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Irdabisant

Catalog No. T32191 CAS 1005402-19-6

Synonyms: CEP-26401, CEP 26401, CEP26401

Irdabisant (CEP-26401) (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant antagonist/inverse agonist of histamine H3 receptor (H3R) (rat H3R Ki= 7.2 nM, human H3R Ki= 2.0 nM). Irdabisant exhibits relatively low inhibitory activity against hERG current (IC50= 13.8 μM). Irdabisant exhibits cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used for research on schizophrenia or cognitive impairment.

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Irdabisant, CAS 1005402-19-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 89.00
5 mg	In stock	$ 228.00
10 mg	In stock	$ 347.00
25 mg	In stock	$ 589.00
50 mg	In stock	$ 842.00
100 mg	In stock	$ 1,160.00
500 mg	In stock	$ 2,330.00
1 mL * 10 mM (in DMSO)	In stock	$ 158.00

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Purity: 99.77%

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Description	Irdabisant (CEP-26401) (CEP-26401) is a selective, orally active and blood-brain barrier (BBB) penetrant antagonist/inverse agonist of histamine H3 receptor (H3R) (rat H3R Ki= 7.2 nM, human H3R Ki= 2.0 nM). Irdabisant exhibits relatively low inhibitory activity against hERG current (IC50= 13.8 μM). Irdabisant exhibits cognition-enhancing and wake-promoting activities in the rat social recognition model. Irdabisant can be used for research on schizophrenia or cognitive impairment.
Targets&IC50	H3 receptor (human):2 nM (Ki), H3 receptor (rat):7.2 nM (Ki)
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[1].
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[1]. 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[2].

Synonyms	CEP-26401, CEP 26401, CEP26401
Molecular Weight	313.39
Formula	C18H23N3O2
CAS No.	1005402-19-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 22.5 mg/mL (71.79 mM)

References and Literature

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. 3. Josef KA, et al. Synthesis of constrained benzocinnolinone analogues of CEP-26401 (irdabisant) as potent, selective histamine H3 receptor inverse agonists. Bioorg Med Chem Lett. 2012 Jun 15;22(12):4198-202. 4. Becknell NC, et al. Synthesis and evaluation of pyridone-phenoxypropyl-R-2-methylpyrrolidine analogues as histamine H3 receptor antagonists. Bioorg Med Chem Lett. 2011 Dec 1;21(23):7076-80.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Clinical Compound Library Anti-Cancer Drug Library GPCR Compound Library Clinical Compound Library Bioactive Compounds Library Max Bioactive Compound Library Neuronal Signaling Compound Library

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Keywords

Irdabisant 1005402-19-6 GPCR/G Protein Immunology/Inflammation Neuroscience Histamine Receptor CEP-26401 CEP 26401 CEP26401 inhibitor inhibit

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