JNJ-7777120

Catalog No.S2905

JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.

Price Stock Quantity  
USD 190 In stock
USD 147 In stock
USD 370 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

JNJ-7777120 Chemical Structure

JNJ-7777120 Chemical Structure
Molecular Weight: 277.75

Validation & Quality Control

Quality Control & MSDS

Related Compound Libraries

JNJ-7777120 is available in the following compound libraries:

Product Information

  • Compare Histamine Receptor Antagonists
    Compare Histamine Receptor Products
  • Research Area

Product Description

Biological Activity

Description JNJ-7777120 is the first potent and selective non-imidazole histamine H4 receptor antagonist with Ki of 4.5 nM, exhibits >1000-fold selectivity over the other histamin receptors.
Targets Histamine H4 receptor [1]
IC50 4.5 nM(Ki)
In vitro JNJ 7777120 binds with high affinity to the H4 receptor and has a greater than 1000-fold selectivity over the other histamine receptors. JNJ 7777120 is a selective and potent H4 receptor antagonist with little or no affinity for over 50 other targets. [2]
In vivo JNJ 7777120 has an oral bioavailability of ~30% in rats and 100% in dogs, with a half-life of ∼3 h in both species. JNJ 7777120 blocks histamine-induced chemotaxis and calcium influx in mouse bone marrow-derived mast cells. JNJ 7777120 can block the histamine-induced migration of tracheal mast cells from the connective tissue toward the epithelium in mice. JNJ 7777120 significantly blocks neutrophil infiltration in a mouse zymosan-induced peritonitis model. [2]
Features

Protocol(Only for Reference)

Kinase Assay: [1]

Binding assay Cell pellets from SK-N-MC cells transfected with human, rat, or mouse H4 receptor, human H3 receptor, or human H1 receptor are used. For the mouse H1 receptor binding, fresh mouse brain is used. Cell pellets or mouse brain are homogenized in 50 mM Tris pH 7.5 containing 5 mM EDTA, and supernatants from an 800g spin are collected and recentrifuged at 30,000g for 30 min. Pellets are rehomogenized in 50 mM Tris pH 7.5 containing 5 mM EDTA. For the H4 competition binding studies, human, mouse, and rat cell membranes are incubated with 10, 40, and 150 nM [3H]histamine (specific activity 23 Ci/mmol), respectively, with or without JNJ 7777120 for 45 min at 25°C. Nonspecific binding is defined using 100 μM unlabeled histamine. The Kd values for the human, mouse, and rat H4 receptor are determined to be 5, 42, and 178 nM, respectively, and the Bmax values are determined to be 1.12, 1.7, and 0.68 pmol/mg protein, respectively. Similarly, the ligand used for the H3receptor-binding assays is [3H]N-α-methyl histamine (specific activity, 82 Ci/mmol), and the nonspecific binding is defined using 100 μM unlabeled histamine. The Kd values for the human and rat H3 receptor are determined to be 1 and 0.8 nM, respectively, and the Bmax values are 2.13 and 0.4 pmol/mg protein, respectively. The ligand used for the human and mouse H1 receptor binding is [3H]pyrilamine (specific activity, 20 Ci/mmol), and the nonspecific binding is defined using 10 μM unlabeled diphenhydramine. The Kd is 1 nM for human receptor and 3 nM for the mouse receptor. The Bmax is 2.68 pmol/mg protein for the human receptor and 0.2 pmol/mg protein for the mouse receptor. The binding to the guinea pig H1 and H2 receptors is determined by Cerep, Inc. For the H1 receptor-binding assays, guinea pig cerebellum is used. The radioligand is [3H]pyrilamine, and 100 μM triprolidine is used to determine the nonspecific binding. For the H2 receptor-binding assays, guinea pig striatum is used. The radioligand is [3H]aspartate amino-transferase, and 100 μM tiotidine is used to determine the nonspecific binding. The Kd of [3H]JNJ 7777120 (specific activity, 84 Ci/mmol) for the human and mouse H4 receptor is determined essentially as described above using increasing concentrations of [3H]JNJ 7777120 instead of [3H]histamine in the presence of 100 μM unlabeled histamine. For all studies, the Ki values are calculated based on an experimentally determined appropriate Kd value.

Animal Study: [2]

Animal Models Female BALB/c mice
Formulation 5% (w/v) dextrose in water
Dosages 200 mg/kg
Administration P.O.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Jablonowski JA, et al. J Med Chem, 2003, 46(19), 3957-3960.

[2] Thurmond RL, et al. J Pharmacol Exp Ther, 2004, 309(1), 404-413.

Chemical Information

Download JNJ-7777120 SDF
Molecular Weight (MW) 277.75
Formula

C14H16ClN3O

CAS No. 459168-41-3
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 56 mg/mL (201.62 mM)
Ethanol 8 mg/mL (28.8 mM)
Water <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 20 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Name Methanone, (5-chloro-1H-indol-2-yl)(4-methyl-1-piperazinyl)-

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Histamine Receptor Products

  • AZD3839

    AZD3839 is a potent and selective BACE1 inhibitor with Ki of 26.1 nM, about 14-fold selectivity over BACE2. Phase 1.

  • Xanthohumol

    Xanthohumol, a prenylated chalcone from hop, inhibits COX-1 and COX-2 activity and shows chemopreventive effects. Phase 1.

  • A-438079 HCl

    A-438079 HCl is a potent, and selective P2X7 receptor antagonist with pIC50 of 6.9.

  • Loratadine

    Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.

  • Azelastine HCl

    Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.

  • Clemastine Fumarate

    Clemastine Fumarate (Clemastine) is a selective histamine H1 receptor antagonist with IC50 of 3 nM.

  • Histamine Phosphate

    Histamine acts directly on the blood vessels to dilate arteries and capillaries mediated by both H 1- and H 2-receptors.

    Features:Histamine phosphate is indicated as a diagnostic aid for evaluation of gastric acid secretory function.

  • Lidocaine

    Lidocaine is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM.

  • Pemirolast potassium

    Pemirolast potassium (BMY 26517) is a histamine H1 antagonist and mast cell stabilizer that acts as an antiallergic agent.

  • Nizatidine

    Nizatidine is a histamine H2 receptor antagonist with IC50 of 0.9 nM, also inhibits AChE with IC50 of 6.7 μM.

Recently Viewed Items

Tags: buy JNJ-7777120 | JNJ-7777120 supplier | purchase JNJ-7777120 | JNJ-7777120 cost | JNJ-7777120 manufacturer | order JNJ-7777120 | JNJ-7777120 distributor
×
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us