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Irdabisant (hydrochloride)

CAT: 0804-HY-109968ASize: 1 EachDry Ice: NoHazardous: No
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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].
CAS Number
1005398-61-7
Product Name Alternative
CEP-26401 (hydrochloride)
UNSPSC
12352005
Target
Histamine Receptor
Type
Reference compound
Related Pathways
GPCR/G Protein; Immunology/Inflammation; Neuronal Signaling
Applications
Neuroscience-Neuromodulation
Field of Research
Neurological Disease
Assay Protocol
https://www.medchemexpress.com/irdabisant-hydrochloride.html
Solubility
10 mM in DMSO
Smiles
C[C@H](CCC1)N1CCCOC2=CC=C(C(C=C3)=NNC3=O)C=C2.[H]Cl
Molecular Formula
C18H24ClN3O2
Molecular Weight
349.86
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
H3 Receptor

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