JNJ-7777120

Names

[ Name ]:
JNJ-7777120

[Synonym ]:
Methanone, (5-chloro-1H-indol-2-yl)(4-methyl-1-piperazinyl)-
(5-Chloro-1H-indol-2-yl)(4-methyl-1-piperazinyl)methanone
JNJ-7777120
(5-chloro-1H-indol-2-yl)(4-methylpiperazin-1-yl)methanone
(5-chloro-1H-indol-2-yl)-(4-methylpiperazin-1-yl)methanone
1-((5-chloro-1H-indol-2-yl)carbonyl)-4-methylpiperazine

Biological Activity

[Description]:

JNJ-7777120 is a selective H4R antagonist with Ki of 4 ±1 nM, exhibits >1000-fold selectivity over the other histamin receptors.IC50 value: 4 ±1 nM (Ki) [1] Target: histamine H4 receptorin vitro: JNJ-7777120 prevents fibronectin-induced lung fibroblast migration, thus suggesting that H4R could represent an attractive target for the development of new drugs for lung fibrosis treatment .[2]in vivo: JNJ 7777120 blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells. In addition, it can block the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice. JNJ 7777120 significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model. [3]

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Inflammation/Immunology

[References]

[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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
477.0±45.0 °C at 760 mmHg

[ Molecular Formula ]:
C₁₄H₁₆ClN₃O

[ Molecular Weight ]:
277.749

[ Flash Point ]:
242.3±28.7 °C

[ Exact Mass ]:
277.098175

[ PSA ]:
39.34000

[ LogP ]:
0.69

[ Appearance of Characters ]:
solid | white

[ Vapour Pressure ]:
0.0±1.2 mmHg at 25°C

[ Index of Refraction ]:
1.656

[ Storage condition ]:
Store at +4°C

[ Water Solubility ]:
H2O: insoluble

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H315-H319-H335

[ Precautionary Statements ]:
P261-P305 + P351 + P338

[ Personal Protective Equipment ]:
dust mask type N95 (US);Eyeshields;Gloves

[ Hazard Codes ]:
Xi

[ Risk Phrases ]:
R36/37/38

[ Safety Phrases ]:
26-36

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

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...

Related Compounds

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