CAS 459168-41-3|JNJ-7777120

Introduction：Basic information about CAS 459168-41-3|JNJ-7777120, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. JNJ-7777120 BiologicalActivity
3. Chemical & Physical Properties
4. Safety Information
5. Articles8
6. Synonyms

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	/
MSDS	ChineseUSA	Flash Point	242.3±28.7 °C
Symbol	GHS07	Signal Word	Warning

Names

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

JNJ-7777120 BiologicalActivity

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 ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch 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.

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 ReceptorSignaling Pathways >>Immunology/Inflammation >>Histamine ReceptorResearch 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.

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
InChIKey	HUQJRYMLJBBEDO-UHFFFAOYSA-N
SMILES	CN1CCN(C(=O)c2cc3cc(Cl)ccc3[nH]2)CC1
Storage condition	Store at +4°C
Water Solubility	H2O: insoluble

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

Articles8

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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