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J3770

Sigma-Aldrich

JNJ7777120

≥98% (HPLC)

Synonyma:

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

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About This Item

Empirický vzorec (Hillův zápis):
C14H16N3OCl
Číslo CAS:
459168-41-3
Molekulová hmotnost:
277.75
MDL number:
MFCD04343337
UNSPSC Code:
12352200
PubChem Substance ID:
329815408
NACRES:
NA.77

Quality Level

100

assay

≥98% (HPLC)

form

solid

color

white to off-white

solubility

DMSO: >20 mg/mL
H2O: insoluble

originator

Johnson & Johnson

storage temp.

room temp

SMILES string

CN1CCN(CC1)C(=O)c2cc3cc(Cl)ccc3[nH]2

InChI

1S/C14H16ClN3O/c1-17-4-6-18(7-5-17)14(19)13-9-10-8-11(15)2-3-12(10)16-13/h2-3,8-9,16H,4-7H2,1H3

InChI key

HUQJRYMLJBBEDO-UHFFFAOYSA-N

Application

JNJ7777120 has been used as a histamine-4 receptor antagonist:
  • to study its effects on the pro-inflammatory microglia in rats
  • to study its effects on the Parkinson′s-like pathology in rat brain
  • to study its effects on the histamine receptor interaction in periodontal ligament fibroblasts (PDLF)

Biochem/physiol Actions

JNJ7777120 may exhibit neuroprotective effects against ischemic brain damage. It acts as an anti-inflammatory agent to treat inflammatory diseases. JNJ7777120 is observed to reduce colonic injury, cytokine production, and neutrophil infiltration.
JNJ7777120 is a potent, selective non-imidazole H4 histamine receptor antagonist.

Features and Benefits

This compound is featured on the Histamine Receptors page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.
This compound was developed by Johnson & Johnson. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

pictograms

Exclamation mark
GHS07

signalword

Warning

Hazard Classifications

Eye Irrit. 2 - Skin Irrit. 2 - STOT SE 3

target_organs

Respiratory system

Storage Class

11 - Combustible Solids

wgk_germany

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

ppe

dust mask type N95 (US), Eyeshields, Gloves

Osvědčení o analýze (COA)

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Navštívit knihovnu dokumentů

Susanne Mommert et al.
International archives of allergy and immunology, 166(3), 225-230 (2015-05-01)
Natural killer (NK) cells have been detected in the lesional skin of patients with inflammatory skin diseases, where high levels of histamine are also present. Therefore, we investigated the effect of histamine, in particular via the histamine H4 receptor (H4R)
Qiuyuan Fang et al.
Brain, behavior, and immunity, 92, 127-138 (2020-11-30)
Growing evidence indicates that microglia activation and a neuroinflammatory trigger contribute to dopaminergic cell loss in Parkinson's disease (PD). Furthermore, increased density of histaminergic fibers and enhanced histamine levels have been observed in the substantia nigra of PD-postmortem brains. Histamine-induced
E Zampeli et al.
Inflammation research : official journal of the European Histamine Research Society ... [et al.], 58(6), 285-291 (2009-02-03)
Although the H(4) receptor localisation in the eye is unresolved, this study aimed to investigate the effects of the H(4) receptor antagonist JNJ7777120 in a model of experimental conjunctivitis. JNJ7777120, at 0.005-1 mmol/l, was instilled into the lower conjunctival fornix
C Hoffmann et al.
Molecular pharmacology, 88(3), 552-560 (2015-07-15)
Over the past decade the kinetics of ligand binding to a receptor have received increasing interest. The concept of drug-target residence time is becoming an invaluable parameter for drug optimization. It holds great promise for drug development, and its optimization
Ilaria Dettori et al.
Frontiers in pharmacology, 9, 1231-1231 (2018-11-14)
Cerebral ischemia is a multifactorial pathology characterized by different events evolving in time. The acute injury, characterized by excitoxicity, is followed by a secondary brain injury that develops from hours to days after ischemia. Extracellular levels of histamine increase in
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