JNJ-7777120

Modify Date: 2024-01-02 18:39:20

JNJ-7777120 Structure
JNJ-7777120 structure
Common Name JNJ-7777120
CAS Number 459168-41-3 Molecular Weight 277.749
Density 1.3±0.1 g/cm3 Boiling Point 477.0±45.0 °C at 760 mmHg
Molecular Formula C14H16ClN3O Melting Point N/A
MSDS Chinese USA Flash Point 242.3±28.7 °C
Symbol GHS07
GHS07
Signal Word Warning

 Use of JNJ-7777120


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]

 Names

Name 1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methyl-piperazine
Synonym More Synonyms

 JNJ-7777120 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
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.

 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

 Safety Information

Symbol GHS07
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

~81%

JNJ-7777120 Structure

JNJ-7777120

CAS#:459168-41-3

Literature: Lazewska, Dorota; Karolak-Wojciechowska, Janina; Kolesinska, Beata; Kaminski, Zbigniew; Kiec-Kononowicz, Katarzyna Heterocyclic Communications, 2011 , vol. 17, # 5-6 p. 207 - 210

 Precursor & DownStream

Precursor  2

DownStream  0

 Articles8

More 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...

 Synonyms

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
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