459168-41-3 | JNJ-7777120

Packsize	Purity	Availability	Price	Discounted Price
1mg	98%	in stock	$10.00	$7.00
5mg	98%	in stock	$15.00	$10.00
10mg	98%	in stock	$19.00	$13.00
25mg	98%	in stock	$32.00	$22.00
50mg	98%	in stock	$50.00	$35.00
100mg	98%	in stock	$85.00	$59.00
250mg	98%	in stock	$106.00	$75.00
1g	98%	in stock	$267.00	$187.00
5g	98%	in stock	$760.00	$532.00
10g	98%	in stock	$1,319.00	$923.00

Description

• Catalog Number: AB49881
• 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

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

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  Journal of dermatological science 20160801

• Histamine H4 and H1 receptors contribute to postinflammatory visceral hypersensitivity.

  Gut 20141201

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

  Journal of medicinal chemistry 20140327

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

  British journal of pharmacology 20121001

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

  Experimental dermatology 20120901

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

  Allergy 20120801

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

  European journal of medicinal chemistry 20120801

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

  Biochemical pharmacology 20120715

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

  Chemical biology & drug design 20120501

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

  Investigative ophthalmology & visual science 20120501

• Synthesis of novel histamine H4 receptor antagonists.

  Bioorganic & medicinal chemistry letters 20120115

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

  Experimental dermatology 20120101

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

  Bioorganic & medicinal chemistry letters 20120101

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

  PloS one 20120101

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

  PloS one 20120101

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

  Pharmacology 20120101

• 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 of medicinal chemistry 20111208

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

  Bioorganic & medicinal chemistry letters 20111101

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

  Bioorganic & medicinal chemistry letters 20111101

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

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

  Melanoma research 20111001

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

  European journal of pharmacology 20110930

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

  Neuroscience 20110908

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

  Naunyn-Schmiedeberg's archives of pharmacology 20110901

• 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.

  Experimental dermatology 20110701

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

  European journal of immunology 20110601

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

  Bioorganic & medicinal chemistry letters 20110515

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

  Naunyn-Schmiedeberg's archives of pharmacology 20110501

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

  Molecular pharmacology 20110401

• 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.

  Molecular pharmacology 20110401

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

  European journal of pharmacology 20110125

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

  Immunology 20110101

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

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

• Molecular determinants of ligand binding to H4R species variants.

  Molecular pharmacology 20100501

• Histamine stimulates human lung fibroblast migration.

  Molecular and cellular biochemistry 20100401

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

  The Journal of investigative dermatology 20100401

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

  Pharmacology 20100101

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

  Respiratory research 20100101

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

  Molecular pharmacology 20091101

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

  Journal of medicinal chemistry 20091022

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

  Bioorganic & medicinal chemistry 20091015

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

  The Journal of toxicological sciences 20091001

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

  Veterinary dermatology 20091001

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

  Current opinion in drug discovery & development 20090901

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

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

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

  International immunopharmacology 20090601

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

  Experimental dermatology 20090101

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

  Journal of medicinal chemistry 20081225

• 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 of medicinal chemistry 20081127

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

  Journal of medicinal chemistry 20081023

• 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 of medicinal chemistry 20081023

• 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.

  The Journal of pharmacology and experimental therapeutics 20081001

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

  Allergy 20081001

• Cloning and pharmacological characterization of the dog histamine H4 receptor.

  European journal of pharmacology 20080911

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

  Journal of medicinal chemistry 20080612

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

  European journal of pharmacology 20080610

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

  Journal of chemical information and modeling 20080601

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

  European journal of medicinal chemistry 20080501

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

  Journal of medicinal chemistry 20080424

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

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

• Histamine downregulates monocyte CCL2 production through the histamine H4 receptor.

  The Journal of allergy and clinical immunology 20070801

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

  European journal of pharmacology 20070601

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

  Pharmacology & therapeutics 20070301

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

  The Journal of allergy and clinical immunology 20070101

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

  Neuroimmunomodulation 20070101

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

  Journal of medicinal chemistry 20060727

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

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

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

  Journal of medicinal chemistry 20051229

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

  European journal of pharmacology 20051017

• 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.

  The Journal of pharmacology and experimental therapeutics 20050901

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

  Bioorganic & medicinal chemistry letters 20041101

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

  The Journal of pharmacology and experimental therapeutics 20040401

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

  Journal of medicinal chemistry 20030911