadiazolo(4,3-a)quinoxalin-1-one
MFCD00792620
1H-[1,2,4]-oxadiazolo[4,3-a]quinoxalin-1-one
ODQ
1H-[1,2,4]Oxadiazolo[4,3-a]quinoxalin-1-one

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮生物活性

[ 描述 ]:

ODQ 是一种有效的选择性可溶性鸟苷酰环化酶 (sGC) 抑制剂。ODQ 增强顺铂促人间皮瘤细胞凋亡的作用。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

研究领域 >> 癌症

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 鸟苷酸环化酶

[体外研究]

在30和50μM时,ODQ可显著诱导NCI-H2452细胞凋亡,使凋亡水平分别提高12倍和15倍。在10μM时,低于ODQ诱导凋亡阈值的浓度,ODQ与顺铂联合使用可增强(事实上,增加了一倍)1μM时顺铂的促凋亡作用[1]。

[体内研究]

ODQ(2mg/kg；i.p.)可减轻麻醉大鼠革兰氏阳性或革兰氏阴性菌壁碎片引起的多器官损伤和功能障碍[2]。动物模型：麻醉雄性Wistar大鼠[2]剂量：2mg/kg给药：静脉注射。结果：减轻脂磷壁酸/肽聚糖或脂多糖引起的肾功能不全、肺损伤和肝细胞损伤。

[参考文献]

[1]. Ronald Fiscus, et al. ODQ, an inhibitor of soluble guanylyl cyclase (nitric oxide-activated enzyme), enhances the pro-apoptotic effects of cisplatin in human mesothelioma cells. Cancer Res May 1 2007 (67) (9 Supplement) LB-43.

[2]. Zacharowski K, et al. The selective guanylate cyclase inhibitor ODQ reduces multiple organ injury in rodent models of Gram-positive and Gram-negative shock. Crit Care Med. 2001;29(8):1599-1608.

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮物理化学性质

[ 密度 ]:
1.6±0.1 g/cm3

[ 沸点 ]:
321.3±25.0 °C at 760 mmHg

[ 熔点 ]:
160-170 °C

[ 分子式 ]:
C₉H₅N₃O₂

[ 分子量 ]:
187.155

[ 闪点 ]:
148.1±23.2 °C

[ 精确质量 ]:
187.038177

[ PSA ]:
60.40000

[ LogP ]:
0.28

[ 外观性状 ]:
灰白色至淡黄色粉末

[ 蒸汽压 ]:
0.0±0.7 mmHg at 25°C

[ 折射率 ]:
1.781

[ 储存条件 ]:
2-8°C

[ 水溶解性 ]:
ethanol: 1.2 mg/mL

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮MSDS

详细MSDS(安全技术说明书)

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮安全信息

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xi: Irritant;

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ 海关编码 ]:
2934999090

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮上下游产品

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮上游产品

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮下游产品

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

1H-[1,2,4]恶二唑并[4,3-a]喹喔啉-1-酮文献

Nitric oxide donors increase PVR/CD155 DNAM-1 ligand expression in multiple myeloma cells: role of DNA damage response activation.

BMC Cancer 15 , 17, (2015)

DNAX accessory molecule-1 (DNAM-1) is an activating receptor constitutively expressed by macrophages/dendritic cells and by T lymphocytes and Natural Killer (NK) cells, having an important role in ant...

Role of Telokin in Regulating Murine Gastric Fundus Smooth Muscle Tension.

PLoS ONE 10 , e0134876, (2015)

Telokin phosphorylation by cyclic GMP-dependent protein kinase facilitates smooth muscle relaxation. In this study we examined the relaxation of gastric fundus smooth muscles from basal tone, or pre-c...

Isosorbide dinitrate inhibits mechanical stress-induced cardiac hypertrophy and autophagy through downregulation of angiotensin II type 1 receptor.

J. Cardiovasc. Pharmacol. 65(1) , 1-7, (2015)

Mechanical stress can induce cardiac hypertrophy and autophagy. Recently, it has been reported that nitric oxide donors inhibited autophagy in human chondrocytes. Therefore, the effect of isosorbide d...

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