Samelisant

SKU: orb1297886

Description

Samelisant (SUVN-G3031) is a potent, selective inverse agonist of the histamine H3 receptor, exhibiting Kis of 8.7 nM (human) and 9.8 nM (rat). It demonstrates anticataplectic activity in vivo and is a valuable research tool for investigating narcolepsy and related sleep/wake disorders in both in vitro and in vivo experimental models.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1394808-82-2
• MW: 373.49
• Purity: 99.59% (May vary between batches)
• Formula: C₂₁H₃₁N₃O₃
• SMILES: O(C1CCN(CC1)C2CCC2)C3=CC=C(NC(CN4CCOCC4)=O)C=C3
• Target: Histamine Receptor
• Solubility: DMSO:50 mg/mL (133.87 mM)

Bioactivity

• In Vivo:
  In orexin knockout mice subjected to sleep EEG, Samelisant (10 and 30 mg/kg; p.o.) significantly increases wakefulness and concomitantly decreases NREM sleep. Samelisant significantly decreases direct REM sleep onset episodes and dose-dependently increases the level of tele-methylhistamine.
• In Vitro:
  Samelisant (1, 10, and 100 nM) increases the pEC50 from 8.5 to 8.2, 7.3, and 6.2 for human H3 receptor and from 8.2 to 7.9, 7.4, and 6.4 for rat H3 receptor, respectively. Samelisant modulates dopamine and norepinephrine levels in the cerebral cortex. Samelisant reversibly binds to the orthosteric site with Kbs of 1.3 nM and 1.1 nM.

Storage & Handling

• Storage: 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

H3 receptor, Histamine Receptor, HistamineReceptor, SUVN-G 3031, SUVN-G3031, SUVN-G-3031, Samelisant

Compound Identifiers

PubChem CID

60151477