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Technical Data
| Formula | C29H32ClF3N2O3 |
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| Molecular Weight | 549.02 | CAS No. | 913358-93-7 | |
| Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (182.14 mM) | |
| Ethanol | 100 mg/mL (182.14 mM) | |||
| Water | Insoluble | |||
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
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Preparing Stock Solutions
Biological Activity
| Description | Almorexant HCl (ACT-078573) is an orally active, dual orexin receptor antagonist with IC50 of 6.6 nM and 3.4 nM for OX1 and OX2 receptor, respectively. Phase 3. | ||||
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| Targets |
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| In vitro | Almorexant inhibits the increase in intracellular Ca2+ induced by 10 nM human orexin-A in Chinese hamster ovary cells with IC50 of 16 nM (rat) and 13 nM (human) for the OX1 receptor and 15 nM (rat) and 8 nM (human) for the OX2 receptor. [1] | ||||
| In vivo | Almorexant (300 mg/kg p.o.) decreases alertness, and increases electrophysiological indices of both non-REM and REM sleep in male Wistar rats. In dogs, Almorexant (100 mg/kg p.o.) causes somnolence and increases surrogate markers of REM sleep. [1] Almorexant induces a robust antidepressant-like effect and the restoration of stress-related HPA axis defect independently from a neurogenic action. [2] In addition, Almorexant also reduces ethanol self-administration in high-drinking rodent models. [3] | ||||
| Features | Orally bioavailable orexin receptor antagonist that has been tested in Phase III clinical trials for treatment of Insomnia. |
Protocol (from reference)
| Animal Study:[1] |
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References
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Customer Product Validation
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Data from [Data independently produced by , , J Pharmacol Exp Ther, 2016, 358(3):492-501. ]
Selleck's Almorexant HCl has been cited by 6 publications
| Impaired microglial glycolysis promotes inflammatory responses after intracerebral haemorrhage via HK2-dependent mitochondrial dysfunction [ J Adv Res, 2024, S2090-1232(24)00359-X] | PubMed: 39142439 |
| Mouse parasubthalamic Crh neurons drive alcohol drinking escalation and behavioral disinhibition [ bioRxiv, 2024, 2024.07.06.602357] | PubMed: 39026704 |
| Cancer genes disfavoring T cell immunity identified via integrated systems approach [ Cell Rep, 2022, 40(5):111153] | PubMed: 35926468 |
| Brain Circuit of Claustrophobia-like Behavior in Mice Identified by Upstream Tracing of Sighing [ Cell Rep, 2020, 31(11):107779] | PubMed: 32553161 |
| Optogenetic identification of hypothalamic orexin neuron projections to paraventricular spinally projecting neurons. [ Am J Physiol Heart Circ Physiol, 2017, 312(4):H808-H817] | PubMed: 28159808 |
| Intrathecal Intermittent Orexin-A Causes Sympathetic Long-Term Facilitation and Sensitizes the Peripheral Chemoreceptor Response to Hypoxia in Rats. [Kim SJ, et al. J Pharmacol Exp Ther, 2016, 358(3):492-501] | PubMed: 27384072 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.