2. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease
  3. Orexin Receptor (OX Receptor) Cytochrome P450
  4. Nivasorexant

Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder.

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

Nivasorexant

Nivasorexant Chemical Structure

CAS No. : 1435480-40-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 1 publication(s) in Google Scholar

Nivasorexant Related Antibodies

Top Publications Citing Use of Products

View All Orexin Receptor (OX Receptor) Isoform Specific Products:

View All Isoforms
OX2 Receptor OX1 Receptor

View All Cytochrome P450 Isoform Specific Products:

View All Isoforms
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A CYP3A4 CYP17A1

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Nivasorexant (ACT-539313) is an orally active, blood-brain barrier penetrant, selective orexin OX1R inhibitor. Nivasorexant specifically blocks central OX1Rs without affecting OX2Rs, and exhibits competitive inhibitory activity against CYP2C8, CYP2C9, CYP2C19 and CYP3A4 (IC50 values are 25 μM, 8.6 μM, 1.6 μM, 19 μM/44 μM, respectively). Nivasorexant significantly reduces binge-like eating behavior of highly palatable food in rat models and has long-acting properties. Nivasorexant shows no relevant off-target activity against over 130 selected proteins, exhibits favorable safety profiles, and can be used for studies related to binge eating disorder[1][2].

IC50 & Target

OX1 Receptor

 

CYP2C9

8.6 μM (IC50)

CYP2C19

1.6<br/> μM (IC50)

CYP3A4

19 μM (IC50)

CYP3A4

44 μM (IC50)

In Vitro

Nivasorexant potently and selectively antagonizes human OX1R over OX2R in CHO cells, with an OX1R appKb of 0.5 nM and an OX2R appKb of 69 nM[1].
Nivasorexant potently and selectively antagonizes human OX1R over OX2R in HEK293 cells, with an OX1R Kb of 1.5 nM and an OX2R Kb of 172 nM[1].
Nivasorexant (up to 100 μM) potently inhibits recombinant CYP2C19 (IC50=1.6 μM, Ki=0.8 μM) and human liver microsomal CYP2C9 (IC50=8.6 μM, Ki=5.0 μM), moderately inhibits human liver microsomal CYP2C8 (IC50=25 μM) and CYP3A4 (IC50=19-44 μM), and weakly inhibits human liver microsomal CYP1A2, CYP2A6, CYP2B6, and CYP2D6 (IC50 >100 μM) in competitive reversible inhibition assays[2].
Nivasorexant (up to 100 μM; 30 min pre-incubated in the presence of NADPH) acts as a time-dependent irreversible inhibitor of recombinant CYP2C19 (IC50 shift=67, Ki=4.2 μM, kinact=0.079 min-1) but does not exhibit time-dependent inhibition of human liver microsomal CYP2C8, CYP2C9, CYP2D6, or CYP3A4[2].

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

Nivasorexant Related Antibodies
In Vivo

Nivasorexant (1.5-50 mg/kg; p.o.; single dose, 1 h pre-test; daily for 10 consecutive days) dose-dependently reduces binge-like highly palatable food intake in a rat model of binge-eating disorder via selective OX1R blockade, with efficacy maintained under repeated stress and chronic daily dosing, and induces compensatory increases in hypothalamic orexin-A and ΔFosB expression[1].

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

Animal Model: Sprague Dawley (female, 9 weeks old, 200-225 g at study start, binge-eating disorder model via three 8-day cycles of intermittent dieting with intermittent highly palatable food access, frustration stress challenge)[1]
Dosage: 1.5 mg/kg; 5 mg/kg; 15 mg/kg; 50 mg/kg
Administration: p.o.; single dose, 1 h pre-test; daily for 10 consecutive days (15 mg/kg only)
Result: Reduced binge-like highly palatable food intake in a dose-dependent manner (p < .001).
Achieved calculated free brain concentrations corresponding to 57%-80% OX1R occupancy and <3% OX2R occupancy at the lowest efficacious dose of 5 mg/kg.
Showed no effect on highly palatable food intake under control conditions (no restriction/no stress, restriction/no stress, no restriction/stress, no restriction/repeated stress).
Maintained efficacy under repeated stress exposure and after chronic daily dosing for 10 days.
Increased the number of orexin-A-positive neurons in the lateral hypothalamus (p < .01), perifornical area (p = .03), and nominally in the dorsomedial hypothalamus (p = .08).
Increased ΔFosB-positive cells in the perifornical area (p = .03) and nominally in the lateral hypothalamus (p = .09).
Molecular Weight

429.47

Formula

C23H23N7O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C1=CC=C(C)C=C1N2N=CC=N2)N3[C@H](CC4=CC=CC(N5N=CC=N5)=C4)COCC3
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 : 100 mg/mL (232.85 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 2.3285 mL 11.6423 mL 23.2845 mL
5 mM 0.4657 mL 2.3285 mL 4.6569 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
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Concentration
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Volume
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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: ≥ 5 mg/mL (11.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (11.64 mM); Clear solution

    This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 2.3285 mL 11.6423 mL 23.2845 mL 58.2113 mL
5 mM 0.4657 mL 2.3285 mL 4.6569 mL 11.6423 mL
10 mM 0.2328 mL 1.1642 mL 2.3285 mL 5.8211 mL
15 mM 0.1552 mL 0.7762 mL 1.5523 mL 3.8808 mL
20 mM 0.1164 mL 0.5821 mL 1.1642 mL 2.9106 mL
25 mM 0.0931 mL 0.4657 mL 0.9314 mL 2.3285 mL
30 mM 0.0776 mL 0.3881 mL 0.7762 mL 1.9404 mL
40 mM 0.0582 mL 0.2911 mL 0.5821 mL 1.4553 mL
50 mM 0.0466 mL 0.2328 mL 0.4657 mL 1.1642 mL
60 mM 0.0388 mL 0.1940 mL 0.3881 mL 0.9702 mL
80 mM 0.0291 mL 0.1455 mL 0.2911 mL 0.7276 mL
100 mM 0.0233 mL 0.1164 mL 0.2328 mL 0.5821 mL
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Nivasorexant 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:

Nivasorexant1435480-40-2ACT-539313ACT539313ACT 539313Orexin Receptor (OX Receptor)Cytochrome P450Hypocretin ReceptorHCRT ReceptorCYPsOX1RCHO cellsCYP2C9orexin 1 receptorHEK293 cellsbinge-eating disorderblood-brain barrierCYP2C19CYP3A4OX2RsInhibitorinhibitorinhibit

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