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Chemical Structure| 459168-41-3 Chemical Structure| 459168-41-3

Structure of JNJ-7777120
CAS No.: 459168-41-3

Chemical Structure| 459168-41-3

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JNJ-7777120 is a selective antagonist of histamine-4 receptor (H4R) with Ki of 4 ± 1 nM.

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Product Details of JNJ-7777120

CAS No. :459168-41-3
Formula : C14H16ClN3O
M.W : 277.75
SMILES Code : O=C(C(N1)=CC2=C1C=CC(Cl)=C2)N3CCN(C)CC3
MDL No. :MFCD04343337
InChI Key :HUQJRYMLJBBEDO-UHFFFAOYSA-N
Pubchem ID :4908365

Safety of JNJ-7777120

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of JNJ-7777120

GPCR

Isoform Comparison

Biological Activity

Target
  • H4 receptor

    Histamine H4 receptor, Ki:4.5 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
Atopic dermatitis outer root sheath keratinocytes 10μM 48 hours Stimulation with histamine or H4R agonist induced proliferation in atopic dermatitis keratinocytes, which was blocked by H4R antagonist JNJ7777120 PMC4447893
H4R-transfected HaCaT keratinocytes 10μM 48 hours Histamine stimulation induced proliferation in H4R-transfected HaCaT cells, which was blocked by H4R antagonist JNJ7777120 PMC4447893
Human primary neonatal keratinocytes 10μM 48 hours Stimulation with histamine or H4R agonist 4-MH induced keratinocyte proliferation, which was blocked by H4R-specific antagonist JNJ7777120 PMC4447893
4T1 cells 10 μmol/L 48 hours To evaluate the cellular uptake and antitumor effect of PP@T, results showed that PP@T significantly enhanced oxidative stress and apoptosis under ultrasound irradiation. PMC7000401
Human retinal endothelial cells (HRECs) 0.1–10 μM 4 hours To evaluate the effect of R-2-HG on endothelial cell migration, results showed that R-2-HG significantly enhanced the migration ability of HRECs. PMC4128071
Mouse whole blood 50 μM 4 hours To evaluate the effect of JNJ-7777120 on LPS-induced TNF production, results showed no inhibition of TNF production by JNJ-7777120 in vitro. PMC3654183

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
C57BL/6 female mice Experimental autoimmune encephalomyelitis (EAE) model Intraperitoneal injection 10 mg/kg Once daily, starting from day 10 post-immunization until the end of the experiment (up to 28 days) Evaluate the effect of JNJ7777120 on the clinical course of EAE, showing that JNJ7777120 treatment exacerbated EAE symptoms, increased spinal cord inflammation and demyelination, increased IFN-γ expression, and decreased IL-4 and IL-10 expression PMC3764850
BALB/c mice 4T1 TNBC model Subcutaneous injection 10 mg/kg Once daily for 15 days Evaluate the effect of JNJ-7777120 on tumor growth and immune modulation in the 4T1 TNBC model, results showed JNJ-7777120 non-significantly reduced tumor weight and spleen weight, while significantly decreasing the percentage of tumor-infiltrating CD4+ T lymphocytes and Tregs in TDLN PMC7000401
Mice Laser-induced choroidal neovascularization (CNV) model Intravitreous injection 1 μg Injected immediately after laser injury and again on day 3 To evaluate the effect of JNJ7777120 on CNV volume and pathological vessel leakage, results showed JNJ7777120 significantly reduced laser-induced CNV volume and pathological leakage without causing retinal toxicity. PMC4128071
BALB/c mice Carrageenan-induced pleurisy model Intraperitoneal injection 30 mg/kg Single dose, lasting 4 hours To evaluate the anti-inflammatory effects of JNJ-7777120 on carrageenan-induced pleurisy. Results showed that JNJ significantly reduced the number of T-cell subsets, GITR+ and GITR+IL-17A+ cells, and decreased the levels of Th1/Th17 cytokines, while up-regulating the expression of Th2 cytokines. PMC4080953
BALB/c mice LPS-induced inflammation model Oral 20 mg/kg Single dose, LPS administered 30 minutes later To evaluate the effect of JNJ-7777120 on LPS-induced TNF production, results showed significant inhibition of TNF production by JNJ-7777120. PMC3654183
BALB/c female mice OVA-induced sub-chronic airway inflammation model Oral 5 mg/kg, 20 mg/kg, 50 mg/kg Once daily, initiated on day 36 through day 58 Therapeutic H4R antagonism inhibited T cell infiltration into the lung and decreased Th2 cytokines IL-13 and IL-5. IL-13 dependent remodeling parameters such as GCH and lung collagen were reduced. Intervention with H4R antagonist also improved measures of central and peripheral airway dysfunction. PMC2914735

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.60mL

0.72mL

0.36mL

18.00mL

3.60mL

1.80mL

36.00mL

7.20mL

3.60mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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