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JNJ-7777120

Catalog No. T2232   CAS 459168-41-3
Synonyms: JNJ7777120

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

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JNJ-7777120 Chemical Structure
JNJ-7777120, CAS 459168-41-3
Pack Size Availability Price/USD Quantity
5 mg In stock $ 64.00
10 mg In stock $ 97.00
25 mg In stock $ 173.00
50 mg In stock $ 288.00
100 mg In stock $ 463.00
500 mg In stock $ 987.00
1 mL * 10 mM (in DMSO) In stock $ 67.00
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Purity: 99.93%
Purity: 99.71%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.
Targets&IC50 H4 receptor:4.5 nM(Ki)
In vitro JNJ 7777120 administration in mice inhibits the migration of tracheal mast cells from connective to epithelial tissues induced by histamine. Furthermore, JNJ 7777120 treatment in mice-derived bone marrow mast cells suppresses histamine-induced chemotaxis and calcium influx. In a peritonitis model induced by yeast polysaccharides in mice, JNJ 7777120 markedly inhibits neutrophil infiltration. The compound demonstrates oral bioavailability, with a 30% rate in rats and 100% in dogs, and a half-life of 3 hours for both species.
In vivo JNJ 7777120 is an effective, selective antagonist for the H4 receptor, with little to no affinity for over 50 other targets. It binds with high affinity to the H4 receptor, exhibiting over a thousand times greater selectivity compared to other histamine receptors.
Synonyms JNJ7777120
Molecular Weight 277.75
Formula C14H16ClN3O
CAS No. 459168-41-3

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

1eq. HCl: 27.8 mg/mL (100 mM)

DMSO: 13.9 mg/mL (50 mM)

TargetMolReferences and Literature

1. Jablonowski JA, et al. J Med Chem, 2003, 46(19), 3957-3960. 2. Thurmond RL, et al. J Pharmacol Exp Ther, 2004, 309(1), 404-413.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Highly Selective Inhibitor Library Membrane Protein-targeted Compound Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Preclinical Compound Library Neuronal Signaling Compound Library Target-Focused Phenotypic Screening Library Neurotransmitter Receptor Compound Library Histamine & Melatonin Receptor-Targeted Compound Library

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Keywords

JNJ-7777120 459168-41-3 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor JNJ 7777120 JNJ7777120 Inhibitor inhibit inhibitor

 

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