2. GPCR/G Protein Neuronal Signaling
  3. Orexin Receptor (OX Receptor)
  4. JNJ-54717793

JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders.

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JNJ-54717793 Chemical Structure

JNJ-54717793 Chemical Structure

CAS No. : 1628843-99-1

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Based on 1 publication(s) in Google Scholar

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Description

JNJ-54717793, as a brain penetrant, is an orally active, selective and high affinity orexin-1 receptor (OX1R) antagonist (plasma EC50=85 ng/mL). The Ki values of JNJ-54717793 for hOX1R (human OX1R) and hOX2R are 16 nM and 700 nM, respectively. JNJ-54717793 is a potent compound of anxiety disorders[1][2].

IC50 & Target[1]

human OX1R

16 nM (Ki)

human OX2R

700 nM (Ki)

OX1 Receptor

85 ng/mL (EC50)

In Vivo

JNJ-5471779 (30 mg/kg; p.o.; 6 hours) significantly reduces the latency for rapid eye movement (REM) sleep and prolongs the time spent in REM sleep[2].
JNJ-5471779 (3~30 mg/kg; p.o.) attenuates bradycardia responses[2].
JNJ-5471779 (5mg/kg; p.o.) shows low clearance[1].

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

Animal Model: OX2R KO mice[2]
Dosage: 30 mg/kg
Administration: P.o.
Result: Significantly reduced the latency for rapid eye movement (REM) sleep and prolonged the time spent in REM sleep.
Animal Model: Rat[2]
Dosage: 3~30 mg/kg
Administration: P.o.
Result: Attenuated bradycardia responses.
Animal Model: Mouse[1]
Dosage: 5.0 mg/kg (Pharmacokinetic Analysis)
Administration: P.o.
Result: Clearance was found to be low.
Molecular Weight

458.41

Formula

C22H18F4N6O
CAS No.
Appearance

Solid

Color

Off-white to pink

SMILES

O=C(C1=C(C2=NC=CC=N2)C(F)=CC=C1)N3[C@H](CC[C@@H]43)C[C@H]4NC5=CN=C(C(F)(F)F)C=N5
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 : 240 mg/mL (523.55 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 2.1815 mL 10.9073 mL 21.8145 mL
5 mM 0.4363 mL 2.1815 mL 4.3629 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • 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: ≥ 6 mg/mL (13.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 6 mg/mL (13.09 mM); Clear solution

    This protocol yields a clear solution of ≥ 6 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (60.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.1815 mL 10.9073 mL 21.8145 mL 54.5363 mL
5 mM 0.4363 mL 2.1815 mL 4.3629 mL 10.9073 mL
10 mM 0.2181 mL 1.0907 mL 2.1815 mL 5.4536 mL
15 mM 0.1454 mL 0.7272 mL 1.4543 mL 3.6358 mL
20 mM 0.1091 mL 0.5454 mL 1.0907 mL 2.7268 mL
25 mM 0.0873 mL 0.4363 mL 0.8726 mL 2.1815 mL
30 mM 0.0727 mL 0.3636 mL 0.7272 mL 1.8179 mL
40 mM 0.0545 mL 0.2727 mL 0.5454 mL 1.3634 mL
50 mM 0.0436 mL 0.2181 mL 0.4363 mL 1.0907 mL
60 mM 0.0364 mL 0.1818 mL 0.3636 mL 0.9089 mL
80 mM 0.0273 mL 0.1363 mL 0.2727 mL 0.6817 mL
100 mM 0.0218 mL 0.1091 mL 0.2181 mL 0.5454 mL
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JNJ-54717793 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.

Keywords:

JNJ-547177931628843-99-1JNJ54717793JNJ 54717793Orexin Receptor (OX Receptor)Hypocretin ReceptorHCRT ReceptorpenetrantorallyselectiveaffinityanxietydisordersInhibitorinhibitorinhibit

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