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Product Description
– Irdabisant (CEP-26401) hydrochloride is a selective, orally active and blood-brain barrier (BBB) penetrant histamine H3 receptor (H3R) inverse agonist/inverse agonist with Ki values of 7.2 nM and 2.0 nM for rat H3R and human H3R, respectively. Irdabisant hydrochloride has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant hydrochloride has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant hydrochloride can be used to research schizophrenia or cognitive impairment[1][2].
Web ID
– HY-109968A
Shipping
– Room temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C18H24ClN3O2
References
– [1]Hudkins RL, et al. Discovery and characterization of 6-{4-[3-(R)-2-methylpyrrolidin-1-yl)propoxy]phenyl}-2H-pyridazin-3-one (CEP-26401, irdabisant): a potent, selective histamine H3 receptor inverse agonist. J Med Chem. 2011 Jul 14;54(13):4781-92.|[2]Raddatz R, et al. CEP-26401 (irdabisant), a potent and selective histamine H₃ receptor antagonist/inverse agonist with cognition-enhancing and wake-promoting activities. J Pharmacol Exp Ther. 2012 Jan;340(1):124-33.
CAS Number
– 1005398-61-7
Molecular Weight
– 349.86
SMILES
– C[C@H](CCC1)N1CCCOC2=CC=C(C(C=C3)=NNC3=O)C=C2.[H]Cl
Clinical Information
– Phase 1
Research Area
– Neurological Disease
Solubility
– 10 mM in DMSO
Target
– Histamine Receptor
Isoform
– H3 Receptor
Pathway
– GPCR/G Protein;Immunology/Inflammation;Neuronal Signaling
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
