1. GPCR/G Protein
    Immunology/Inflammation
  2. Histamine Receptor
  3. JNJ-39758979

JNJ-39758979 

Cat. No.: HY-101189 Purity: 98.01%
Handling Instructions

JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM.

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

JNJ-39758979 Chemical Structure

JNJ-39758979 Chemical Structure

CAS No. : 1046447-90-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 321 In-stock
Estimated Time of Arrival: December 31
1 mg USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 396 In-stock
Estimated Time of Arrival: December 31
10 mg USD 600 In-stock
Estimated Time of Arrival: December 31
50 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
100 mg USD 2520 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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Description

JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM.

IC50 & Target

Ki: 12.5 nM (histamine H4 receptor)[1]

In Vitro

JNJ-39758979 is a selective, high-affinity histamine H4 receptor antagonist with a Ki of 12.5 nM. The affinity of JNJ-39758979 for the rat (Ki=188 nM) and guinea pig H4R (Ki=306 nM) is moderate, and JNJ-39758979 has little if any affinity for the dog H4R (Ki≥10 μM). JNJ-39758979 is metabolically stable (t1/2 >120 min) when incubated in vitro with human, rat, dog, or monkey liver microsomes[1].

In Vivo

JNJ-39758979 shows dose-proportional pharmacokinetic (PK) in rat in the range of 2 to 500 mpK. JNJ-39758979 rapidly reaches the kidneys and liver (mean tmax=2.0 h). The elimination of JNJ-39758979 is slow from the brain, liver, and kidneys, with mean t1/2 values of 42.5, 22.3, and 20.5 h, respectively. The highest exposure (based on Cmax and AUC0-inf values) is observed in the liver followed by the kidney and brain. Tissue-to-plasma ratios for liver and kidney range from 23.2 to 95.8; the tissue-to-plasma ratios in brain increases with time from 0.256 to 22.7 up to 48 h after dosing. JNJ-39758979 is able to inhibit histamine-induced itch at doses of 5 and 20 mg/kg in mice. JNJ-39758979 exhibits dose-dependent inhibition of the clinical score in a mouse collagen-induced arthritis model[1].

Clinical Trial
Storage

4°C, protect from light

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (150.61 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.5188 mL 22.5938 mL 45.1875 mL
5 mM 0.9038 mL 4.5188 mL 9.0375 mL
10 mM 0.4519 mL 2.2594 mL 4.5188 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

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

    Solubility: ≥ 3.5 mg/mL (15.82 mM); Clear solution

  • 2.

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

    Solubility: ≥ 3.5 mg/mL (15.82 mM); Clear solution

  • 3.

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

    Solubility: ≥ 3.5 mg/mL (15.82 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Animal Administration
[1]

The model of histamine-induced scratching in C57/bl6 mice (n=6 to 8 per group) is used to judge the antipruritic effects of JNJ-39758979. JNJ-39758979 is given p.o. in 20% hydroxypropyl-β-cyclodextran 30 min before an intradermal injection of histamine (100 μg). Bouts of scratching are calculated using an automated system. Immediately after histamine injection, mice are placed in containers above a solenoid, and magnets previously placed on the mouse ear generate scratch-specific signals that are counted over a 20 min time span[1].

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

References
Molecular Weight

221.30

Formula

C₁₁H₁₉N₅

CAS No.

1046447-90-8

SMILES

NC1=NC(C(C)C)=CC(N2C[[email protected]](N)CC2)=N1

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
JNJ-39758979
Cat. No.:
HY-101189
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JNJ-39758979

Cat. No.: HY-101189