JNJ-7777120 - Moligand™, 10mM in DMSO , Antagonist of H 4 receptor, CAS No.459168-41-3, Antagonist of H 4 receptor

CAS: 459168-41-3 Cat. No.: J408337 Molecular Weight: 277.75 EC Number: 636-930-4

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

Methanone, (5-chloro-1H-indol-2-yl)(4-methyl-1-piperazinyl)-

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

JNJ-7777120 is the first potent and selective non-imidazolehistamine H4 receptorantagonist withKiof 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.
In vitro

JNJ 7777120 binds with high affinity to the H4 receptor and has a greater than 1000-fold selectivity over the other histamine receptors. JNJ 7777120 is a selective and potent H4 receptor antagonist with little or no affinity for over 50 other targets.

In vivo

JNJ 7777120 has an oral bioavailability of ~30% in rats and 100% in dogs, with a half-life of ∼3 h in both species. JNJ 7777120 blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells. JNJ 7777120 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.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

Methanone, (5-chloro-1H-indol-2-yl)(4-methyl-1-piperazinyl)-

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with K_i of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Antagonist of H 4 receptor

Names and Identifiers

• Isomeric SMILES: CN1CCN(CC1)C(=O)C2=CC3=C(N2)C=CC(=C3)Cl
• WGK Germany: 3
• Alternate CAS: 459168-41-3
• MeSH Entry Terms: 1-((5-chloro-1H-indol-2-yl)carbonyl)-4-methylpiperazine;JNJ 7777120;JNJ7777120
• Molecular Weight: 277.75
• Reaxy-Rn: 9495563
• Reaxys-RN_link_address: https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=9495563&ln=

Associated Targets(Human)

HRH4 Tchem Histamine H4 receptor (64 Activities)

Discover Target: HRH4

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro Water: 9 mg/mL (49.95 mM); DMSO: Insoluble

References

1. Xu Rui-Qi, Ma Ling, Chen Timson, Zhang Wei-Xiong, Chang Kuan, Wang Jing.  (2023)  Sophorolipid inhibits histamine-induced itch by decreasing PLC/IP3R signaling pathway activation and modulating TRPV1 activity.  Scientific Reports,  13  (1): (1-13).  [PMID:37198299] [10.1038/s41598-023-35158-9]

2. Hongming Tang, Tao Hou, Han Zhou, Han Liao, Fangfang Xu, Xiaomin Xie, Wenjie Yuan, Zhixin Guo, Yanfang Liu, Jixia Wang, Weijia Zhou, Xinmiao Liang.  (2024)  Label-free cell phenotypic profiling of histamine H4R receptor and discovery of non-competitive H4R antagonist from natural products.  BIOORGANIC CHEMISTRY,      [PMID:38643561] [10.1016/j.bioorg.2024.107387]