1. GPCR/G Protein
  2. Orexin Receptor (OX Receptor)

Nemorexant (Synonyms: ACT-541468)

Cat. No.: HY-109095 Purity: 99.47%
Handling Instructions

Nemorexant (ACT-541468) is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively.

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

Nemorexant Chemical Structure

Nemorexant Chemical Structure

CAS No. : 1505484-82-1

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 446 In-stock
Estimated Time of Arrival: December 31
1 mg USD 150 In-stock
Estimated Time of Arrival: December 31
5 mg USD 450 In-stock
Estimated Time of Arrival: December 31
10 mg USD 750 In-stock
Estimated Time of Arrival: December 31
25 mg USD 1500 In-stock
Estimated Time of Arrival: December 31
50 mg USD 2200 In-stock
Estimated Time of Arrival: December 31
100 mg USD 3500 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Nemorexant (ACT-541468) is a potent orexin receptor antagonist extracted from patent WO2015083094A1, compound example 7, has IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively.

IC50 & Target

IC50: 2 nM (Ox1 receptor ), 3 nM (Ox2 receptor)[1]

In Vitro

Nemorexant (Compound example 7) is a orexin receptor antagonist with IC50s of 2 nM and 3 nM for Ox1 receptor and Ox2 receptor, respectively[1].

Solvent & Solubility
In Vitro: 

DMSO : ≥ 250 mg/mL (554.42 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2177 mL 11.0884 mL 22.1769 mL
5 mM 0.4435 mL 2.2177 mL 4.4354 mL
10 mM 0.2218 mL 1.1088 mL 2.2177 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[1]

Chinese hamster ovary (CHO) cells expressing the human orexin-1 receptor and the human orexin-2 receptor, respectively, are grown in culture medium (Ham F-12 with L-Glutamine) containing 300 μg/mL G418, 100 U/mL Penicillin, 100 μg/mL Streptomycin and 10 % heat inactivated fetal calf serum (FCS). The cells are seeded at 20,000 cells / well into 384-well black clear bottom sterile plates. The seeded plates are incubated overnight at 37°C in 5% CO2. Human orexin-A as an agonist is prepared as 1 mM stock solution in MeOH: water (1 :1), diluted in HBSS containing 0.1 % bovine serum albumin (BSA), NaHCO3: 0.375g/L and 20 mM HEPES for use in the assay at a final concentration of 3 nM. Antagonists are prepared as 10 mM stock solution in DMSO, then diluted in 384-well plates using DMSO followed by a transfer of the dilutions into in HBSS containing 0.1 % bovine serum albumin (BSA), NaHCO3: 0.375g/L and 20 mM HEPES. On the day of the assay, 50 μL of staining buffer (HBSS containing 1 % FCS, 20 mM HEPES, NaHCO3: 0.375g/L, 5 mM probenecid and 3 μM of the fluorescent calcium indicator fluo-4 AM (1 mM stock solution in DMSO, containing 10% pluronic) is added to each well. The 384-well cell-plates are incubated for 50 min at 37°C in 5% CO2 followed by equilibration at RT for 30 min before measurement. Within the Fluorescent Imaging Plate Reader, antagonists are added to the plate in a volume of 10 μL/well, incubated for 120 min and finally 10 μL/well of agonist is added. Fluorescence is measured for each well at 1 second intervals, and the height of each fluorescence peak is compared to the height of the fluorescence peak induced by an approximate EC70 (for example 5 nM) of orexin-A with vehicle in place of antagonist. The IC50 value is determined[1].

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

References
Molecular Weight

450.92

Formula

C₂₃H₂₃ClN₆O₂

CAS No.

1505484-82-1

SMILES

C[[email protected]](CCC1)(C2=NC3=CC=C(Cl)C(C)=C3N2)N1C(C4=C(N5N=CC=N5)C=CC(OC)=C4)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Nemorexant
Cat. No.:
HY-109095
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Nemorexant

Cat. No.: HY-109095