Almorexant hydrochloride

SKU: orb1688486

Description

Almorexant hydrochloride is an orally bioavailable dual orexin receptor antagonist that inhibits intracellular Ca2+ signaling. It has been used in sleep research to study orexin's role in arousal and has shown effects in reducing methamphetamine-induced excitatory responses in both in vitro and in vivo models.

Research Area

Cell Biology, Metabolism Research, Neuroscience, Pharmacology & Drug Discovery, Protein Biochemistry

Key Properties

• CAS Number: 913358-93-7
• MW: 549.02
• Purity: 99.85% (May vary between batches)
• Formula: C₂₉H₃₂ClF₃N₂O₃
• SMILES: C(CC1=CC=C(C(F)(F)F)C=C1)[C@H]2C=3C(=CC(OC)=C(OC)C3)CCN2[C@@H](C(NC)=O)C4=CC=CC=C4.Cl
• Target: Calcium Channel,Others,OX Receptor,Apoptosis,Caspase
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.64 mM);Ethanol:48 mg/mL (87.43 mM);DMSO:40 mg/mL (72.86 mM);H2O:< 0.1 mg/mL (insoluble)

Bioactivity

• Target IC50:
  OX1:1.3 nM(ki)|OX2:0.17 nM(ki)
• In Vivo:
  Daily intraperitoneal injection of Almorexant hydrochloride (1.8 μmol/kg) at day 0 in mice xenografted with AsPC-1 cells and up to the mice sacrifices resulted in a significant decrease in tumor volume (> 50%), as compared to untreated mice. Treatment with Almorexant hydrochloride started after AsPC-1 tumors were developed, rapidly and strongly reduced the volume of established tumors. OX1R expression revealed by immunodetection was not affected by Almorexant hydrochloride treatment.
• In Vitro:
  AsPC-1 cells preincubated or not with the SHP2 inhibitor NSC-87877 (50 μM) were challenged for 5 min without or with 1 μM orexin-A or 1 μM Almorexant hydrochloride. In parallel, HPAF-II cells were also challenged for 5 min without or with 1 μM orexin-A. Orexin-A and Almorexant hydrochloride promote tyrosine phosphorylation of SHP2/OX1R complex.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, orexin, Orexin Receptor (OX Receptor), Orexin-RA-1 hydrochloride, OX Receptor, OX1, OX2, pancreatic cancer, Pancreatic ductal adenocarcinoma, PDAC, narcolepsy, hypocretin, Hypocretin Receptor, GPCR, HPAF-II cells, HCRT Receptor, A 573 hydrochloride, ACT 078573, ACT 078573 hydrochloride, ACT078573, ACT-078573, ACT078573 Hydrochloride, ACT-078573 hydrochloride, Almorexant, Almorexant HCl, Ca channels, Calcium Channel, Ca2+ channels, Caspase, Apoptosis, AsPC-1 cells, Cataplexy

Compound Identifiers

PubChem CID

25227440