Almorexant free base · Synonyms: ACT-078573

Almorexant is an orally active, potent and competitive dual orexin receptor antagonist.

For research use only. Not for human or veterinary use.

Target Orexin Receptor (OX Receptor) Calcium Channel Caspase Apoptosis

Research area Neurological Disease Endocrinology Cancer

Purity >99% Stock Inquire

Data Sheet SDS COA

Almorexant structure

CAS No.: 871224-64-5

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
25 mg	USD 315.00	BP-02093-25mg	In stock	Get quote
50 mg	USD 504.00	BP-02093-50mg	In stock	Get quote
100 mg	USD 806.00	BP-02093-100mg	In stock	Get quote
250 mg	USD 1,580.00	BP-02093-250mg	In stock	Get quote
500 mg	USD 2,580.00	BP-02093-500mg	In stock	Get quote
1 g	USD 4,130.00	BP-02093-1g	In stock	Get quote
2 g	Inquire	BP-02093-2g	In stock	Inquire

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Description

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].

Biological activity

In Vitro Almorexant (1 μM) promotes tyrosine phosphorylation of SHP2/OX1R complex. Almorexant (1 μM) inhibits the cellular growth of AsPC-1 cells. In Vivo Almorexant (1.8 μmol/kg, 100 μL; IP, daily) reduces the volume of tumors. Almorexant (300 mg/kg, PO, once) can help rats to be fully capable of spatial and avoidance learning. 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.

Identifiers

SMILES: CNC(=O)[C@H](N1CCC2=C(C=C(OC)C(OC)=C2)[C@H]1CCC1=CC=C(C=C1)C(F)(F)F)C1=CC=CC=C1
InChIKey: DKMACHNQISHMDN-SHQCIBLASA-N

Specifications

MW (average): 512.5632
Formula: C₂₉H₃₁F₃N₂O₃
CAS No.: 871224-64-5
Physical state: Solid
Color: white to off-white
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder 4℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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.

[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.

[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.

[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.

Same target

Search Orexin Receptor (OX Receptor)

Same research area

Search Neurological Disease