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Irdabisant

CAT: 0804-HY-109968-01Size: 5 mgDry Ice: NoHazardous: No
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CAT#:0804-HY-109968-01Size:5 mg
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Description
Irdabisant (CEP-26401) 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 has relatively low inhibitory activity against hERG current with an IC50 of 13.8 μM. Irdabisant has cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used to research schizophrenia or cognitive impairment[1][2].
CAS Number
1005402-19-6
Product Name Alternative
CEP-26401
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.html
Purity
99.38
Solubility
DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)
Smiles
C[C@H](CCC1)N1CCCOC2=CC=C(C(C=C3)=NNC3=O)C=C2
Molecular Formula
C18H23N3O2
Molecular Weight
313.39
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
Storage Conditions
-20°C, 3 years; 4°C, 2 years (Powder)
Scientific Category
Reference compound1
Clinical Information
Phase 1
Isoform
H3 Receptor