Irdabisant

SKU: orb1696917

Description

Irdabisant (CEP-26401) is a potent, brain-penetrant H3 receptor inverse agonist with demonstrated in vivo efficacy, enhancing cognition and wakefulness in rodent models. It is a selective research tool for studying cognitive deficits associated with conditions like schizophrenia, showing low hERG channel affinity.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1005402-19-6
• MW: 313.39
• Purity: 99.96%
• Formula: C₁₈H₂₃N₃O₂
• SMILES: O(CCCN1[C@H](C)CCC1)C2=CC=C(C=C2)C=3C=CC(=O)NN3
• Target: Histamine Receptor
• Solubility: DMSO:22.5 mg/mL (71.8 mM)

Bioactivity

• Target IC50:
  H3 receptor (rat):7.2 nM (Ki)|H3 receptor (human):2 nM (Ki)
• In Vivo:
  Irdabisant (0.0001-0.1 mg/kg; i.v. or p.o.; single dosage) improves performance in the rat social recognition model of short-term memory. Irdabisant (0.01-0.3 mg/kg; p.o.; single dosage) dose-dependently inhibits H3R agonist RAMH-induced dipsogenia. Irdabisant (1 mg/kg for i.v. and 3 mg/kg for p.o.; single dosage) is rapidly absorbed with high oral bioavailability in rat and monkey, and exhibits a moderate clearance in monkey and dog compared to the rat. Irdabisant (3-30 mg/kg; p.o.; single dosage) exhibits wake-promoting activity in rat. Irdabisant (3-30 mg/kg; i.p.) increases prepulse inhibition (PPI) in DBA/2NCrl mice.
• In Vitro:
  Irdabisant exhibits inverse agonist activity with EC50 values of 2.0 nM and 1.1 nM for rat H3R and human H3R, respectively; exhibits antagonist activity with Kb, app values of 1.0 nM and 0.4 nM for rat H3R and human H3R, respectively. Irdabisant exhibits moderate activity at Muscarinic M2 (Ki = 3.7 ± 0.0 μM) and Adrenergic α1A (Ki = 9.8 ± 0.3 μM) receptors, Norepinephrine transporters (Ki = 10 ± 1 μM), Dopamine transporters (Ki = 11 ± 2 μM), and phosphodiesterase PDE3 (IC50 = 15 ± 1 μM). Irdabisant inhibits the cytochrome P450 enzymes CYP1A2, 2C9, 2C19, 2D6, and 3A4 with IC50 values of greater than 30 μM, indicating less potential for drug-drug interactions.

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

CEP 26401, CEP26401, CEP-26401, Irdabisant, H3 receptor, HistamineReceptor, Histamine Receptor

Compound Identifiers

PubChem CID

25070031