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459168-41-3,MFCD04343337
Catalog No.:AA0037Q5

459168-41-3 | JNJ-7777120

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1mg
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$7.00   $5.00
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5mg
98%
in stock  
$11.00   $8.00
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10mg
98%
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$14.00   $10.00
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25mg
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  • Technical Information
  • Properties
  • Literature
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  • Technical Information
  • Properties
  • Literature
Technical Information
Catalog Number:
AA0037Q5
Chemical Name:
JNJ-7777120
CAS Number:
459168-41-3
Molecular Formula:
C14H16ClN3O
Molecular Weight:
277.7493
MDL Number:
MFCD04343337
SMILES:
CN1CCN(CC1)C(=O)c1cc2c([nH]1)ccc(c2)Cl
Properties
Computed Properties
 
Complexity:
344  
Covalently-Bonded Unit Count:
1  
Heavy Atom Count:
19  
Hydrogen Bond Acceptor Count:
2  
Hydrogen Bond Donor Count:
1  
Rotatable Bond Count:
1  
XLogP3:
2.3  

Literature

Title: Allergic inflammation is augmented via histamine H4 receptor activation: The role of natural killer cells in vitro and in vivo.

Journal: Journal of dermatological science 20160801

Title: Histamine H4 and H1 receptors contribute to postinflammatory visceral hypersensitivity.

Journal: Gut 20141201

Title: Discovery and SAR of 6-alkyl-2,4-diaminopyrimidines as histamine H₄ receptor antagonists.

Journal: Journal of medicinal chemistry 20140327

Title: Histamine H4 receptor antagonists as potent modulators of mammalian vestibular primary neuron excitability.

Journal: British journal of pharmacology 20121001

Title: Advantages of histamine H4 receptor antagonist usage with H1 receptor antagonist for the treatment of murine allergic contact dermatitis.

Journal: Experimental dermatology 20120901

Title: The antagonism of histamine H1 and H4 receptors ameliorates chronic allergic dermatitis via anti-pruritic and anti-inflammatory effects in NC/Nga mice.

Journal: Allergy 20120801

Title: Detailed structure-activity relationship of indolecarboxamides as H4 receptor ligands.

Journal: European journal of medicinal chemistry 20120801

Title: Incomplete activation of human eosinophils via the histamine H4-receptor: evidence for ligand-specific receptor conformations.

Journal: Biochemical pharmacology 20120715

Title: A bioinformatics search for selective histamine h4 receptor antagonists through structure-based virtual screening strategies.

Journal: Chemical biology & drug design 20120501

Title: Role of histamine and its receptor subtypes in stimulation of conjunctival goblet cell secretion.

Journal: Investigative ophthalmology & visual science 20120501

Title: Synthesis of novel histamine H4 receptor antagonists.

Journal: Bioorganic & medicinal chemistry letters 20120115

Title: Strain-dependent effects of the histamine H₄ receptor antagonist JNJ7777120 in a murine model of acute skin inflammation.

Journal: Experimental dermatology 20120101

Title: Ligand based design of novel histamine H₄ receptor antagonists; fragment optimization and analysis of binding kinetics.

Journal: Bioorganic & medicinal chemistry letters 20120101

Title: Opposite effects of mepyramine on JNJ 7777120-induced amelioration of experimentally induced asthma in mice in sensitization and provocation.

Journal: PloS one 20120101

Title: Deletion and down-regulation of HRH4 gene in gastric carcinomas: a potential correlation with tumor progression.

Journal: PloS one 20120101

Title: Effects of histamine H4 receptor ligands in a mouse model of gastric ulceration.

Journal: Pharmacology 20120101

Title: Molecular determinants of ligand binding modes in the histamine H(4) receptor: linking ligand-based three-dimensional quantitative structure-activity relationship (3D-QSAR) models to in silico guided receptor mutagenesis studies.

Journal: Journal of medicinal chemistry 20111208

Title: Challenges of drug discovery in novel target space. The discovery and evaluation of PF-3893787: a novel histamine H4 receptor antagonist.

Journal: Bioorganic & medicinal chemistry letters 20111101

Title: Mepyramine-JNJ7777120-hybrid compounds show high affinity to hH(1)R, but low affinity to hH(4)R.

Journal: Bioorganic & medicinal chemistry letters 20111101

Title: Discovery of a series of potent and selective human H4 antagonists using ligand efficiency and libraries to explore structure-activity relationship (SAR).

Journal: Bioorganic & medicinal chemistry letters 20111101

Title: Role of H4 receptor in histamine-mediated responses in human melanoma.

Journal: Melanoma research 20111001

Title: Histamine H(4) receptor antagonist reduces dermal inflammation and pruritus in a hapten-induced experimental model.

Journal: European journal of pharmacology 20110930

Title: Histamine H1, H3 and H4 receptors are involved in pruritus.

Journal: Neuroscience 20110908

Title: Role of the second and third extracellular loops of the histamine H(4) receptor in receptor activation.

Journal: Naunyn-Schmiedeberg's archives of pharmacology 20110901

Title: Lack of preventing effect of systemically and topically administered histamine H(1) or H(4) receptor antagonists in a dog model of acute atopic dermatitis.

Journal: Experimental dermatology 20110701

Title: Histamine H₄ receptor activation enhances LPS-induced IL-6 production in mast cells via ERK and PI3K activation.

Journal: European journal of immunology 20110601

Title: Triamino pyrimidines and pyridines as histamine H(4) receptor modulators.

Journal: Bioorganic & medicinal chemistry letters 20110515

Title: Expression and functional properties of canine, rat, and murine histamine H₄ receptors in Sf9 insect cells.

Journal: Naunyn-Schmiedeberg's archives of pharmacology 20110501

Title: Agonist-biased signaling at the histamine H4 receptor: JNJ7777120 recruits β-arrestin without activating G proteins.

Journal: Molecular pharmacology 20110401

Title: Paradoxical stimulatory effects of the 'standard' histamine H4-receptor antagonist JNJ7777120: the H4 receptor joins the club of 7 transmembrane domain receptors exhibiting functional selectivity.

Journal: Molecular pharmacology 20110401

Title: Histamine H(4) receptor antagonism inhibits allergen-specific T-cell responses mediated by human dendritic cells.

Journal: European journal of pharmacology 20110125

Title: Histamine H(4) receptor activation on human slan-dendritic cells down-regulates their pro-inflammatory capacity.

Journal: Immunology 20110101

Title: [Effect of histamine H4 receptor and its antagonist on allergic rhinitis in rats].

Journal: Zhonghua er bi yan hou tou jing wai ke za zhi = Chinese journal of otorhinolaryngology head and neck surgery 20100601

Title: Molecular determinants of ligand binding to H4R species variants.

Journal: Molecular pharmacology 20100501

Title: Histamine stimulates human lung fibroblast migration.

Journal: Molecular and cellular biochemistry 20100401

Title: The histamine H4 receptor mediates inflammation and pruritus in Th2-dependent dermal inflammation.

Journal: The Journal of investigative dermatology 20100401

Title: Does the histamine H4 receptor have a pro- or anti-inflammatory role in murine bronchial asthma?

Journal: Pharmacology 20100101

Title: Histamine H4 receptor antagonism diminishes existing airway inflammation and dysfunction via modulation of Th2 cytokines.

Journal: Respiratory research 20100101

Title: Interactions of histamine H1-receptor agonists and antagonists with the human histamine H4-receptor.

Journal: Molecular pharmacology 20091101

Title: Synthesis and structure-activity relationships of cyanoguanidine-type and structurally related histamine H4 receptor agonists.

Journal: Journal of medicinal chemistry 20091022

Title: 2,4-Diaminopyrimidines as histamine H4 receptor ligands--Scaffold optimization and pharmacological characterization.

Journal: Bioorganic & medicinal chemistry 20091015

Title: Expression of histamine H4 receptor in human epidermal tissues and attenuation of experimental pruritus using H4 receptor antagonist.

Journal: The Journal of toxicological sciences 20091001

Title: The histamine H receptor as a new target for treatment of canine inflammatory skin diseases.

Journal: Veterinary dermatology 20091001

Title: A new generation of anti-histamines: Histamine H4 receptor antagonists on their way to the clinic.

Journal: Current opinion in drug discovery & development 20090901

Title: The histamine H4 receptor antagonist JNJ7777120 induces increases in the histamine content of the rat conjunctiva.

Journal: Inflammation research : official journal of the European Histamine Research Society ... [et al.] 20090601

Title: Effect of histamine H4 receptor antagonist on allergic rhinitis in mice.

Journal: International immunopharmacology 20090601

Title: Histamine H4 receptor antagonism reduces hapten-induced scratching behaviour but not inflammation.

Journal: Experimental dermatology 20090101

Title: Discovery of quinazolines as histamine H4 receptor inverse agonists using a scaffold hopping approach.

Journal: Journal of medicinal chemistry 20081225

Title: cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), a new histamine H4R antagonist that blocks pain responses against carrageenan-induced hyperalgesia.

Journal: Journal of medicinal chemistry 20081127

Title: Structure-activity studies on a series of a 2-aminopyrimidine-containing histamine H4 receptor ligands.

Journal: Journal of medicinal chemistry 20081023

Title: Rotationally constrained 2,4-diamino-5,6-disubstituted pyrimidines: a new class of histamine H4 receptor antagonists with improved druglikeness and in vivo efficacy in pain and inflammation models.

Journal: Journal of medicinal chemistry 20081023

Title: Phenylalanine 169 in the second extracellular loop of the human histamine H4 receptor is responsible for the difference in agonist binding between human and mouse H4 receptors.

Journal: The Journal of pharmacology and experimental therapeutics 20081001

Title: Histamine H4 receptors modulate dendritic cell migration through skin--immunomodulatory role of histamine.

Journal: Allergy 20081001

Title: Cloning and pharmacological characterization of the dog histamine H4 receptor.

Journal: European journal of pharmacology 20080911

Title: Discovery of novel human histamine H4 receptor ligands by large-scale structure-based virtual screening.

Journal: Journal of medicinal chemistry 20080612

Title: Histamine H(4) receptors regulate ACTH release in AtT-20 cells.

Journal: European journal of pharmacology 20080610

Title: Activation mechanism of the human histamine H4 receptor--an explicit membrane molecular dynamics simulation study.

Journal: Journal of chemical information and modeling 20080601

Title: Binding mode analysis and enrichment studies on homology models of the human histamine H4 receptor.

Journal: European journal of medicinal chemistry 20080501

Title: Fragment based design of new H4 receptor-ligands with anti-inflammatory properties in vivo.

Journal: Journal of medicinal chemistry 20080424

Title: Histamine receptor H4R-selective ligands influence the STAT6 Transcription Activation Domain (TAD) and the DNA-binding.

Journal: Inflammation research : official journal of the European Histamine Research Society ... [et al.] 20080101

Title: Histamine downregulates monocyte CCL2 production through the histamine H4 receptor.

Journal: The Journal of allergy and clinical immunology 20070801

Title: Antiinflammatory and antinociceptive effects of the selective histamine H4-receptor antagonists JNJ7777120 and VUF6002 in a rat model of carrageenan-induced acute inflammation.

Journal: European journal of pharmacology 20070601

Title: The histamine H(4) receptor: a novel modulator of inflammatory and immune disorders.

Journal: Pharmacology & therapeutics 20070301

Title: Histamine H4 receptor antagonists are superior to traditional antihistamines in the attenuation of experimental pruritus.

Journal: The Journal of allergy and clinical immunology 20070101

Title: Role of histamine H3 and H4 receptors in mechanical hyperalgesia following peripheral nerve injury.

Journal: Neuroimmunomodulation 20070101

Title: Characterization of the histamine H4 receptor binding site. Part 1. Synthesis and pharmacological evaluation of dibenzodiazepine derivatives.

Journal: Journal of medicinal chemistry 20060727

Title: The histamine H4 receptor mediates allergic airway inflammation by regulating the activation of CD4+ T cells.

Journal: Journal of immunology (Baltimore, Md. : 1950) 20060601

Title: Preparation and biological evaluation of indole, benzimidazole, and thienopyrrole piperazine carboxamides: potent human histamine h(4) antagonists.

Journal: Journal of medicinal chemistry 20051229

Title: Inhibitory effects of histamine H4 receptor antagonists on experimental colitis in the rat.

Journal: European journal of pharmacology 20051017

Title: Evaluation of histamine H1-, H2-, and H3-receptor ligands at the human histamine H4 receptor: identification of 4-methylhistamine as the first potent and selective H4 receptor agonist.

Journal: The Journal of pharmacology and experimental therapeutics 20050901

Title: Synthesis and structure-activity relationships of indole and benzimidazole piperazines as histamine H(4) receptor antagonists.

Journal: Bioorganic & medicinal chemistry letters 20041101

Title: A potent and selective histamine H4 receptor antagonist with anti-inflammatory properties.

Journal: The Journal of pharmacology and experimental therapeutics 20040401

Title: The first potent and selective non-imidazole human histamine H4 receptor antagonists.

Journal: Journal of medicinal chemistry 20030911

Title: 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.

Title: 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.

Title: 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.

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Tags:459168-41-3 Molecular Formula|459168-41-3 MDL|459168-41-3 SMILES|459168-41-3 JNJ-7777120