Almorexant hydrochloride
Based on 9 publication(s) in Google Scholar
Almorexant (ACT 078573) hydrochloride 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 hydrochloride reversibly blocks signaling of orexin-A and orexin-B peptides. Almorexant hydrochloride totally blocked the intracellular Ca2+ signal pathway. Almorexant hydrochloride stimulates caspase-3 activity in AsPC-1 cells and induces apoptosis.
For research use only. We do not sell to patients.
- Purity : 99.98%
- CAS No.: 913358-93-7
- Formula: C29H32ClF3N2O3
- Molecular Weight:549.02
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Storage:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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HY-100452
TCS-OX2-29OX2R Antagonist -
HY-10895
SB-334867OX1 Receptor Antagonist -
HY-101103
HP-β-CDCo-solvent -
HY-76612
SB-408124 HydrochlorideOX1 Receptor Antagonist -
HY-109012A
Seltorexant hydrochlorideOrexin-2 Receptor Antagonist -
HY-70068
SB-408124OX1 Receptor Antagonist -
HY-136181
YNT-185 dihydrochlorideOrexin Receptor 2 Agonist -
HY-10805
AlmorexantOrexin Receptor Antagonist -
HY-19914
MK-1064OX2R Antagonist -
HY-10895A
SB-334867 free baseOX1 Antagonist -
HY-10805AR
Almorexant hydrochloride (Standard)Reference Standard -
HY-10898
SB-674042OX1 Receptor Antagonist
Publications Citing Use of MedChemExpress (MCE) Almorexant hydrochloride
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
More
Biological Activity
Description
IC50 & Target
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human OX2R 0.17 nM (Kd) |
human OX1R 1.3 nM (Kd) |
Caspase-3 |
In Vitro
Almorexant hydrochloride (1 μM) promote tyrosine phosphorylation of SHP2/OX1R complex[1].
Almorexant hydrochloride (1 μM) inhibits the cellular growth of AsPC-1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
Almorexant hydrochloride (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning[4].
Almorexant hydrochloride (30-300 mg/kg) dose-dependently increases rapid eye movement (REM) and non-REM (NREM) sleep and decreases wakefulness apparently without inducing either cataplexy 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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 913358-93-7
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Appearance Solid
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Molecular Weight 549.02
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Formula C29H32ClF3N2O3
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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.Cl
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Synonyms
ACT 078573 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 hydrochloride 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
In Vitro:
DMSO : 100 mg/mL (182.14 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.55 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.55 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 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:
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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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Protocols
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Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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TUNEL staining for apoptotic DNA fragmentation
TUNEL staining detects DNA strand breaks by using terminal deoxynucleotidyl transferase to add labeled nucleotides to exposed 3′-OH DNA termini, generating either microscopic staining in fixed cells or tissue sections, or fluorescence/cytometric signal in cell suspensions. TUNEL positivity reflects DNA fragmentation but should not be interpreted alone as definitive apoptosis, because TUNEL can also label necrotic, autolytic, mechanically damaged, or DNA-repair-associated DNA breaks.
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Annexin V plus membrane-impermeant dye apoptosis staining
Annexin V-based apoptosis assays rely on the detection of phosphatidylserine (PS) externalization from the inner leaflet of the plasma membrane to the outer leaflet, an early biochemical hallmark of apoptosis. Fluorescently labeled Annexin V binds PS in a calcium-dependent manner, enabling identification of early apoptotic cells by flow cytometry or fluorescence microscopy. When combined with a membrane-impermeant DNA-binding dye (e. g. , propidium iodide), this approach allows discrimination between viable (Annexin V−/dye−), early apoptotic (Annexin V+/dye−), and late apoptotic or necrotic (Annexin V+/dye+) cell populations by assessing membrane integrity and PS exposure.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Ca2+ Staining Technique
Ca2+ staining is an experimental technique that utilizes specific fluorescent probes (such as Fluo-4 AM, Fura-2, etc.) to qualitatively or quantitatively detect dynamic changes in intracellular Ca2+ concentrations; this is achieved by monitoring the changes in fluorescent signals generated when these probes bind to free intracellular calcium ions. The underlying principle relies primarily on the presence of chelating groups within the probe's molecular structure that possess high affinity for calcium ions.
Purity & Documentation
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Data Sheet (286 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 1.8214 mL | 9.1071 mL | 18.2143 mL | 45.5357 mL |
| 5 mM | 0.3643 mL | 1.8214 mL | 3.6429 mL | 9.1071 mL | |
| 10 mM | 0.1821 mL | 0.9107 mL | 1.8214 mL | 4.5536 mL | |
| 15 mM | 0.1214 mL | 0.6071 mL | 1.2143 mL | 3.0357 mL | |
| 20 mM | 0.0911 mL | 0.4554 mL | 0.9107 mL | 2.2768 mL | |
| 25 mM | 0.0729 mL | 0.3643 mL | 0.7286 mL | 1.8214 mL | |
| 30 mM | 0.0607 mL | 0.3036 mL | 0.6071 mL | 1.5179 mL | |
| 40 mM | 0.0455 mL | 0.2277 mL | 0.4554 mL | 1.1384 mL | |
| 50 mM | 0.0364 mL | 0.1821 mL | 0.3643 mL | 0.9107 mL | |
| 60 mM | 0.0304 mL | 0.1518 mL | 0.3036 mL | 0.7589 mL | |
| 80 mM | 0.0228 mL | 0.1138 mL | 0.2277 mL | 0.5692 mL | |
| 100 mM | 0.0182 mL | 0.0911 mL | 0.1821 mL | 0.4554 mL |
Almorexant hydrochloride Related Classifications
HY-10805A Related Classifications
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