Almorexant
Based on 9 publication(s) in Google Scholar
Almorexant (ACT 078573) is an orally active, potent and competitive dual orexin receptor antagonist, with Kd values of 1.3 nM (OX1) and 0.17 nM (OX2), respectively. Almorexant reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant totally blocked the intracellular Ca2+ signal pathway. Almorexant stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.
For research use only. We do not sell to patients.
- Purity: 99.96%
- CAS No.: 871224-64-5
- Formula: C29H31F3N2O3
- Molecular Weight:512.56
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Apoptosis Compound Library
HY-L003
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GPCR/G Protein Compound Library
HY-L006
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Membrane Transporter/Ion Channel Compound Library
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HY-L025
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HY-L059
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Mass Spectrometry Human Metabolite Library
HY-L215
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Lactylation Compound Library
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Publications Citing Use of MedChemExpress (MCE) Almorexant
More- Cell Metab. 2018 Jul 3;28(1):118-129.e5. [Abstract]
- Nat Neurosci. 2024 Sep;27(9):1774-1782. [Abstract]
- Eur J Pharmacol. 2025 Jul 5:998:177498. [Abstract]
- Brain Res Bull. 2026 Mar:236:111762. [Abstract]
- ETH Zurich. 2025.
- SSRN. 2025 Jun 18.
- bioRxiv. 2025 February 25.
- bioRxiv. 2023 Jul 19.
- Oncotarget. 2018 Jan 9;9(6):6952-6967. [Abstract]
Customer Validation & Images
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WB
All Orexin Receptor (OX Receptor) Isoforms
MoreAll Calcium Channel Isoforms
MoreAll Caspase Isoforms
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Biological Activity
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human OX2R 0.17 nM (Kd) |
human OX1R 1.3 nM (Kd) |
Caspase-3 |
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Cell Line
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Type | Value | Description | References |
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| CHO | IC50 |
13 nM
Compound: ACT-078573
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Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
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[PMID: 23719231] |
| CHO | IC50 |
13 nM
Compound: 15
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Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release
Antagonist activity at human OX1R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release
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[PMID: 26317591] |
| CHO | IC50 |
8 nM
Compound: ACT-078573
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Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of calcium mobilization by FLIPR assay
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[PMID: 23719231] |
| CHO | IC50 |
8 nM
Compound: 15
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Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release
Antagonist activity at human OX2R expressed in CHO cells assessed as inhibition of orexin-A-induced intracellular calcium release
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[PMID: 26317591] |
Almorexant (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning[4].
Almorexant (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy18 or deficits in next-day performance[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice xenografted with AsPC-1 cells[2]
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Dosage:1.8 μmol/kg, 100 μL
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Administration:IP, daily, starting at day 0 or day 38
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Result:Resulted in a significant decrease in tumor volume when treatment starting at day 0. Started after AsPC-1 tumors were developed (day 38), rapidly and strongly reduced the volume of established tumors.
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Animal Model:Long-Evans rats (24, male, 16-18 weeks of age)[4]
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Dosage:300 mg/kg
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Administration:PO, once
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Result:Successfully learned the spatial task, established spatial memory.
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Animal Model:Male C57BL/6 mice (Orexin/ataxin-3 transgenic (TG) mice and WT mice, 32 ± 0.9 g, age 15 ± 0.5 week)[3]
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Dosage:30, 100, 300 mg/kg (3, 10, and 30 mg/mL; 10 mL/kg)
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Administration:IP, once every 3 days
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Result:Exacerbated cataplexy in TG mice and increased nonrapid eye movement (NREM) sleep with heightened sleep/wake fragmentation in both genotypes during the 12-h dark period after dosing. Showed greater hypnotic potency in WT mice than in TG mice.
Chemical Information
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CAS No. 871224-64-5
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Appearance Solid
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Molecular Weight 512.56
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Formula C29H31F3N2O3
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Color White to off-white
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SMILES
CNC([C@@H](C1=CC=CC=C1)N2CCC3=CC(OC)=C(OC)C=C3[C@@H]2CCC4=CC=C(C(F)(F)F)C=C4)=O
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Synonyms
ACT 078573
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (9)
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Journal Impact Factor
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Most Recent
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Cell Metab
A Role for Hypocretin/Orexin in Metabolic and Sleep Abnormalities in a Mouse Model of Non-metastatic Breast Cancer. [Abstract]2018 Jul 3;28(1):118-129.e5. PMID: 29805100 -
Nat Neurosci
2024 Sep;27(9):1774-1782. PMID: 39107488 -
Eur J Pharmacol
Parishin A alleviates insomnia by regulating hypothalamic-pituitary-adrenal axis homeostasis and directly targeting orexin receptor OX2. [Abstract]2025 Jul 5:998:177498. PMID: 40064224 -
Brain Res Bull
Orexin dual receptor antagonist attenuates neurological deficits possibly via PI3K/Akt/mTOR pathway activation in sleep-deprived stroke rats. [Abstract]2026 Mar:236:111762. PMID: 41651248 -
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Oncotarget
In vitro, in vivo and ex vivo demonstration of the antitumoral role of hypocretin-1/orexin-A and almorexant in pancreatic ductal adenocarcinoma. [Abstract]2018 Jan 9;9(6):6952-6967. PMID: 29467942
Almorexant purchased from MedChemExpress. Usage Cited in: Oncotarget. 2018 Jan 9;9(6):6952-6967. [Abstract]
Orexin-A and Almorexant promote tyrosine phosphorylation of SHP2/OX1R complex
Solvent & Solubility
DMSO : 100 mg/mL (195.10 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.88 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (283 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Dayot S, et al. In vitro, in vivo and ex vivo demonstration of the antitumoral role of hypocretin-1/orexin-A and almorexant in pancreatic ductal adenocarcinoma. Oncotarget. 2018 Jan 9;9(6):6952-6967. [Content Brief]
[2]. Malherbe P, et al. Biochemical and electrophysiological characterization of almorexant, a dual orexin 1 receptor (OX1)/orexin 2 receptor (OX2) antagonist: comparison with selective OX1 and OX2 antagonists. Mol Pharmacol. 2009 Sep;76(3):618-31. [Content Brief]
[3]. Black SW, et al. Almorexant promotes sleep and exacerbates cataplexy in a murine model of narcolepsy. Sleep. 2013 Mar 1;36(3):325-36. [Content Brief]
[4]. Dietrich H, et al. Intact learning and memory in rats following treatment with the dual orexin receptor antagonist almorexant. Psychopharmacology (Berl). 2010 Oct;212(2):145-54. [Content Brief]
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 | 1.9510 mL | 9.7550 mL | 19.5099 mL | 48.7748 mL |
| 5 mM | 0.3902 mL | 1.9510 mL | 3.9020 mL | 9.7550 mL | |
| 10 mM | 0.1951 mL | 0.9755 mL | 1.9510 mL | 4.8775 mL | |
| 15 mM | 0.1301 mL | 0.6503 mL | 1.3007 mL | 3.2517 mL | |
| 20 mM | 0.0975 mL | 0.4877 mL | 0.9755 mL | 2.4387 mL | |
| 25 mM | 0.0780 mL | 0.3902 mL | 0.7804 mL | 1.9510 mL | |
| 30 mM | 0.0650 mL | 0.3252 mL | 0.6503 mL | 1.6258 mL | |
| 40 mM | 0.0488 mL | 0.2439 mL | 0.4877 mL | 1.2194 mL | |
| 50 mM | 0.0390 mL | 0.1951 mL | 0.3902 mL | 0.9755 mL | |
| 60 mM | 0.0325 mL | 0.1626 mL | 0.3252 mL | 0.8129 mL | |
| 80 mM | 0.0244 mL | 0.1219 mL | 0.2439 mL | 0.6097 mL | |
| 100 mM | 0.0195 mL | 0.0975 mL | 0.1951 mL | 0.4877 mL |
Almorexant Related Classifications
HY-10805 Related Classifications
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