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1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪

1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪用途

JNJ-7777120是一种选择性的组胺H4受体拮抗剂, Ki值为4 ±1 nM,比作用于其他组胺受体选择性高1000多倍。

1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪名称

[ CAS 号 ]:
459168-41-3

[ 中文名 ]:
1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪

[ 英文名 ]:
JNJ-7777120

[英文别名 ]:

JNJ-7777120

1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪生物活性

[ 描述 ]:

JNJ-7777120是一种选择性的组胺H4受体拮抗剂, Ki值为4 ±1 nM,比作用于其他组胺受体选择性高1000多倍。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 炎症/免疫

[参考文献]

[1]. Jablonowski JA, et al. The first potent and selective non-imidazole human histamine H4 receptor antagonists. J Med Chem. 2003 Sep 11;46(19):3957-3960.

[2]. Rosa AC, et al. Prevention of bleomycin-induced lung inflammation and fibrosis in mice by naproxen and JNJ-7777120 treatment. J Pharmacol Exp Ther. 2014 Nov;351(2):308-316.

[3]. Thurmond RL, et al. A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties. J Pharmacol Exp Ther. 2004 Apr;309(1):404-413.

[相关活性小分子]

1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
477.0±45.0 °C at 760 mmHg

[ 分子式 ]:
C₁₄H₁₆ClN₃O

[ 分子量 ]:
277.749

[ 闪点 ]:
242.3±28.7 °C

[ 精确质量 ]:
277.098175

[ PSA ]:
39.34000

[ LogP ]:
0.69

[ 外观性状 ]:
solid | white

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.656

[ 储存条件 ]:
Store at +4°C

[ 水溶解性 ]:
H2O: insoluble

1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪MSDS

1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

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

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38

[ 安全声明 (欧洲) ]:
26-36

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

[ WGK德国 ]:
3

1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪合成路线

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1-[(5-氯-1H-吲哚-2-基)羰基]-4-甲基哌嗪文献

Involvement of the H1 Histamine Receptor, p38 MAP Kinase, Myosin Light Chains Kinase, and Rho/ROCK in Histamine-Induced Endothelial Barrier Dysfunction.

Microcirculation 22 , 237-48, (2015)

The mechanisms by which histamine increases microvascular permeability remain poorly understood. We tested the hypothesis that H1 receptor activation disrupts the endothelial barrier and investigated ...

Histamine H4 receptor as a new therapeutic target for choroidal neovascularization in age-related macular degeneration.

Br. J. Pharmacol. 171(15) , 3754-63, (2014)

The present treatment for choroidal neovascularization (CNV) associated with age-related macular degeneration (AMD) is not sufficient. Hence, we examined the therapeutic efficacy of reducing histamine...

Analysis of the histamine H2-receptor in human monocytes.

Biochem. Pharmacol. 92(2) , 369-79, (2014)

Histamine receptors are G-protein-coupled receptors (GPCRs). Canonically, the histamine H2-receptor (H2R) couples to Gs-proteins and activates adenylyl cyclases (ACs) with subsequent adenosine-3',5'-c...

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