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

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.

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JNJ-7777120 Chemical Structure

JNJ-7777120 Chemical Structure

CAS No. : 459168-41-3

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Solid + Solvent
10 mM * 1 mL in DMSO
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10 mg USD 120 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].

MedChemExpress (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].

MedChemExpress (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.
Appearance

Solid

Color

White to off-white

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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (180.02 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 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

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.85%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6004 mL 18.0018 mL 36.0036 mL 90.0090 mL
5 mM 0.7201 mL 3.6004 mL 7.2007 mL 18.0018 mL
10 mM 0.3600 mL 1.8002 mL 3.6004 mL 9.0009 mL
15 mM 0.2400 mL 1.2001 mL 2.4002 mL 6.0006 mL
20 mM 0.1800 mL 0.9001 mL 1.8002 mL 4.5005 mL
25 mM 0.1440 mL 0.7201 mL 1.4401 mL 3.6004 mL
30 mM 0.1200 mL 0.6001 mL 1.2001 mL 3.0003 mL
40 mM 0.0900 mL 0.4500 mL 0.9001 mL 2.2502 mL
50 mM 0.0720 mL 0.3600 mL 0.7201 mL 1.8002 mL
60 mM 0.0600 mL 0.3000 mL 0.6001 mL 1.5002 mL
80 mM 0.0450 mL 0.2250 mL 0.4500 mL 1.1251 mL
100 mM 0.0360 mL 0.1800 mL 0.3600 mL 0.9001 mL
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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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