1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. JNJ-7777120

JNJ-7777120 

Cat. No.: HY-13508 Purity: 99.97%
COA Handling Instructions

JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory.

For research use only. We do not sell to patients.

JNJ-7777120 Chemical Structure

JNJ-7777120 Chemical Structure

CAS No. : 459168-41-3

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Solution
10 mM * 1 mL in DMSO USD 95 In-stock
Estimated Time of Arrival: December 31
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10 mM * 1 mL
ready for reconstitution
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10 mg USD 145 In-stock
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50 mg USD 396 In-stock
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100 mg USD 660 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

JNJ-7777120 is a potent and selective histamine H4 receptor antagonist (Ki=4.5 nM). JNJ-7777120 effectively blocks histamine-induced migration of mouse tracheal mast cells from connective tissue to epithelial cells. JNJ-7777120 also significantly blocks neutrophil infiltration in a mouse Zymosan-induced peritonitis model. JNJ-7777120 has a good potential to study antipruritic and anti-inflammatory[1][2].

IC50 & Target

H4 receptor

 

In Vitro

JNJ-7777120 (0, 10, 100, 1000 nM; ~6 h) shows functional antagonism of the human and mouse histamine H4 receptors in SK-N-MC cells[1].
JNJ-7777120 (10 µM; 10 min) blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells[1].
JNJ7777120 (30-100 µM; 30 min) inhibits dose-dependently the production of thymus and activation-regulated chemokine/CCL17 and macrophage-derived chemokine/CCL22 from antigen-stimulated BMMC[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: SK-N-MC cells (expressing the human or mouse histamine H4 receptor)
Concentration: 0, 10, 100, 1000 nM
Incubation Time: ~6 h
Result: Exhibited antagonistic effect on human and mouse histamine H4 receptors.

Immunofluorescence[1]

Cell Line: Mouse mast cells
Concentration: 10 µM
Incubation Time: 10 min
Result: Exhibited a very potent antagonistic effect on the H4 receptor in primary cells.

Cell Viability Assay[1]

Cell Line: BMMC
Concentration: 30-100 µM
Incubation Time: 30 min
Result: Significantly inhibited the production of TARC (thymus and activation-regulated chemokine) and MDC (macrophage-derived chemokine).
In Vivo

JNJ-7777120 shows equipotent against the human, mouse, and rat receptors and exhibits at least 1000-fold selectivity over H1, H2, or H3 receptors[1].
JNJ-7777120 has an oral bioavailability of ~30% in rats and 100% in dogs, with a half-life of ~3 h in both species[1].
JNJ-7777120 (20 mg/kg; s.c.; single daily for 2 days) blocks the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice[1].
JNJ-7777120 (10 mg/kg; s.c.; single) significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c mice[1].
Dosage: 20 mg/kg
Administration: Subcutaneous injection; single daily for 2 days
Result: Blocked histamine induced an increase in the number of mast cells per tracheal section and a significant migration of mast cells towards the tracheal epithelium.
Animal Model: Male outbred Swiss albino mice (zymosan-induced peritonitis model)[1].
Dosage: 10 mg/kg
Administration: Subcutaneous injection; single
Result: Led to a statistically significant reduction of neutrophil infiltration.
Molecular Weight

277.75

Formula

C14H16ClN3O

CAS No.
SMILES

O=C(C(N1)=CC2=C1C=CC(Cl)=C2)N3CCN(C)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (180.02 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.6004 mL 18.0018 mL 36.0036 mL
5 mM 0.7201 mL 3.6004 mL 7.2007 mL
10 mM 0.3600 mL 1.8002 mL 3.6004 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (9.00 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (9.00 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (9.00 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.97%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
JNJ-7777120
Cat. No.:
HY-13508
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