1. GPCR/G Protein
    Neuronal Signaling
    Immunology/Inflammation
  2. Histamine Receptor
  3. JNJ-5207852

JNJ-5207852 

Cat. No.: HY-12190 Purity: >98.0%
Handling Instructions

JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.

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

JNJ-5207852 Chemical Structure

JNJ-5207852 Chemical Structure

CAS No. : 398473-34-2

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
Estimated Time of Arrival: December 31
10 mg USD 140 In-stock
Estimated Time of Arrival: December 31
50 mg USD 580 In-stock
Estimated Time of Arrival: December 31
100 mg USD 980 In-stock
Estimated Time of Arrival: December 31
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Description

JNJ-5207852 is a selective and potent histamine H3 receptor (H3R) antagonist, with pKis of 8.9, 9.24 for rat and human H3R, respectively.

IC50 & Target[1][2]

H3 receptor

8.9 (pKi, for rat)

H3 receptor

9.24 (pKi, for human)

In Vivo

In mice and rats, JNJ-5207852 (1-10mg/kg s.c.) increases time spent awake and decreases REM sleep and slow-wave sleep, but fails to have an effect on wakefulness or sleep in H3 receptor knockout mice. No rebound hypersomnolence, as measured by slow-wave delta power, is observed. The wake promoting effects of this H3 receptor antagonist are not associated with hypermotility. A 4-week daily treatment of mice with JNJ-5207852 (10 mg/kg i.p.) does not lead to a change in body weight, possibly due to the compound being a neutral antagonist at the H3 receptor. JNJ-5207852 is extensively absorbed after oral administration and reaches high brain levels[1].

Molecular Weight

316.48

Formula

C₂₀H₃₂N₂O

CAS No.

398473-34-2

SMILES

N1(CCCOC2=CC=C(CN3CCCCC3)C=C2)CCCCC1

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 : 77.5 mg/mL (244.88 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.1598 mL 15.7988 mL 31.5976 mL
5 mM 0.6320 mL 3.1598 mL 6.3195 mL
10 mM 0.3160 mL 1.5799 mL 3.1598 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: ≥ 2.58 mg/mL (8.15 mM); Clear solution

  • 2.

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

    Solubility: ≥ 2.58 mg/mL (8.15 mM); Clear solution

  • 3.

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

    Solubility: ≥ 2.58 mg/mL (8.15 mM); Clear solution

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

Rats[1]
Male, Sprague-Dawley rats weighing 282-334 g are used. The animals are individually housed with free access to food and water. To assure that there are no pre-existing group differences in activity levels prior to the initiation of treatment, LMA is monitored and recorded during a 2 h habituation period. Following the 2 h habituation period, testing is briefly interrupted and animals are s.c. injected with either saline (1 mL/kg; n=6), JNJ-5207852 (3, 10, 30 mg/kg; n=6-7 animals/group) or Damphetamine (0.75 mg/kg; n=6). Testing is immediately resumed following the compound injection[1].

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

References
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Product Name:
JNJ-5207852
Cat. No.:
HY-12190
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