1. GPCR/G Protein Neuronal Signaling
  2. Orexin Receptor (OX Receptor)
  3. JNJ-10397049

JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold selective for the OX2R over the OX1R.

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

JNJ-10397049 Chemical Structure

JNJ-10397049 Chemical Structure

CAS No. : 708275-58-5

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Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 141 In-stock
Solution
10 mM * 1 mL in DMSO USD 141 In-stock
Solid
5 mg USD 132 In-stock
10 mg USD 220 In-stock
25 mg USD 440 In-stock
50 mg USD 770 In-stock
100 mg USD 1155 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

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  • Biological Activity

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Description

JNJ-10397049 is a potent and selective orexin 2 receptor (OX2R) antagonist, with a pKi of 8.3. JNJ-10397049 is 600-fold selective for the OX2R over the OX1R[1][2].

In Vivo

JNJ-10397049 (10-30 mg/kg) decreases the latency for persistent sleep and increased nonrapid eye movement and rapid eye movement sleep time[2].
JNJ-10397049 blocks ethanol self-administration, place preference and reinstatement[3].

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

Animal Model: Male Sprague-Dawley rats[2].
Dosage: 10 mg/kg.
Administration: Subcutaneous administration.
Result: Induced a significant reduction in NREM sleep latency and an increase in NREM sleep duration during the first 2 h after administration relative to vehicle treatment.
Molecular Weight

484.18

Formula

C19H20Br2N2O3

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

BrC1=C(NC(N[C@@H]2[C@H](C3=CC=CC=C3)OC(C)(C)OC2)=O)C=CC(Br)=C1

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 : 170 mg/mL (351.11 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0653 mL 10.3267 mL 20.6535 mL
5 mM 0.4131 mL 2.0653 mL 4.1307 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)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

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: 4.25 mg/mL (8.78 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 4.25 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (42.5 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% Corn Oil

    Solubility: ≥ 4.25 mg/mL (8.78 mM); Clear solution

    This protocol yields a clear solution of ≥ 4.25 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (42.5 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

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
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 2.0653 mL 10.3267 mL 20.6535 mL 51.6337 mL
5 mM 0.4131 mL 2.0653 mL 4.1307 mL 10.3267 mL
10 mM 0.2065 mL 1.0327 mL 2.0653 mL 5.1634 mL
15 mM 0.1377 mL 0.6884 mL 1.3769 mL 3.4422 mL
20 mM 0.1033 mL 0.5163 mL 1.0327 mL 2.5817 mL
25 mM 0.0826 mL 0.4131 mL 0.8261 mL 2.0653 mL
30 mM 0.0688 mL 0.3442 mL 0.6884 mL 1.7211 mL
40 mM 0.0516 mL 0.2582 mL 0.5163 mL 1.2908 mL
50 mM 0.0413 mL 0.2065 mL 0.4131 mL 1.0327 mL
60 mM 0.0344 mL 0.1721 mL 0.3442 mL 0.8606 mL
80 mM 0.0258 mL 0.1291 mL 0.2582 mL 0.6454 mL
100 mM 0.0207 mL 0.1033 mL 0.2065 mL 0.5163 mL
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JNJ-10397049 Related Classifications

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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