459168-41-3

459168-41-3 structure

Name: JNJ-7777120
Chemical Name: 1-[(5-Chloro-1H-indol-2-yl)carbonyl]-4-methyl-piperazine
CAS Number: 459168-41-3
Molecular Formula: C₁₄H₁₆ClN₃O
Molecular Weight: 277.749
Catalog: Biochemical Inhibitor Neuronal Signaling Histamine Receptor Antagonist
Create Date: 2018-12-22 16:05:52
Modify Date: 2024-01-02 18:39:20
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]

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

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.

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	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

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

109-01-3

10517-21-2

~81%

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 2
109-01-3 10517-21-2
DownStream 0

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